A Rapid Method for the Evaluation of New Antituberculous Agents
作者:
D.R. Ashtekar,
F. Fernandes,
B.G. Khadse,
M.V.N. Shirodkar,
期刊:
Chemotherapy
(Karger Available online 1987)
卷期:
Volume 33,
issue 1
页码: 22-27
ISSN:0009-3157
年代: 1987
DOI:10.1159/000238472
出版商: S. Karger AG
关键词: Radiometry;Antituberculous activity;Replication time;Inhibition of14CO2;Broth dilution test
数据来源: Karger
摘要:
Fifty-one new synthetic compounds belonging to four different series, namely (1a) substituted aryl-4-(substituted phenyl) succinimide; (1b) N-(substituted methyl)-4-(heterocyclic) succinimide; (2) heterocyclic 4-(5′-nitro-2-furyl) thiazoles; (3) substituted aryl-4-(3′, 4′-dihydroxy phenyl) thiazoles, and (4) phenyl-N, N-1,2,3-bis-methoxy carbonyl guanidines were screened for antituberculous activity using a conventional broth dilution test (BDT) and a liquid scintillation radiometric method (LSRM). Eight compounds showed in vitro activity. LSRM showed 100% agreement with BDT. LSRM is completed within 60 h, while BDT requires 8–9 days. Unlike BDT, LSRM allowed one to measure the graded changes in the metabolism and the growth rate of Mycobacterium tuberculosis in response to various concentrations of the drug. It permits the measurement of the relative prolongation of the replication time by the drug or the test compound. With LSRM it was possible to detect the phase of growth during which the test compound shows or begins its antituberculous activity. It improves our understanding of the antituberculous activity of the test compound and hence is more advantageous. It is rapid, reliable, quantitative and more sensitive than BDT. LSRM is thus suitable for the evaluation of ne
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