Antimycobacterial compounds. Optimization of the BM 212 structure, the lead compound for a new pyrrole derivative class

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• 作者：Biava ; Mariangela ; Porretta ; Giulio Cesare ; Poce ; Giovanna ; Deidda ; Delia ; Pompei ; Raffaello ; et. al.
• 关键词：Pyrrole derivatives ; Thiomorpholinomethyl substituent ; Antimycobacterial activity ; Pharmacophore model
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2005
• 出版时间：February 15, 2005
• 年：2005
• 卷：13
• 期：4
• 页码：1221-1230
• 全文大小：389 K

文摘

Our work on antitubercular agents led to the identification of BM 212 as a lead compound among a series of pyrrole derivatives with good in vitro activity against mycobacteria and candidae. Further studies led us to synthesize additional pyrroles bearing the thiomorpholinomethyl moiety and different aryl substituents at N1 and C5. Some of them revealed very active, prompting us to design the new pyrrole derivatives 5aaa20 in the hope of increasing the activity and better understanding the influence of ortho halogens on the antimycobacterial activity. Microbiological data showed interesting in vitro activity toward Mycobacterium tuberculosis and atypical mycobacteria.