Journal Paper

Abstract:
Elham N.Al-Kaisi; Manal A.Habib; Layla S.Al-Omer Iraqi J.of Med.Sciences 3,3,2004




Al-Kaissi E, " Value and limitation of several commonly used epidemiologic typing methods for Pseudomonas aeruginosa " , "European J of scientific research",Vol.11,No., EJSR, UK, 04/11/2005 Abstract:
This study was designed to assess the value and limitation of several epidemiologic typing methods for investigation of outbreaks due to Pseudomonas aeruginosa and the effect of antimicrobial treatment on the value of these methods in differentiating 58 isolateof Pseudomonas aeruginosa recovered from varios clinical samples from 29 hospitalized patients in medical city hospital / Baghdad / Iraq during 15 months period, encompassing all patients at the hospital from where Pseudomonas aeruginosa was isolated. All isolates (58 isolates from 29 patients before and after antimicrobial treatment) were examined for their antibiogram, biochemical activities, pyocin typing and serotype patterns. The results show a high antimicrobial resistance to some β-lactams, chloramphenicol, tetracycline and cefalotin, among the isolated stains. The isolated strains were classified as multi-drug resistant. The result indicates that 69% of the isolates undergo changes in their serotyping and 72.4% in their pyocin typing respectively and there were considerable changes in their biogram when comparing the pre and post antimicrobial therapy isolates. The major antimicrobial agent used for treatment at the time of investigation was gentamicin (40%) and treatment was started on non rational quests. The results suggested that the common methods used for typing Ps.aerugenosa strains did not clearly differentiate between clinically-related and epidemiologically unrelated isolates if antimicrobials were initiated, thus tracing the source that could contributed to Ps. aerugenosa hospital acquired infections is difficult after antimicrobial treatment is started.




Abstract:
Al-Mustansirya J. of pharmaceutical sciences ,2 (2005): 1-5




Azhar AF. Al-Aattraq, " Rapid diagnosis of systemic candidiasis by latex particle " , "Ruropean journal of scientific research ",Vol.12,No.1, Eurojournals.com , UK, 04/06/2005 Abstract:
Systemic candidiasis remains a major cause of disease and death, particularly among patient suffering from hematological malignancies, and it presents both diagnostic and therapeutic problems. The diagnosis of most cases of systemic Candidiasis is usually based on isolation of candida species from blood cultures or tissue biopsy, both are invasive, impracticable, time consuming procedures and may delay initiating appropriate treatment leading to high mortality rate. For rapid diagnosis of systemic Candidiasis in immunocompromized patients a serological diagnosis based on detection of circulating antibody was developed by preparing a suitable slide latex particle assay kit. A cytoplasmic antigen of Candida albicans was prepared, and used to sensitize latex particles, these particles were used to detect antibodies to C. albicans cytoplasmic antigen in 30 serum samples from immunocompromized patients and in other 20 serum samples from normal individuals (negative control group). The results were compared with the blood culture results for the same patients. Sensitized serum was prepared by subcutaneous injection of the cytoplasmic antigen into rabbit, and used as a positive control. C. albicans was isolated from 2 patients (6.7%) using blood culture technique, while the prepared latex particle agglutination test gave positive results in 14 patient serum samples (46.7%).The 50% positively still to the dilution of 1:16 of each serum. These results indicate that latex agglutination test using C. albicans cytoplasmic antigen to sensitize the latex is a reliable test for rapid diagnosis of systemic Candidiasis in patients with malignancies. Key words: Candida albicans, cytoplasmic antigen, latex agglutination test, systemic Candidiasis, Hospital acquired infections. Download




E. N. Al-Kaissi, M M, " Aetiology and epidemiology of sever infantile diarrhoea in Bagdad, Iraq " , "European Journal of Scientific Research",Vol.14,No.3, Eurojournals.com, UK, 04/03/2006 Abstract:
The epidemiology and aetiology of acute diarrhoeal dehydration in a group of 200 infants less than two years of age in Baghdad / Iraq were studied. Infants at the age of 7 to 12 months were found to be at grater risk of acquiring diarrhoea. Stool specimens were analyzed using, microscopy, routine bacteriological analysis including culture for enteropathogens, enterotoxin bioassay, and enzyme linked immunosorbent assay (ELISA) for rotavirus detection. Rotavirus was the most frequent enteric pathogen isolated (29.5%) followed by Enteropathogenic Escherichia coli (EPEC) then Campylobacter. Rotavirus and other enteric pathogens infections were more prevalent during summer. In about 47.5% of the cases, antimicrobial agent was used prior to admission to hospital. A symptomatic carriage of Salmonella, Campylobacter, EPEC, Giardia, Entameba were detected in less than 5% of cases. Oral rehydration therapy proved to be simple, safe and effective for acute diarrhoeal dehydration if prepared correctly Key words: Aetiology, diarrhea, dehydration, Gastroenteritis, enteric pathogens, Rotavirus Download




Abstract:
Journal of Arab Universities for Basic and Applied sciences, 6 (2008) 47-55




Jinan A. Al-Qaisi a,, " Synthesis and anti-inflammmatory activities of noval salicylic acid and diflunisal amide derivatives " , "Arabian J of Chemistry ",Vol.in press,No.in press, Elsevier, Suadia, 05/11/2009 Abstract:
Abstract Aminoacetylenic isoindoline-1,3-dione derivatives were synthesized from the reaction of potassium phthalimide with propargyl bromide to generate 2-(prop-2-yn-1-yl)isoindoline-1,3-dione (ZM1). Treatment of 2-(prop-2-yn-1-yl)isoindoline-1,3-dione with appropriate cyclic amines through Mannich reaction yielded five desired aminoacetylenic isoindoline-1,3-diones called, ZM2–ZM6. The IR, NMR and elemental analysis were consistent with the assigned structures. These synthetic compounds, except ZM6, produced significant (p< 0.05–0.01) dose-related inhibition of carrageenan-induced edema in rats following 3 and 5 h post-oral administration of 5, 10, and 20 mg/kg doses. The percent inhibition of edema varied between the compounds at 10 mg/kg dose being ZM3 >ZM5 > ZM4> ZM2. These percent inhibitions for ZM3 and ZM5 were not significantly different than those of induced by Ibuprofen, Diclofenac and Celecoxib. At 20 mg/kg dose, ZM4 produced a statistically significant reduction of inflammation (p< 0.01) 1 h following administration and persisted for 5 h. Furthermore, all the compounds showed inhibition of COX-1 and COX-2 with maximum inhibition at 5 lM. However, the inhibition values were less than Diclofenac Download




Zuhair Muhi-eldeen, , " Acute toxicological studies on the extract of Iraqi Peganum harmala in rats " , "European Journal of Scientific Research",Vol.22,No.4, Eurojournals.com, UK, 06/11/2008 Abstract:
Acute toxicological studies of the aqueous extract of Iraqi Peganum harmala in rats were conducted. The LD50 value of the extract in rats given intramuscularly was 420 mg/kg. Tremor and convulsion were observed in most of the treated rats specially those given large dose. These toxic signs are probably due to the alkaloids content of the extracts which have a central nervous system stimulant effects. Histological examination of organs and tissues of treated rats were normal indicating that the extract has a low level of toxicity: However, sever local inflammatory reaction in the muscles at the site of injection was observed which caused a significant increase in the counts of leucocytes and neutrophil. This indicates that the intramuscular route is not a proper route of administration. Keywords: Peganum harmala, Acute and subacute toxicity. Download




Elham Al-kaissi and , " Pathogenicity of Blastocystis hominis in relation to entropathogens in Gastroenteritis cases in Baghdad " , "European Journal of Scientific Research",Vol.25,No.4, Eurojournals.com, UK, 03/10/2009 Abstract:
Blastocystis hominis was considered to be a member of normal intestinal flora in the past; recently it has been accepted as a controversial pathogen. In this study 200 stool specimens of patients suffering from gastroenteritis were studies by applying direct microscopic stool examination and culture. 67% of these specimens showed single entropathogen, 20% mixed and 12% were negative. These results were significant when compared with control specimens. No mixed bacterial and fungal or mixed bacterial alone were identified. As B. hominis is receiving increased attention as potential causative agent for diarrhoea, the role of this protozoon in relation to other pathogens in diarrhoeal disease in Baghdad area was investigated. Eighty two individuals whose stool examination revealed B. hominis were evaluated for clinical symptoms.12% of the cases were mixed infections with other organisms, where as 29% were infected with B. hominis only, on both occasion B. hominis showed significant relation to the presence of blood, leucocytes, and stool consistency of the specimens investigated. Metronidazole was administered for 10 days to the patients infected with B. hominis. At the end of treatment, the investigation was repeated and stools examination gave negative results for B. hominis. Keywords: Blastocystis hominis, Gastroenteritis, Metronidazole, pathogenicity. Download




Abstract:
Some reaction of Influenza viruses adsorbed to polystyrene for ELISA E. Al-kaissi, A. Mostratos J.Virol.Meth. ,4,353-358(1982)




Abstract:
Assessment of Substrates for horseredish Peroxidase J. Immunol.Meth.,58,227-232 (1983)




Abstract:
Preparation &properties of Vibrio cholerae antifimbrial antibody J. Appl. Bact.58, 221-229 (1985)




Abstract:
Sulphamethaxol Sensitive strains among multiple antibiotics resistant Staph.aureus E.Al-Kaissi, S. Salih, L. Al-omer Scient. Nurs. J ,4 (2),78-97 (1988)




Abstract:
Bact. evaluation of scrub technique in the operating room E. al-kaissi, Shaio J, Alwash,F Scien.Nurs.J. ,5,5- 26 (1989)




Abstract:
The role of Blast. hominis in relation to entoropathogen in Iraq. Al-kaissi, Magdi,K. Iraqi J. Pharm.Scien.,2(2),33-43 (1989




Al-kaissi E N 1, Al-, " Synthesis and antimicrobial evaluation of 4,5-diaryl-2-[4-(t-amino)-2-butynyl]-2,4-dihydro-3H- " , "medicinal chemistry research ",Vol.in press,No.in press, springer, germany, 11/07/2011 Abstract:
A series of 4,5-diaryl-2-[4-(t-amino)-2-butynyl]-2,4-dihydro-3H-1,2,4-triazol-3-ones were synthesized and characterized by infrared spectrum (IR), 1H-NMR spectra and elemental analyses. Investigation of their antimicrobial activity was performed. Antimicrobial activity profile of the title compounds were evaluated against Gram positive bacteria, Gram negative bacteria and fungi. The synthesized compounds displayed different degrees of antimicrobial activities as shown in Table III. Compound 12 was the most active one. This may be attributed to 4,5-diphenylsubstituent on the triazoline-3-one ring and the nature of the amino groups at terminal acetylenic moiety. Download




Najah Al- Muhtaseb 1, " The role of Human xanthine oxidoreductase (HXOR), anti-HXOR antibodies and microorganisms in synovial fluid of patients with joint inflammation " , "rheumatology international ",Vol.in press,No.in press, springer, Germany, 10/03/2011 Abstract:
Objectives: This work is to investigate the levels of human xanthine oxidoreductase (HXOR), its antibodies and microorganisms in synovial fluid of patients with untreated rheumatoid joint diseases and to assess a possible relationship between severity of the inflammatory condition and the level of anti-XOR titers. Methods: Synovial fluids were collected from sixty four patients with rheumatoid joint diseases who had not been treated with corticosteroid or disease modifying antirheumatic drugs prior to study. Sixty four age matched individuals were included as control. XOR proteins level and anti XOR antibodies were determined in the blood and synovial fluid, using human XOR as antigen, by enzyme linked immunosorbent assay (ELISA technique). C-reactive protein, ESR and rheumatoid factors were measured in patient's blood, and were culture for bacteria and fungi. Results: The titers of XOR protein in the synovial fluid of patients with rheumatoid arthritis were 90.43 ± 23.37 µg/ml (mean ± SD, n=29) and up to 62.42 ± 8.74 µg/ml (mean ± SD, n=35) in other joint inflammation. Anti-HXOR antibodies titers in patients were (167.72 ± 23.64 µg/ ml, n= 64) which was significantly higher in rheumatoid arthritis patients compared to patients with other joint inflammations. No microorganisms were detected. Conclusions: A good correlation was found between the severity of the disease and the levels of HXOR protein. In contrast, it seems that anti-HXOR antibodies in synovial fluids have a protective role as high concentrations against XOR were detected in inflammatory arthritis. These antibodies play role in eliminating XOR from synovial fluids (positive role). However, immune complex formation could activate complement and participate in propagating the inflammatory cycle. Synovial aspirate Ordinary microbial cultures were negative for any bacteria or fungi but that does not exclude organisms of special culture requirements. Download




Zuhair Muhi-eldeen, , " Synthesis and pharmacological evaluation of N-[4-(t-amino)-2-butynyloxy] phthalimides " , "issn:2250-3013",Vol.2,No.1, iosr/pharm, international, 01/15/2012 Abstract:
A series of aminoacetylenicoxyphthalimide namely N-[4-(t-amino)-2-butynyloxy] phthalimides were synthesized from the reaction of N-hydroxyphthalimide with propargyl bromide in sodium ethoxide to generate N-(2-butynyloxy)phthalimide. The desired compounds were prepared through Mannich reaction of N-(2-butynyloxy)phthalimide with formaldehyde, appropriate amine in peroxide-free dioxin and cuprous chloride as catalyst. The N-[4-(t-amino)-2-butynyloxy] phthalimides were investigated for their rectal temperature, motor activity and palpebral pitosis effects in comparison with harmaline, all compounds showed similar activity to harmaline, however compound 4 was more potent than harmaline. Download




Zuhair A Muhi-eldeen, " Synthesis and biological evaluation of N1,N2-bis-[4-(t-amino)-2-butynyl]phthalamides " , "Medicinal chemistry research ",Vol.22,No.4, Springer , Germany, 02/01/2013 Abstract:
A series of N1,N2-bis-[4-(t-amino)-2-butynyl]phthalamides have been synthesized and investigated for the blocking of the motor effect of oxotremorine in intact mice and for their antagonistic activity towards acetylcholine on isolated guinea-pig ileum preparations. All N1,N2-bis-[4-(t-amino)-2-butynyl]phthalamides showed more selectivity as oxotremorine antagonists than atropine and less potent than atropine on peripheral cholinergic antagonistic activity. Powered by Download




Muhi-eldeen, Z., Jum, " Antimicrobial activity of some new oxadiazole derivatives " , "Jordan journal of chemistry ",Vol.3,No., Al-yarmouk university , Jordan , 04/03/2008 Abstract:
Muhi-eldeen, Z., Juma'a, G., Al-Kaissi, E., Nouri, L Jordan J. of Chemistry. 2008; 3: 233-243




Najah Al- Muhtaseb 1, " Dyslipidemia and Xanthine Oxidoreductase level in Jordanian Patients with Rheumatoid Arthritis " , "European Journal of Scientific Research ",Vol.99,No.1, EJSR, UK, 04/08/2013 Abstract:
Context: Rheumatoid arthritis (RA) is associated with an excess mortality from cardiovascular disease which might be due to an increased prevalence of cardiovascular risk factors such as dyslipidemia, and free radical generating enzyme such as xanthine oxidoreductase (XOR). Thus, they appear to be suitable markers for clinical studies of lipid profile and XOR level in patient with RA and related cardiovascular risk. Objectives: of the study were to assess the prevalence of blood dislipidemia and the levels of blood and synovial XOR in Jordanian patients with untreated active rheumatoid joint diseases and to investigate the clinical and biological associated factors. Methods: Synovial fluids and blood were collected from one hundred twenty seven patients with active RA (63 male and 64 female). One hundred eleven age matched individuals were included as control. Blood lipid profile, apolipoproteins (Apo), blood and synovial XOR proteins level were determined. Results: the levels of patient serum cholesterol (C), low density lipoprotein (LDL)-Cholesterol, Apo B, triglyceride (TG), very low density lipoprotein (VLDL-TG), LDL-TG, Apo C-III, Apo C-III/TG, Apo B/Apo A-I, and LDL-C/high density lipoprotein (HDL)HDL2-C ratios were significantly increased in RA patients. A significant reduction in the levels of HDL-, HDL2-, HDL3-C, serum Apo A-I, ApoA-II, HDL-Apo A-I, and HDL2-C/HDL3-C ratio were found in RA patients compared to healthy controls. Increased XOR in serum and synovial fluid were observed in the RA patients studied. . Conclusions: Abnormalities in lipids, lipoproteins, apolipoproteins and XOR were found in RA patients. Our data favor an enhanced affinity towards atherosclerosis in these patients. Management of dyslipidemia should consider as a part of cardiovascular risk management in RA patients. Attention must be paid to lipids profile for those RA patients with previous history of a cardiovascular event. Download




ibrahim Al- Adham, H, " studies on the kinetics of killing and proposed mechanism of action of microemulsions against fungi " , "International J of Pharmaceutics",Vol.454,No., Elsevier , UK , 01/01/2013 Abstract:
Microemulsions are physically stable oil/water clear dispersions, spontaneously formed and thermodynamically stable. They are composed in most cases of water, oil, surfactant and cosurfactant. Microemulsions are stable, self-preserving antimicrobial agents in their own right. The observed levels of antimicrobial activity associated with microemulsions may be due to the direct effect of the microemulsions themselves on the bacterial cytoplasmic membrane. The aim of this work is to study the growth behaviour of different microbes in presence of certain prepared physically stable microemulsion formulae over extended periods of time. An experiment was designed to study the kinetics of killing of a microemulsion preparation (17.3% Tween-80, 8.5% n-pentanol, 5% Isopropyl myristate and 69.2% sterile distilled water) against selected test microorganisms (Candida albicans, Aspergillus niger, Schizosaccharomyces pombe and Rhodotorula spp). Secondly, an experiment was designed to study the effects of the microemulsion preparation on the plasma membrane structure and function of selected fungal species by observation of 260nm component leakage. Finally, the effects of the microemulsion on the fungal membrane structure and function using S. pombe were studied using transmission electron microscopy. The results showed that the prepared microemulsions are stable, effective antimicrobial systems with effective killing rates against C. albicans, A. niger, S. pombe and Rhodotorula spp. The results indicate a proposed mechanism of action of significant anti-membrane activity, resulting in the gross disturbance and dysfunction of the plasma membrane structure which followed by cell wall modifications, cytoplasmic coagulation, disruption of intracellular metabolism and cell death. Download




Elham Al-Kaissi 1?, , " The influence of adding antibiotic in treatment of rheumatoid arthritis patients on Streptococcus pyogenes carrier rate and on the lipids profile " , "International journal of pharmacy and pharmaceutical sciences",Vol.7,No.2, Academic Sciences, , 02/08/2015 Abstract:
Objective: The main goal is to evaluate the clinical efficacy, safety, and tolerability of antibiotics and methotrexate (MTX) treatment on the disease severity, on Streptococcus pyogenes carrier rate and on the lipid profile of patients with rheumatoid arthritis (RA). Methods: In a 6-months, double –blind trial, 130 patients with active RA were treated for four weeks with MTX therapy at a stable low dose of 12.5 mg/week instructed to receive either levofloxacin (500 mg) or placebo orally once daily while continuing to receive MTX. Before and after the treatment, disease activity parameters, rheumatoid factor (CF), C reactive protein (CRP), anti-streptolysin O (ASO) titer and lipid profile were measured. Throat swab cultures were done on suitable medium. Results: Antibiotic adds to treatment causes a significant reduction in disease activity, lower the side effects and concomitant decrease in MTX treatment dose, most of the lipid levels had returned to baseline levels, decreased S. pyogenes carrier rate from 25-30% to 3.2-6% and lower ASO titers to undetectable. Conclusion: RA patients who are treated with MTX, addition of antibiotics lower the signs, symptoms and risk factors of RA patient and S. pyogenes could be important in the etiopathogenesis of RA Download




Muhi-eldeen, Z., Jum, " Antimicrobial activity of some new oxadiazole derivatives " , "Jordan journal of chemistry ",Vol.3,No., Al-yarmouk university , Jordan , 04/03/2008 Abstract:
Alkyl, alkenyl, sulfonyl, thiocarbamates and Mannich derivatives were synthesized and characterized through IR, NMR, and Elemental analysis. It is of interest to report the isomerization rearrangement of propynyl to allene group in Mannich reaction under basic condition. The most promising compound as antibacterial agent was 5-(pyridyl)-1, 3, 4-oxadiazole-2-benzylthiocarbamates. Download




ibrahim Al- Adham, H, " studies on the kinetics of killing and proposed mechanism of action of microemulsions against fungi " , "International J of Pharmaceutics",Vol.454,No., Elsevier , UK , 01/01/2013 Abstract:
Microemulsions are physically stable oil/water clear dispersions, spontaneously formed and thermodynamically stable. They are composed in most cases of water, oil, surfactant and cosurfactant. Microemulsions are stable, self-preserving antimicrobial agents in their own right. The observed levels of antimicrobial activity associated with microemulsions may be due to the direct effect of the microemulsions themselves on the bacterial cytoplasmic membrane. The aim of this work is to study the growth behaviour of different microbes in presence of certain prepared physically stable microemulsion formulae over extended periods of time. An experiment was designed to study the kinetics of killing of a microemulsion preparation (17.3% Tween-80, 8.5% n-pentanol, 5% Isopropyl myristate and 69.2% sterile distilled water) against selected test microorganisms (Candida albicans, Aspergillus niger, Schizosaccharomyces pombe and Rhodotorula spp). Secondly, an experiment was designed to study the effects of the microemulsion preparation on the plasma membrane structure and function of selected fungal species by observation of 260nm component leakage. Finally, the effects of the microemulsion on the fungal membrane structure and function using S. pombe were studied using transmission electron microscopy. The results showed that the prepared microemulsions are stable, effective antimicrobial systems with effective killing rates against C. albicans, A. niger, S. pombe and Rhodotorula spp. The results indicate a proposed mechanism of action of significant anti-membrane activity, resulting in the gross disturbance and dysfunction of the plasma membrane structure which followed by cell wall modifications, cytoplasmic coagulation, disruption of intracellular metabolism and cell death. Download




MARIAM AL-JOMAILY1, , " SYNTHESIS OF AMINO ACETYLENIC BENZOPHENONE DERIVATIVES AS H3-ANTAGONISTS " , "",Vol.,No., , , 02/28/1915 Abstract:
Objective: To synthesize new amino acetylenic benzophenone derivatives with significant H3-antagonist’s activity. Methods: Amino acetylenic benzophenone derivatives were synthesized from the reaction of 2-hydroxybenzophenone with 3-bromoprop-1-in to generate 2-(prop-2-yn-1-yloxy)-1,3-benzophenone (AZ-1). A mixture of 2-(prop-2-yn-1-yloxy)-1,3-benzophenone, paraformaldehyde, cyclic amine, cuprous chloride (catalytic amount) in peroxide free dioane through Mannich reaction yielded the designed amino acetylenic benzophenone derivatives (AZ-2-7). Results: The IR, H1-NMR, 13C NMR, and elemental analysis were consistent with the assigned structures. The designers of these compounds as H3-antagonists were based on the nationalization of the important criteria that provide effective inhibitory binding with H3-receptor. Molecular docking results of compounds (AZ-2-7) showed a good H3-receptor antagonistic activity relative to thioperamide of-6% (kcal/mol) especially AZ-2 which has-8.6 (kcal/mol). Conclusion: Docking results provide a good lead to designing more effective H3 antagonists in managing many CNS diseases like Alzheimer, epilepsy, depression, schizophrenia and many others. Keywords: Amino acetylenic benzophenone derivative, CNS diseases, H3-antagonist activity, Molecular docking Download




MARIAM AL-JOMAILY1, , " SYNTHESIS OF AMINO ACETYLENIC BENZOPHENONE DERIVATIVES AS H3-ANTAGONISTS " , "international journal of pharmacy and pharmaceutical sciences ",Vol.7,No.6, Academic Sciences, India, India , 02/28/2015 Abstract:
Objective: To synthesize new amino acetylenic benzophenone derivatives with significant H3-antagonist’s activity. Methods: Amino acetylenic benzophenone derivatives were synthesized from the reaction of 2-hydroxybenzophenone with 3-bromoprop-1-in to generate 2-(prop-2-yn-1-yloxy)-1,3-benzophenone (AZ-1). A mixture of 2-(prop-2-yn-1-yloxy)-1,3-benzophenone, paraformaldehyde, cyclic amine, cuprous chloride (catalytic amount) in peroxide free dioane through Mannich reaction yielded the designed amino acetylenic benzophenone derivatives (AZ-2-7). Results: The IR, H1-NMR, 13C NMR, and elemental analysis were consistent with the assigned structures. The designers of these compounds as H3-antagonists were based on the nationalization of the important criteria that provide effective inhibitory binding with H3-receptor. Molecular docking results of compounds (AZ-2-7) showed a good H3-receptor antagonistic activity relative to thioperamide of-6% (kcal/mol) especially AZ-2 which has-8.6 (kcal/mol). Conclusion: Docking results provide a good lead to designing more effective H3 antagonists in managing many CNS diseases like Alzheimer, epilepsy, depression, schizophrenia and many others. Keywords: Amino acetylenic benzophenone derivative, CNS diseases, H3-antagonist activity, Molecular docking. Download




ZUHAIR MUHI-ELDEEN1?, " ACETYLENIC DIMERIZATION UNDER BASIC CONDITIONS " , "international Journal of pharmacy and pharmaceutical science ",Vol.7,No.8, Academic Sciences, India, India , 06/01/2015 Abstract:
Objective: The lack of information concerning the pharmacological activity of aminoacetylenic amide derivatives in which the cyclic amine is aziridine or azetidine promoted our interest to synthesize N-[4-(1-azeridinyl)-2-butynyl]pyrrolide-1,3-dione 4, N-[4-(1-azetidinyl)-2-butynyl]pyrrolidine-1,3-dione 5 and N-[4-(1-pyrrolidnyl)-2-butynyl]pyrrolide-1,3-dione 6. Methods: Melting points, IR, 1H-NMR 13 CNMR spectra were measured. Results: Dimerization of 2-(prop-2-yn-1-yl)pyrrolidine-1,3-dione was generated rather than Mannich product, while using pyrrolidine as base in Mannich reaction generated the expected Mannich product. Rationalization for the mechanism of dimerization and Mannich adduct are discussed. Conclusion: Mannich reaction may afford the dimerization product of the acetylenic compounds rather than Mannich adduct. Download




Zuhair Muhi-eldeen1*, " CYCLOPRPAN FORMATION VERSUS SIGMATROPIC REARRANGE PRODUCTS IN ETHYLDIAZACETATE ADDITION TO ALLYLTHIOTETRAPYRAN " , "European journal of Pharmaceutical and Medical researchy",Vol.2,No.5, EJPMR, UK, 09/03/2015 Abstract:
During the course of our investigation to the synthesis of 2-(2'-tetrahydropyranyl thio) methyl-1-carboxycyclopropane through the cyclic addition of 2-allythiotetropyran with ethyldiazoacetate results in cyclopropane derivatives in cis and trans form in addition to sigmatropic rearrangement of 1,3 and 1,5 shift were obtained. Conformation of the structure of cyclopropane, sigmatropic rearrange products is confirmed through elemental analysis, IR, NMR and MP. The mechanisms of sigmatropic arrangement are discussed. Download




Abstract:
The synthesis and structural elucidation of α-amino-N-phenylsuccinimide through the IR, hNMR, ORD, and elemental analysis was described as precursor to thionimides, L-(S)-aspartic acid served as starting material and was utilized to investigate routes applicable to the synthesis of α-amino-N-phenyls Download




Abstract:
Objective: The main goal is to evaluate the clinical efficacy, safety, and tolerability of antibiotics and methotrexate (MTX) treatment on the disease severity, on Streptococcus pyogenes carrier rate and on the lipid profile of patients with rheumatoid arthritis (RA). Methods: In a 6-months, doubl Download




Abstract:
Objective: A new series of 2-{4-(t-amino)-2-(but-2-yn-1-yl)}-1,3-benzothiazole derivatives, 2-[4-(pyrrolidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ2), 2-[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ3), 2-[4-(piperidin-1-yl) but-2-yn-1-yl]-1,3-benzothiazole (BZ4), 2-[4- (azepan Download




Abstract:
Objective: This study aim to investigate the levels of oxidative stress, antioxidants besides uric acid, C-reactive protein (CRP), lipid profile and cardiac biomarker enzymes in young men admitted to the hospital for the first time with acute myocardial infarction (AMI), to investigate any Relations Download




Abstract:
Objective: Increasing use of medicinal plants in the treatment of infectious diseases are due to the development of multi-antibiotics resistant microorganisms, and had alerted our interest in the examination of some natural products. This study was carried out to investigate the antimicrobial acti




Abstract:
Objective: To determine the time needed for killing different types of microorganisms by a newly synthesized 2-mercapto-1,3-benzothiazole derivative in comparison to ciprofloxacin and fluconazole. Methods: The minimum bactericidal concentration (MBC) and minimum fungicidal concentration (MFC) for 2




Abstract:
The objectives are to synthesize of 2-mercaptobenzoxazole derivatives with amino acetylenic side chain as new and possibly with excellent antimicrobial agents, to reach structural selectivity of higher antifungal activity without or low antibacterial interference. A new series of 2-{[4-(t-amino-1




Abstract:
Objective: The aim of this study was to design and synthesize new amino acetylenic 5-ethoxy-2-mercaptobenzimidazole derivatives as potential antimicrobial agents. Methods: New series of 5-ethoxy-2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1H-benzimidazole derivatives were synthesized by Mannich




Abstract:
Objective: To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents. Methods: A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate




Abstract:
The aminoacetylenicoxyquinazoline were synthesized and their structures were confirmed through Infra-Red (IR), Proton Nuclear Magnetic Resonance (1H-NMR), Carbon-13 Nuclear Magnetic Resonance (13C-NMR) and elemental analysis. Docking with Epidural Growth Factor Receptor (EGFR) kinase were carried out and showed effective overlap. The aminoacetylenicoxyquinazoline were tested for their antitumor activities using breast (MCF) and colon (CaCO-2) cancer cell lines. All synthesized compounds exhibited antiproliferative activity but it was weaker than the well-known standard Doxorubicin. Further structural modifications are needed to enhance their antiproliferative effects.




Abstract:
A new series of 7-methoxy-2-[4-(t-amino-1-yl)oxy]-naphthalene derivatives; 7-methoxy-2-{[4-(2-methylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ2), 7-methoxy-2-{[4-(2,6-dimethylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ3), 7-methoxy-2{[4-(piperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ4), 7-methoxy-2-{[4-(pyrrolidine)but-2-yn-1-yl]oxy}-naphthalene (RZ5), 7-methoxy-2-{[4-(N-methylpiperazine)but-2-yn-1-yl]oxy}-naphthalene (RZ6), 7-methoxy -2-{[4-(hexamethyleneimine)but-2-yn-1-yl]oxy}-naphthalene (RZ7) were synthesized and screened in vitro as potential antimicrobial agents. Antimicrobial activity were evaluated by measuring the minimum inhibitory and bactericidal/fungicidal concentration (MIC, MBC and MFC). RZ2, RZ5, RZ6 and RZ7 showed the highest antimicrobial activity against S. aureus with MIC value 62.5 μg/ml, compounds RZ2, RZ4, RZ5, and RZ7 have the highest antimicrobial activity against B. subtilis with MIC vale 62.5 μg/ml, RZ3, RZ6 have the same antimicrobial activity with MIC value 125μg/ml, compounds. RZ4, RZ5, RZ6 and RZ7 have the highest antimicrobial activity against E. coli with MIC value 125 μg/ml, all compounds have the same MIC value against P. aeruginosa (125 μg/ml). RZ2, RZ4, RZ5, RZ6, RZ7 showed the highest antifungal activity with MIC of 62.5 μg/ml. In conclusion, the synthesized compounds showed good antimicrobial activity and promising potency against gram positive bacteria, gram negative bacteria and fungi