Discovery of novel antitubercular 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues.
Bioorg Med Chem Lett
; 21(18): 5259-61, 2011 Sep 15.
Article
en En
| MEDLINE
| ID: mdl-21807509
ABSTRACT
In the present investigation, a series of 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues were synthesized and were evaluated for antitubercular activity by two fold serial dilution technique. All the newly synthesized compounds showed low to high inhibitory activities against Mycobacterium tuberculosis H(37)Rv and INH resistant M. tuberculosis. The compound 3-(4-fluorophenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carbothioamide (4o) was found to be the most promising compound active against M. tuberculosis H(37)Rv and isoniazid resistant M. tuberculosis with minimum inhibitory concentration 3.12 µM and 6.25 µM, respectively.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Pirazoles
/
Tioamidas
/
Descubrimiento de Drogas
/
Indenos
/
Mycobacterium tuberculosis
/
Antituberculosos
Límite:
Animals
Idioma:
En
Año:
2011
Tipo del documento:
Article