合成、表征、生物评价及 11-取代苯基-12-苯基-11a,12-二氢-11H-茚并[2,1-c][1,5]苯并噻嗪作为潜在抗菌剂的定量构效关系研究。
Synthesis, characterization, biological evaluation and QSAR studies of 11-p-substituted phenyl-12-phenyl-11a,12-dihydro-11H-indeno[2,1-c][1,5]benzothiazepines as potential antimicrobial agents.
机构信息
Department of Chemistry, Guru Jambheshwar University of Science and Technology, Hisar 125001, Haryana, India.
出版信息
Eur J Med Chem. 2012 Nov;57:196-210. doi: 10.1016/j.ejmech.2012.09.003. Epub 2012 Sep 11.
A novel series of 11-p-substituted phenyl-12-phenyl-11a,12-dihydro-11H-indeno[2,1-c][1,5]benzothiazepines (3) has been synthesized and screened for their antimicrobial activity against Gram-positive (Bacillus subtilis and Staphylococcus aureus) and Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacteria and fungi (Aspergillus fumigates and Candida albicans). The antimicrobial evaluation data indicated that the compounds, 3d, 3g, 3h, 3k-3p exhibited very promising antibacterial activity and the derivatives 3k, 3l, 3o and 3p exhibited high antifungal activity. The QSAR studies carried out to find out the correlation between the antimicrobial activity and physicochemical properties of synthesized benzothiazepines (3) indicated the predominance of electronic parameters in describing their antimicrobial activity.
已经合成了一系列新型的 11-p-取代苯基-12-苯基-11a,12-二氢-11H-茚并[2,1-c][1,5]苯并噻嗪（3），并对其进行了革兰氏阳性（枯草芽孢杆菌和金黄色葡萄球菌）和革兰氏阴性（大肠杆菌和铜绿假单胞菌）细菌以及真菌（烟曲霉和白色念珠菌）的抗菌活性进行了筛选。抗菌评价数据表明，化合物 3d、3g、3h、3k-3p 表现出非常有前景的抗菌活性，衍生物 3k、3l、3o 和 3p 表现出很强的抗真菌活性。为了找出合成的苯并噻嗪（3）的抗菌活性与理化性质之间的相关性而进行的 QSAR 研究表明，电子参数在描述其抗菌活性方面占主导地位。
Zotero 插件