Antimycobacterial compounds. New pyrrole derivatives of BM212

被引:86
作者
Biava, M
Porretta, GC
Deidda, D
Pompei, R
Tafi, A
Manetti, F
机构
[1] Univ Roma La Sapienza, Dipartimento Studi Chim & Tecnol Sostanze Biol At, I-00185 Rome, Italy
[2] Univ Cagliari, Fac Sci Matemat Fis Nat, Cattedra Microbiol Applicata, I-09124 Cagliari, Italy
[3] Univ Siena, Dipartimento Farmacochim Tecnol, I-53100 Siena, Italy
关键词
pyrrole derivatives; thiomorpholine substituent; antimycobacterial activity; pharmacophore model;
D O I
10.1016/j.bmc.2003.12.037
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
We have identified BM212 as a lead compound among a series of pyrrole derivatives with good in vitro activity against mycobacteria and candidae. First studies led us to synthesize some pyrrole compounds in which the thiomorpholine fragment was present. Some compounds revealed very active and these findings prompted us to prepare new pyrrole derivatives 2-15 in the hope of increasing the activity. The microbiological data showed interesting in vitro activity against Mycobacterium tuberculosis and atypical mycobacteria. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1453 / 1458
页数:6
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