Pharmacophoric screening of newly synthesized isoniazid derivatives and their antimycobacterial activity.
Pak J Pharm Sci
; 31(2): 567-573, 2018 Mar.
Article
em En
| MEDLINE
| ID: mdl-29618449
ABSTRACT
Mycobacterium tuberculosis is clinically recognized as a causative agent of Tuberculosis. Keeping in view, this study was endeavored to screen our previously synthesized seventeen INH analogues for their antimycobacterial potential using proportion method. During this process, INH and all the seventeen compounds were examined at different concentrations of 0.05, 0.1 and 0.2µg/mL which were prepared using Lowenstein-Jensen (LJ) base. For drug susceptibility test, three Mycobacterial strains ATCC H37Rv, known INH-sensitive and INH-resistant strains were selected, sub-cultured on LJ Medium and serial diluted to achieve 110, 1100, 11000 and 110000 from calibrated bacterial suspension Mcfarland No. 1. Dilutions of 1100 and 110000 were added to drug free medium and 1100 bacterial suspension was added to each of the test concentrations and finally incubated for 4-6 weeks at 37°C. It was observed that only compounds II and XI were active against MTb. Compounds III, IX and X also showed activity but were less potent. Ligand Scout 3.02[il_10] was used to perform pharmacophore-based screening where important pharmacophoric features were identified in the structures of these compounds which could be related to their observed antimycobacterial activity.
Buscar no Google
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Isoniazida
/
Antituberculosos
Tipo de estudo:
Diagnostic_studies
/
Screening_studies
Idioma:
En
Revista:
Pak J Pharm Sci
Assunto da revista:
FARMACIA
/
FARMACOLOGIA
/
QUIMICA
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Paquistão