Clubbed [1,2,3] triazoles by fluorine benzimidazole: A novel approach to H37Rv inhibitors as a potential treatment for tuberculosis

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 23, 2008, Pages 6244-6247

  Gill, Charansingh ^a   Jadhav, Ganesh ^a,b   Shaikh, Mohammad ^a,b   Kale, Rajesh ^a,b   Ghawalkar, Anant ^a   Nagargoje, Deepak ^a   Shiradkar, Mahendra ^c  

^a DR BABASAHEB AMBEDKAR MARATHWADA UNIVERSITY   (India)

^b Wockhardt Research Centre   (India)

^c OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

Author keywords

1,2,3 Triazole; Antimicrobial activity; Antitubercular activity; Benzimidazole; H37Rv strain

Indexed keywords

(1H [1,2,3]TRIAZOL 4 YLMETHYL) 1H BENZO[D]IMIDAZOLE; 1,2,3 TRIAZOLE DERIVATIVE; 2 (3 FLUOROPHENYL) 1 [1 (2,3,4 TRIFLUOROPHENYL) 1H [1,2,3]TRIAZOL 4 YLMETHYL] 1H BENZ[D]IMIDAZOLE; BENZIMIDAZOLE DERIVATIVE; FLUOROBENZIMIDAZOLE DERIVATIVE; GENTAMICIN; RIFAMPICIN; UNCLASSIFIED DRUG;

ANTIBACTERIAL ACTIVITY; ARTICLE; BACTERIAL STRAIN; DRUG STRUCTURE; MINIMUM INHIBITORY CONCENTRATION; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS; TUBERCULOSIS;

ANTITUBERCULAR AGENTS; BENZIMIDAZOLES; DRUG DESIGN; ESCHERICHIA COLI; HYDROCARBONS, FLUORINATED; MICROBIAL SENSITIVITY TESTS; MOLECULAR STRUCTURE; MYCOBACTERIUM TUBERCULOSIS; PSEUDOMONAS AERUGINOSA; RIFAMPIN; SALMONELLA TYPHI; STAPHYLOCOCCUS AUREUS; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZOLES;

EID: 55749092597     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.09.096     Document Type: Article

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29. General experimental procedure for the synthesis of 2-(3-fluoro-phenyl)-1-[1-(substituted-phenyl)-1H-[1,2,3]-triazol-4-yl-me thyl)-1H-benzo[d] imidazole 9a-9k. To a suspension of sodium hydride (0.94 mmol) in dimethyl formamide was added 2-(3-fluorophenyl)-1H-benz[d] imidazole (8) (0.47 mmol) at room temperature and stirred the reaction mixture for 30 min. To this reaction mixture, substituted 4-bromomethyl-1H-[1,2,3]-triazole (5a-i) (0.52 mmol) was then added at room temperature and stirred for 30 min. After completion, the reaction mixture was quenched with ice water. The solid that separates was filtered and dried at room temperature 9a-9k.
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