Alkyl, alkenyl, sulfonyl, thiocarbamates and Mannich derivatives were synthesized and tested for antimicrobial activity. The thiocarbamates derivatives were the most potent compounds.
Objectives: Previous research from this group has identified significant antimicrobial activity associated with oil-in-water (O/W) microemulsions. This activity has been exhibited against both bacteria and fungi (including yeasts) and bacterial biofilms and is dependent upon the position of the microemulsion within its stability zone. This novel work aims to identify antimicrobial activity of water-in-oil (W/O) microemulsions. Materials & Methods: A simple, thermodynamically stable water-in-oil microemulsion was tested for its time-related antimicrobial activity against a selected panel of test microorganisms (i.e.: Pseudomonas aeruginosa ATCC 9027, Escherichia coli ATCC 8739, Candida albicans ATCC 10231 and Staphylococcus aureus ATCC 6538P) and its effectiveness as a self-preserving system against a similar panel (Pseudomonas aeruginosa ATCC 9027, Candida albicans ATCC 10231, Staphylococcus aureus ATCC 6538P and Aspergillus niger ATCC 16404). Results: The microemulsion exhibited significant antimicrobial activity against all the selected microorganisms. Decreases in the viability of cultures (P. aeruginosa, C. albicans, E. coli and S. aureus) were observed over a short period of time after exposure to a known concentration of the first microemulsion. The results for the four samplings in the preservative effectiveness test according to the European Pharmacopeia requires a significant reduction in bacterial count, and this requirement was achieved in all samplings. Conclusions: Thermodynamically stable water-in-oil microemulsions are antimicrobially active, self-preserving systems, as are their oil-in-water counterparts.
Background: The previously reported circulating human antibodies against the Bovine Milk Fat Globule Membrane (BMFGM) were found to primarily target xanthine oxidase (XO) enzyme that produces uric acid and reactive oxygen species. It is suggested that XO could potentially be implicated in the pathogenesis of acute myocardial infarction. Methods: In this study, anti-BMFGM and anti-XO IgG, IgM and IgA antibodies were assayed in the sera of acute myocardial infarction patients and healthy control from the Jordanian population using the highly sensitive Enzymelinked immunosorbent assay (ELISA). Results: Serum high in antibodies against xanthine oxidase was used as a reference serum to standardize the assay. The levels of anti-BMFGM IgM antibodies were found to be higher in male controls than myocardial infarction male patients in contrast to female group, but no significant differences were observed in the levels of IgG and IgA antibodies. The levels of anti-xanthine oxidase IgM and IgG antibodies were significantly higher in myocardial infarction patients when compared with their corresponding controls. Conflicting results were obtained when different personnel measured the IgM antibody titres, likely due to infarction factors of IgM aggregation within the assay. Results from this study demonstrate significant differences in the levels of antiMFGM and anti-XO IgM antibodies between myocardial infarction patients and controls. Conclusion: Collectively, the data suggest that XO may be a risk factor in myocardial infarction patients and the presence of antibodies may act as a protective factor
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-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ5), 2-[4-(4-methylpiperazin-1-yl) but-2-yn-1-yl]-1,3-benzothiazole (BZ6), 2-[4-(2, 6-dimethylpiperidin-1-yl) but-2-yn-1-yl]-1, 3-benzothiazole (BZ7) were synthesized and screened in vitro as potential antimicrobial agents. Methods : In-vitro antimicrobial activity evaluation was done, by agar diffusion method and broth dilution test against Staphylococcus aureus ATCC 6538p, Candida albicans ATCC 10231, Pseudomonas aeruginosa ATCC 9027, Escherichia coli ATCC 8739, and Bacillus subtilis ATCC 6633. Minimum inhibitory concentration (MIC) and Minimum bactericidal concentration (MBC) were determined. The results of antimicrobial testing were compared to two positive control drugs ciprofloxacin (5 µg/ml) and fluconazole (500µg/ml). Results : Compound 2-[4-(azepan-1-yl) but-2-yn-1-yl]-1,3-benzothiazole (BZ5) showed the highest antibacterial activity against S. aureus with MIC value of 15.62 µg/ml while; Compound 2-[4-(2,6-dimethylpiperidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ7) exhibited the highest antibacterial activity against P. aeruginosa with MIC value of 31.25 µg/ml. Compounds 2-[4-(pyrrolidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ2) and 2-[4-(azepan-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ5) showed the highest antifungal activity against C. albicans with MIC value of 15.62 µg/ml (for both). Conclusion : The results obtained showed variation in the antibacterial and antifungal activity based on the structure of the cyclic amines in these amino acetylenic benzothiazole derivatives. Keywords : Benzothiazole, Aminoacetylenic, Antibacterial, Antifungal, Mannich reaction
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-{[4-(2,6-dimethylPiperidin-1-yl)but-2-yn-1-yl]Sulfanyl}-1,3-benzothiazole(AZ3) compound were determined, using the broth dilution method. The MBC and MFC dilutions were prepared. Broth cultures of Staphylococcus aureus (S. aureus), Bacillus subtilis (B. subtilis), Escherichia coli (E. coli), and Pseudomonas aeruginosa (P. aeruginosa) were incubated at 37 °C for 24 h, and Candida albicans (C. albicans) was incubated at 25 °C for 48 h. 0.1 ml of each broth culture represent 1.5 x 106 CFU/ml was challenged with 9.9 ml broth containing the MBC or MFC concentrations of the AZ3 compound. From each sample at different time intervals, 1 ml was taken and added to 9 ml of sterile distilled water, in order to neutralize the effect of AZ3. Serial dilution was done and a viable count was determined from the appropriate dilutions.Results: The viability of the P. aeruginosa, E. coli, S. aureus, B. subtilis and C. albicans were killed within 3.5 h, 5 h, 24 h, 3 h and 5 h respectively. The time killing curves showed that AZ3 needed longer time for killing S. aureus than the time needed to kill B. subtilis. On the other hand, AZ3 needed a shorter time to kill P. aeruginosa, than the time needed to kill E. coli. In comparison with ciprofloxacin, AZ3 needed a shorter time to kill P. aeruginosa and E. coli, and the same time to kill B. subtilis, while it needed longer time than ciprofloxacin to kill S. aureus. In comparison with fluconazole, AZ3 with lower MFC than fluconazole needed longer time to kill C. albicans.Conclusion: AZ3 showed promising antimicrobial killing activities, in compared with ciprofloxacin and fluconazole, which promoted our interest to investigate the time of killing needed for other 2-mercaptobenzothiazole derivatives against different types of microorganisms.
Objective : To synthesize new amino acetylenic benzophenone derivatives with significant H 3 -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, H 1 -NMR, 13 C NMR, and elemental analysis were consistent with the assigned structures. The designers of these compounds as H 3 -antagonists were based on the nationalization of the important criteria that provide effective inhibitory binding with H 3 -receptor. Molecular docking results of compounds (AZ-2-7) showed a good H 3 -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 H 3 antagonists in managing many CNS diseases like Alzheimer, epilepsy, depression, schizophrenia and many others.
A recent approach in cancer treatment is the angiogenesis inhibitors, as represented by the endothelial growth factor receptor inhibitors and vascular endothelial growth factor receptor inhibitors such as thalidomide and lenalidomide.We envision structural analogues to lenalidomide namely aminoacetylenic-2-methylindoline series as a novel and new angiogenesis inhibitors.Aminoacetylenic-2-methylindoline derivatives were synthesized from reaction of 2methylindoline with 3-bromoprop-1-yne to generate 2-methyl-1-(prop-2-yn-1-yl)-2,3-dihydro-1H-indole (AZ-1).A mixture of 2-methyl-1-(prop-2-yn-1-yl)-2,3-dihydro-1H-indole, paraformaldehyde, cyclic amine and cuprous chloride catalytic amount, in peroxide free dioxane through Mannich reaction yielded the desired aminoacetylenic-2-methylindoline derivatives (AZ2-7).The IR, DSC, 1 H-NMR, 13 C-NMR and elemental analysis results were consistent with
The presence of fimbriae on the Vibrio cholerae strains used was assessed by pellicle formation, haemagglutination activity and electron microscopy. Fimbrial suspensions were prepared by shearing them off the organisms, then separating them from other components by absorbing them on to rabbit red blood cells. Rabbits were then immunized with the fimbrial‐red cell suspensions and the antibodies evoked were titrated by haemagglutination inhibition, agglutination, vibriocidal and immobilization techniques.
Several compounds were derived from the conversion of the carboxyl group in salicylic acid and diflunisal into amides of various heterocyclic rings such as 2-amino-5-methyl-2- thiazole, 3-amino-5-methylisooxazole, 2-amino-5-methylthio-1,3,4-thiadiazole and 2- aminothiazole. The synthetic steps involve esterification of the phenolic group in diflunisal, followed by activation of the carboxyl group in aspirin and the esterified difluninal. Coupling of the corresponding anhydride with the above mentioned heterocyclic rings yielded the intermediates 8-11 and 18-21. Removal of the acetate generated the designed compounds 12-15 and 22-25. The anti-inflammatory activities of these compounds were tested using the % inhibition of granuloma. The results were 64%, 50% and 67% for compounds 25, Roficoxib and Indomethacin respectively. The ulcerogenic potential of tested compounds indicate that compound 25 in this novel series showed better anti-inflammatory activity and least ulcerogenic side effect relative to Roficoxib and Indomethacin.
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