1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings

被引：84

作者：

Biava, Mariangela ^{[1
]}

Porretta, Giulio Cesare ^{[1
]}

Poce, Giovanna ^{[1
]}

De Logu, Alessandro ^{[2
]}

Saddi, Manuela ^{[2
]}

Meleddu, Rita ^{[2
]}

Manetti, Fabrizio ^{[3
]}

De Rossi, Edda ^{[4
]}

Botto, Maurizio ^{[3
]}

机构：

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

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

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

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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 12期

关键词：

D O I：

10.1021/jm701560p

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis and biological evaluation of new derivatives of 1,5-bis(4-chlorophenyl)-2-methyl-3-(4-methylpipcrazin-1-yl)methyl-1H-pyrrole (BM 212, 16) are reported. Variously substituted phenyl rings with different substitution pattern and lipophilicity were added to the pyrrole nucleus to evaluate their influence on the activity toward Mycobacterium tuberculosis (MTB) and atypical mycobacteria. The most active derivatives showed activity between 0.125-0.5 mu g/mL (better than 16 and streptomycin) and protection index (64-256) higher than 16 (4) and similar to isoniazid and streptomycin (128).

引用

页码：3644 / 3648

页数：5

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