Synthesis and Antimicrobial Activity of some Amide Derivatives Bearing Thiazole, Benzhydryl and Piperidine Moieties
作者:Ahmet Ozdemir
DOI:10.2174/157018013804142410
日期:2013.1.1
In the present study, N-(benzhydryl/thiazol-2-yl)-2-(piperidin-1-yl)acetamide derivatives were obtained by the reaction of 2-chloro-N-(benzhydryl/thiazole-2-yl)acetamides with piperidine derivatives. The chemical structures of the compounds were elucidated by IR, 1H-NMR, and mass spectral data and elemental analyses. These compounds were investigated for their antimicrobial effects. The microbiological results revealed that the compounds were more effective against C. albicans (ATCC-22019) than bacteria. Among all compounds (1-9), compound 3 bearing benzhydryl and 4- methylpiperidin-1-yl moieties was found to be the most effective compound against C. albicans. Compound 3 exhibited antibacterial activity against P. aeruginosa with a MIC value of 62.5 μg/mL, whereas streptomycin showed antibacterial activity against P. aeruginosa with a MIC value of 125 μg/mL. Furthermore, compound 3 exhibited the same level of antibacterial activity against S. aureus when compared with streptomycin. Other derivatives did not show significant activity against the tested bacteria.
在本研究中,通过2-氯-N-(二苯甲基/噻唑-2-基)乙酰胺与哌啶衍生物反应,获得了N-(二苯甲基/噻唑-2-基)-2-(哌啶-1-基)乙酰胺衍生物。通过IR、1H-NMR和质谱数据以及元素分析阐明了化合物的化学结构。这些化合物被研究了其抗微生物活性。微生物学结果揭示,这些化合物对C. albicans(ATCC-22019)比对细菌更有效。在所有化合物(1-9)中,带有二苯甲基和4-甲基哌啶-1-基基团的化合物3被发现是对C. albicans最有效的化合物。化合物3对P. aeruginosa表现出抗菌活性,MIC值为62.5 μg/mL,而链霉素对P. aeruginosa的抗菌活性MIC值为125 μg/mL。此外,化合物3与链霉素相比对S. aureus表现出相同的抗菌活性水平。其他衍生物对测试的细菌没有显示出显著的活性。