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首页> 外文期刊>Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry >Synthesis and biological evaluation of some novel optically active 3-chloro-1-[4-({4-[(S)-(4-chlorophenyl)(phenyl)methyl]--piperazinyl} acetyl)phenyl]-4-aryl-2-azetidinone derivatives
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Synthesis and biological evaluation of some novel optically active 3-chloro-1-[4-({4-[(S)-(4-chlorophenyl)(phenyl)methyl]--piperazinyl} acetyl)phenyl]-4-aryl-2-azetidinone derivatives

机译:某些新型旋光性3-氯-1- [4-({4-[(S)-(4-氯苯基)(苯基)甲基]-哌嗪基}乙酰基)苯基] -4-芳基-的合成及生物评价2-氮杂环丁酮衍生物

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摘要

Various novel optically active substituted aryl 2-Azetidinone 4a-j have been prepared from corresponding Schiff’s bases 3a-j and chloroacetyl chloride in presence of glacial acetic acid in benzene using Dien and Stark apparatus. Structure of the synthesized compound was confirmed by Spectral data (IR, 1H NMR) and elemental analysis. All the newly synthesized compounds were evaluated for their antimicrobial activities. Investigation of antimicrobial activities of compounds was done by Broth dilution method used for the determination of minimum inhibitory concentration. The synthesize compounds were screened for antibacterial against gram-positive bacteria [Staphylococcus aureus (MTCC96), Streptococcus pyogenes (MTCC442)] and gram-negative bacteria [Escherichia coli (MTCC443), Pseudomonas aeruginosa (MTCC424)] and antifungal against Candida albicans (MTCC227), Aspergillus niger (MTCC282) and Aspergillus clavatus (MTCC1323).The compounds showed good antibacterial activity but less active against fungal strain used.
机译:各种新颖的光学活性取代的芳基2-氮杂环丁酮4a-j已经通过使用Dien和Stark装置在苯中的冰乙酸存在下,由相应的席夫氏碱3a-j和氯乙酰氯制备。通过光谱数据(IR,1 H NMR)和元素分析确认合成的化合物的结构。评价所有新合成的化合物的抗菌活性。通过用于确定最小抑菌浓度的肉汤稀释法研究化合物的抗菌活性。筛选合成的化合物对革兰氏阳性菌[金黄色葡萄球菌(MTCC96),化脓性链球菌(MTCC442)]和革兰氏阴性菌[大肠杆菌(MTCC443),铜绿假单胞菌(MTCC424)]和针对白色念珠菌的抗真菌药),黑曲霉(MTCC282)和克拉夫曲霉(MTCC1323),这些化合物显示出良好的抗菌活性,但对使用的真菌菌株没有活性。

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