- SAR study of clubbed [1,2,4]-triazolyl with fluorobenzimidazoles as antimicrobial and antituberculosis agents
-
In the present study, a series of novel 2-[4-(1H-[1,2,4]-triazol-1-yl)phenyl]-1-substituted-4,6-difluoro-1H-benz o[d]imidazole derivatives are synthesized by the alkylation of 2-[4-(1H-[1,2,4]-triazol-1-yl)phenyl]-4,6-difluoro-1H-benzo[d]imidazole with substituted alkyl and aryl halides. The compounds were evaluated for their preliminary in-vitro antibacterial activity against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, and Salmonella typhosa and then were screened for their antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth microdilution assay method. The antibacterial data suggested that the analogs with electronegative substituents emerged as promising antimicrobials. It was also observed that the promising antimicrobials have proved to be better antimycobacterials. Few of selected analogs are under further evaluation for secondary antitubercular screening, as they have shown better activity compared to rifampin.
- Jadhav, Ganesh Rajaram,Shaikh, Mohammad Usman,Kale, Rajesh Prabhakar,Shiradkar, Mahendra Ramesh,Gill, Charansingh Harnamsingh
-
experimental part
p. 2930 - 2935
(2009/10/02)
-
- Synthesis, characterization, and antimicrobial activities of clubbed [1,2,4]-oxadiazoles with fluorobenzimidazoles
-
(Chemical Equation Presented) In this study, a novel series of substituted 4,6-difluoro-2-{2-[3-(substituted-phenyl)-[1,2,4]-oxadiazol-5-yl]-ethyl} -1H-benzo[d]imidazole derivatives were synthesized by condensation of 2,4-difluoro-6-nitrophenyl amine with 3-(substitutedphenyl-[1,2,4]-oxadiazol- 5yl) propionic acid by using 2,4,6-trichlorobenzoyl chloride in the presence of triethyl amine base. The compounds were evaluated for their preliminary in vitro antibacterial activity against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, and Salmonella typhosa. The antibacterial data of the tested compounds indicated that most of the synthesized compounds showed moderate activity with reference standard Gentamycin.
- Jadhav, Ganesh R.,Shaikh, Mohammad U.,Kale, Rajesh P.,Ghawalkar, Anand R.,Gill, Charansingh H.
-
experimental part
p. 980 - 987
(2009/12/05)
-
- Synthesis of novel fluorobenzofuroxans by oxidation of anilines and thermal cyclization of arylazides
-
The synthesis of several fluorobenzofuroxans by oxidation of fluoroanilines and thermal cyclization of fluoroarylazides is presented. The fluorobenzofuroxans prepared in this study presented tautomerism as evidenced by their NMR data. Benzofuroxans in general have biological activity and are synthetic intermediates for the preparation of several compounds with important pharmaceutical applications.
- Leyva, Socorro,Castanedo, Víctor,Leyva, Elisa
-
p. 171 - 175
(2007/10/03)
-
- O-Nitroaniline derivatives. Part 14. Cyclisations leading to benzimidazole N-oxides, N-hydroxybenzimidazolones and N-hydroxyquinoxaline-2,3-diones: A mechanistic borderline
-
The base-induced cyclisations of N-(o-nitrophenyl)glycine derivatives (nitriles 9 or esters 13) bearing additional substituents at the other ortho-position are anomalous, resembling those involving N-(o-nitrophenyl)sarcosine analogues. The nitriles are co
- Collins Cafiero, Pamela A.,French, Colin S.,McFarlane, Michael D.,Mackie, Raymond K.,Smith, David M.
-
p. 1375 - 1384
(2007/10/03)
-