Dehydrozingerone Inspired Styryl Hydrazine Thiazole Hybrids as Promising Class of Antimycobacterial Agents.
ACS Med Chem Lett
; 7(7): 686-91, 2016 Jul 14.
Article
en En
| MEDLINE
| ID: mdl-27437078
ABSTRACT
Series of styryl hydrazine thiazole hybrids inspired from dehydrozingerone (DZG) scaffold were designed and synthesized by molecular hybridization approach. In vitro antimycobacterial activity of synthesized compounds was evaluated against Mycobacterium tuberculosis H37Rv strain. Among the series, compound 6o exhibited significant activity (MIC = 1.5 µM; IC50 = 0.48 µM) along with bactericidal (MBC = 12 µM) and intracellular antimycobacterial activities (IC50 = <0.098 µM). Furthermore, 6o displayed prominent antimycobacterial activity under hypoxic (MIC = 46 µM) and normal oxygen (MIC = 0.28 µM) conditions along with antimycobacterial efficiency against isoniazid (MIC = 3.2 µM for INH-R1; 1.5 µM for INH-R2) and rifampicin (MIC = 2.2 µM for RIF-R1; 6.3 µM for RIF-R2) resistant strains of Mtb. Presence of electron donating groups on the phenyl ring of thiazole moiety had positive correlation for biological activity, suggesting the importance of molecular hybridization approach for the development of newer DZG clubbed hydrazine thiazole hybrids as potential antimycobacterial agents.
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1
Colección:
01-internacional
Banco de datos:
MEDLINE
Idioma:
En
Revista:
ACS Med Chem Lett
Año:
2016
Tipo del documento:
Article
País de afiliación:
Sudáfrica