ANTIMYCOBACTERIAL ACTIVITY OF A SERIES OF PYRAZINOIC ACID-ESTERS

被引:86
作者
CYNAMON, MH
KLEMENS, SP
CHOU, TS
GIMI, RH
WELCH, JT
机构
[1] SUNY HLTH SCI CTR,SYRACUSE,NY 13210
[2] SUNY ALBANY,DEPT CHEM,ALBANY,NY 12222
关键词
D O I
10.1021/jm00085a007
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of pyrazinoic acid esters has been prepared and evaluated for in vitro antimycobacterial activity. Several of the pyrazinoate esters have substantially better activity than the first-line antituberculous agent pyrazinamide against susceptible isolates of Mycobacterium tuberculosis as well as activity against pyrazinamide-resistant isolates. The minimal inhibitory concentrations (MICs) were lower for each organism and at each pH than the MICs for pyrazinamide. The esters have activity against Mycobacterium bovis and Mycobacterium kansasii, two species resistant to pyrazinamide, but not against Mycobacterium avium complex.
引用
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页码:1212 / 1215
页数:4
相关论文
共 20 条
[1]  
BLOCH AB, 1989, CLIN CHEST MED, V10, P297
[2]  
BRANDER E, 1972, Tubercle, V53, P128, DOI 10.1016/0041-3879(72)90029-3
[3]   THE ANTITUBERCULOSIS ACTIVITY OF SOME ETHYLMERCAPTO COMPOUNDS [J].
BROWN, HD ;
MATZUK, AR ;
BECKER, HJ ;
CONBERE, JP ;
CONSTANTIN, JM ;
SOLOTOROVSKY, M ;
WINSTEN, S ;
IRONSON, E ;
QUASTEL, JH .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1954, 76 (14) :3860-3860
[4]   RESURGENT TUBERCULOSIS IN NEW-YORK-CITY - HUMAN-IMMUNODEFICIENCY-VIRUS, HOMELESSNESS, AND THE DECLINE OF TUBERCULOSIS-CONTROL PROGRAMS [J].
BRUDNEY, K ;
DOBKIN, J .
AMERICAN REVIEW OF RESPIRATORY DISEASE, 1991, 144 (04) :745-749
[5]  
CHORINE MV, 1945, CR HEBD ACAD SCI, V220, P150
[6]  
DAVID HL, 1976, DHEW CDC768316 PUBL
[7]  
GANGADHARAM PRJ, 1988, ANTIMICROBIAL AGENTS, V3, P15
[8]  
GROSSET JH, 1989, REV INFECT DIS, V11, pS347
[9]  
HIEFETS LB, 1989, ANTIMICROB AGENTS CH, V33, P1252
[10]  
KONNO K, 1967, AM REV RESPIR DIS, V95, P461