1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: Design, synthesis, and microbiological evaluation
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- 作者：Mariangela Biava ; Giulio C. Porretta ; Giovanna Poce ; Aless ; ro De Logu ; Rita Meleddu ; Edda De Rossi ; Fabrizio Manetti ; Maurizio Botta
- 关键词：BM 212 ; 1 ; 5-Diarylpyrroles ; Mycobacterium tuberculosis ; Pharmacophoric model ; Antitubercular agents
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2009
- 出版时间：November 2009
- 年：2009
- 卷：44
- 期：11
- 页码：4734-4738
- 全文大小：469 K
文摘
During the search of novel antitubercular drugs related to BM 212, new diarylpyrroles were designed and synthesized on the basis of a structure–activity relationship analysis of many pyrroles previously described by us. Among them, 1-(4-fluorophenyl)-2-ethyl-3-(thiomorpholin-4-yl)methyl-5-(4-methylphenyl)-1H-pyrrole (2b) proved to be particularly active, with a minimum inhibitory concentration (MIC, expressed as μg/mL) and a protection index (PI) better than or comparable to those of reference compounds. Also the remaining compounds were very active, although their MIC and PI were in general lower than those of their parent 2-methyl analogues.