Importance of the thiomorpholine introduction in new pyrrole derivatives as antimycobacterial agents analogues of BM 212

被引：77
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 Biologi, I-00185 Rome, Italy
[2] Univ Cagliari, Fac Sci Matemat Fis Nat, Cattedra Microbiol Applicata, I-09124 Cagliari, Italy
[3] Univ Siena, Dipartimento Farm Chim Tecnol, I-53100 Siena, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 04期
关键词：
D O I：
10.1016/S0968-0896(02)00455-8
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：
During the course of our investigations in the field of azole antimicrobial agents, we have identified BM 212, a pyrrole derivative with good in vitro activity against mycobacteria and candidae. These findings prompted us to prepare new pyrrole derivatives 1-10 in the hope of increasing the activity. The microbiological data showed interesting in vitro activity against Mycobacterium tuberculosis and atypical mycobacteria. (C) 2002 Elsevier Science Ltd. All rights reserved.
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页码：515 / 520
页数：6
相关论文
共 15 条
[1]   Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity [J].
Barbachyn, MR ;
Hutchinson, DK ;
Brickner, SJ ;
Cynamon, MH ;
Kilburn, JO ;
Klemens, SP ;
Glickman, SE ;
Grega, KC ;
Hendges, SK ;
Toops, DS ;
Ford, CW ;
Zurenko, GE .
JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (03) :680-685
[2]   TREATMENT OF TUBERCULOSIS AND TUBERCULOSIS INFECTION IN ADULTS AND CHILDREN [J].
BASS, JB ;
FARER, LS ;
HOPEWELL, PC ;
OBRIEN, R ;
JACOBS, RF ;
RUBEN, F ;
SNIDER, DE ;
THORNTON, G .
AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE, 1994, 149 (05) :1359-1374
[3]  
Biava M, 1999, MED CHEM RES, V9, P19
[4]   New pyrrole derivatives as antimycobacterial agents analogs of BM212 [J].
Biava, M ;
Fioravanti, R ;
Porretta, GC ;
Deidda, D ;
Maullu, C ;
Pompei, R .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (20) :2983-2988
[5]  
Biava M, 2002, MED CHEM RES, V11, P50
[6]   CHARMM - A PROGRAM FOR MACROMOLECULAR ENERGY, MINIMIZATION, AND DYNAMICS CALCULATIONS [J].
BROOKS, BR ;
BRUCCOLERI, RE ;
OLAFSON, BD ;
STATES, DJ ;
SWAMINATHAN, S ;
KARPLUS, M .
JOURNAL OF COMPUTATIONAL CHEMISTRY, 1983, 4 (02) :187-217
[7]   DRUG-TREATMENT OF TUBERCULOSIS - 1992 [J].
DAVIDSON, PT ;
LE, HQ .
DRUGS, 1992, 43 (05) :651-673
[8]   Bactericidal activities of the pyrrole derivative BM212 against multidrug-resistant and intramacrophagic Mycobacterium tuberculosis strains [J].
Deidda, D ;
Lampis, G ;
Fioravanti, R ;
Biava, M ;
Porretta, GC ;
Zanetti, S ;
Pompei, R .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1998, 42 (11) :3035-3037
[9]  
Fioravanti R, 1999, MED CHEM RES, V9, P162
[10]  
Grosset J, 1990, Bull Int Union Tuberc Lung Dis, V65, P86
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