Design, synthesis and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetohydrazide derivatives with anti-inflammatory-analgesic activities.
Arch Pharm Res
; 36(12): 1465-79, 2013 Dec.
Article
en En
| MEDLINE
| ID: mdl-23712380
ABSTRACT
The present work describes the synthesis and evaluation of some new acetohydrazones, 1,3,4-oxadiazoles and 1,2,4-triazoles of 1,2,4-triazolo[1,5-a]benzimidazole as anti-inflamm atory-analgesic agents. Structure elucidation of these compounds was confirmed by IR, (1)H NMR, and mass spectrometry along with elemental microanalyses. Most compounds exhibited significant anti-inflammatory activity in comparison to indomethacin. Further, some compounds were tested for their analgesic effects where two compounds showed results comparable to indomethacin at 4 h interval. The most active anti-inflammatory and analgesic compounds (4c and 11a) were examined on gastric mucosa and didn't show any gastric ulcerogenic effect compared with the reference indomethacin. Moreover, LD50 of compounds (4c and 11a) were determined in mice; they were found non toxic up to 240 and 300 mg/kg (i.p.). Also, docking simulation of some compounds into COX active sites was studied.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Triazoles
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Bencimidazoles
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Diseño de Fármacos
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Simulación del Acoplamiento Molecular
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Analgésicos
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Antiinflamatorios
Límite:
Animals
Idioma:
En
Revista:
Arch Pharm Res
Año:
2013
Tipo del documento:
Article
País de afiliación:
Egipto