1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: Design, synthesis, and microbiological evaluation

被引：72

作者：

Biava, Mariangela ^{[1
]}

Porretta, Giulio C. ^{[1
]}

Poce, Giovanna ^{[1
]}

De Logu, Alessandro ^{[2
]}

Meleddu, Rita ^{[2
]}

De Rossi, Edda ^{[3
]}

Manetti, Fabrizio ^{[4
]}

Botta, Maurizio ^{[4
]}

机构：

[1] Univ Roma La Sapienza, Dipartimento Chim & Tecnol Farmaco, I-00185 Rome, Italy

[2] Dipartimento Sci & Tecnol Biomed, Sez Microbiol Med, I-09123 Cagliari, Italy

[3] Univ Pavia, Dipartimento Genet & Microbiol, I-27100 Pavia, Italy

[4] Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 11期

关键词：

BM; 212; 1,5-Diarylpyrroles; Mycobacterium tuberculosis; Pharmacophoric model; Antitubercular agents; MULTIDRUG-RESISTANT TUBERCULOSIS; MYCOBACTERIUM-TUBERCULOSIS; ANTITUBERCULOSIS DRUGS; COINFECTION; UPDATE; HIV; TB;

D O I：

10.1016/j.ejmech.2009.06.005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 mu g/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. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：4734 / 4738

页数：5

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