RESUMEN
In the present study a series of 2-substituted-5-[isopropylthiazole] clubbed 1,2,4-triazole and 1,3,4-oxadiazole derivatives have been synthesized and characterized by IR, 1H NMR, 13C NMR and mass spectral analysis. Synthesized compounds were evaluated for their preliminary cytotoxicity, antimicrobial and antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth dilution assay method. Antimycobacterial activity tested against M. tuberculosis indicated that compounds 4b and 6g exhibited twofold enhanced potency than parent compound 1 and the results indicate that some of them exhibited promising activities and they deserve more consideration as potential antitubercular agents. Compound 3c, 4b and 6c exhibited good or moderate antibacterial inhibition and compounds 3h and 7c showed excellent antifungal activity.
Asunto(s)
Antibacterianos/farmacología , Antineoplásicos/farmacología , Antituberculosos/farmacología , Mycobacterium tuberculosis/efectos de los fármacos , Tiazoles/farmacología , Antibacterianos/síntesis química , Antibacterianos/química , Antineoplásicos/síntesis química , Antineoplásicos/química , Antituberculosos/síntesis química , Antituberculosos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Oxadiazoles/química , Estereoisomerismo , Relación Estructura-Actividad , Tiazoles/síntesis química , Tiazoles/química , Triazoles/químicaRESUMEN
In the present study a series of 4-isopropylthiazole-2-carbohydrazide analogs, derived clubbed oxadiazole-thiazole and triazole-thiazole derivatives have been synthesized and characterized by IR, (1)H NMR, (13)C NMR, elemental and mass spectral analyses. The synthesized compounds were evaluated for their preliminary in vitro antibacterial, antifungal and antitubercular activity against Mycobacterium tuberculosis H(37)Rv strain by broth dilution assay method. The synthesized compounds 7a, 7b, 7d and 4 showed an antitubercular efficacy considerably greater than that of the parent 4-isopropyl-1,3-thiazole-2-carbohydrazide 1, suggesting that the substituted 4-isopropylthiazole-2-carbohydrazide moiety plays an important role in enhancing the antitubercular properties of this class of compounds. Compounds 2c, 3, 4, 6d, 7a and 7b exhibited good or moderate antibacterial and antifungal activity. Compounds 4 and 7b showed appreciable cytotoxicity at a concentration of 250muM.