PMID- 3103991 OWN - NLM STAT- MEDLINE DCOM- 19870505 LR - 20180216 IS - 0009-3157 (Print) IS - 0009-3157 (Linking) VI - 33 IP - 1 DP - 1987 TI - A rapid method for the evaluation of new antituberculous agents. PG - 22-7 AB - 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 new drugs. FAU - Ashtekar, D R AU - Ashtekar DR FAU - Fernandes, F AU - Fernandes F FAU - Khadse, B G AU - Khadse BG FAU - Shirodkar, M V AU - Shirodkar MV LA - eng PT - Comparative Study PT - Journal Article PL - Switzerland TA - Chemotherapy JT - Chemotherapy JID - 0144731 RN - 0 (Antitubercular Agents) RN - 0 (Guanidines) RN - 0 (Succinimides) RN - 0 (Thiazoles) RN - 142M471B3J (Carbon Dioxide) RN - 2KNI5N06TI (Pyrazinamide) RN - 8G167061QZ (Ethambutol) RN - V83O1VOZ8L (Isoniazid) RN - VJT6J7R4TR (Rifampin) RN - Y45QSO73OB (Streptomycin) SB - IM MH - Antitubercular Agents/*pharmacology MH - Carbon Dioxide/metabolism MH - Ethambutol/pharmacology MH - Guanidines/pharmacology MH - Isoniazid/pharmacology MH - Mycobacterium tuberculosis/*drug effects/growth & development/metabolism MH - Pyrazinamide/pharmacology MH - Rifampin/pharmacology MH - *Scintillation Counting/methods MH - Streptomycin/pharmacology MH - Succinimides/pharmacology MH - Thiazoles/pharmacology MH - Time Factors EDAT- 1987/01/01 00:00 MHDA- 1987/01/01 00:01 CRDT- 1987/01/01 00:00 PHST- 1987/01/01 00:00 [pubmed] PHST- 1987/01/01 00:01 [medline] PHST- 1987/01/01 00:00 [entrez] AID - 10.1159/000238472 [doi] PST - ppublish SO - Chemotherapy. 1987;33(1):22-7. doi: 10.1159/000238472.