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

被引：53

作者：

Biava, M

Porretta, GC

Poce, G

Deidda, D

Pompel, R

Tafi, A

Manetti, F

机构：

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

[2] Univ Cagliari, Fac Sci Matemat Fis Nat, Cattedrea Microbiol Aplicata, I-09124 Rome, Italy

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2005年 / 13卷 / 04期

关键词：

pyrrole derivatives; thiomorpholinomethyl substituent; antimycobacterial activity; pharmacophore model;

D O I：

10.1016/j.bmc.2004.11.018

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：

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 5-20 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 Myeobacterium tuberculosis and atypical mycobacteria. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：1221 / 1230

页数：10

共 22 条

[1]

*ACC INC, CAT 4 8 CER 4 8 1 DI

[2] Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity [J].