RESUMO
A series of 3,6-disubstituted-7H-s-triazolo(3,4-b)(1,3,4)thiadiazines was synthesized by the condensation of the appropriate 3-substituted-4-amino-5-mercapto (1,2,4) triazoles with substituted phenacyl bromides in alcoholic medium. These compounds have been studied for their in vivo anthelmintic activity in albino mice. A number of compounds showed promising activity when given by the oral route.
Assuntos
Anti-Helmínticos/síntese química , Anti-Helmínticos/farmacologia , Himenolepíase/tratamento farmacológico , Hymenolepis/efeitos dos fármacos , Tiadiazinas/síntese química , Tiadiazinas/farmacologia , Triazóis/síntese química , Triazóis/farmacologia , Animais , Anti-Helmínticos/química , Fenômenos Químicos , Físico-Química , Avaliação Pré-Clínica de Medicamentos , Himenolepíase/parasitologia , Espectroscopia de Ressonância Magnética , Camundongos , Ratos , Espectrofotometria Infravermelho , Tiadiazinas/químicaRESUMO
A series of sulfonamides and S-benzyl derivatives of substituted/unsubstituted S-triazolo-(3,4,-b)-benzothiazole-3-thiones were synthesized. These triazolobenzolobenzothiazole derivatives were evaluated for antitubercular activity against H37Rv strain of Mycobacterium tuberculosis. A number of promising compounds have been obtained.
Assuntos
Antituberculosos/síntese química , Antituberculosos/farmacologia , Tiazóis/síntese química , Tiazóis/farmacologia , Triazóis/síntese química , Triazóis/farmacologia , Fenômenos Químicos , Físico-Química , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/efeitos dos fármacos , Espectrofotometria InfravermelhoRESUMO
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.
