Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 2 de 2
Filter
Add more filters

Database
Language
Affiliation country
Publication year range
1.
Eur J Med Chem ; 45(5): 2063-74, 2010 May.
Article in English | MEDLINE | ID: mdl-20149496

ABSTRACT

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.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antineoplastic Agents/pharmacology , Antitubercular Agents/pharmacology , Mycobacterium tuberculosis/drug effects , Thiazoles/pharmacology , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antitubercular Agents/chemical synthesis , Antitubercular Agents/chemistry , Cell Line, Tumor , Cell Proliferation/drug effects , Drug Screening Assays, Antitumor , Humans , Microbial Sensitivity Tests , Molecular Structure , Oxadiazoles/chemistry , Stereoisomerism , Structure-Activity Relationship , Thiazoles/chemical synthesis , Thiazoles/chemistry , Triazoles/chemistry
2.
Eur J Med Chem ; 44(11): 4739-46, 2009 Nov.
Article in English | MEDLINE | ID: mdl-19589626

ABSTRACT

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.


Subject(s)
Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Hydrazines/chemistry , Hydrazines/pharmacology , Thiazoles/chemistry , Thiazoles/pharmacology , Antitubercular Agents/chemistry , Antitubercular Agents/pharmacology , Bacteria/drug effects , Cell Line, Tumor , Cell Survival/drug effects , Fungi/drug effects , Humans , Microbial Sensitivity Tests , Molecular Structure , Mycobacterium tuberculosis/drug effects , Structure-Activity Relationship
SELECTION OF CITATIONS
SEARCH DETAIL