Journal :   Asian Journal of Research in Chemistry

Volume No. :   10

Issue No. :  2

Year :  2017

Pages :   158-165

ISSN Print :  0974-4169

ISSN Online :  0974-4150


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Synthesis, characterization and anti-inflammatory activity some 1-(4-substituted)-2-(-4-(piperazine-1-yl) bis-thiazole-5-yl) 2-methyl-4-nitro-1h-imidazole-1-yl) ethanone



Address:   Aejaz Ahmed1*, Khurshid I. Molvi2, Gulam Javed Khan3
1Department of Pharmaceutical Chemistry, Ali-Allana College of Pharmacy, Akkalkuwa, 425451, Nandurbar, Maharashtra, India
2Department of Clinical Pharmacy, Ibne-Sina National Medical College Jeddah, Saudi Arabia
3Department of Pharmacology, Ali-Allana College of Pharmacy, Akkalkuwa, 425451, Nandurbar, Maharashtra, India
*Corresponding Author
DOI No: 10.5958/0974-4150.2017.00027.X

ABSTRACT:
Novel set of 1-(4-substituted)-2-(-4-(piperazine-1-yl) bis-thiazole-5-yl) 2-Methyl-4-Nitro-1H-imidazole-1-yl) ethanon compounds were synthesized. The adduct of piperazine were synthesized by nucleophilic addition of benzoyl isothiocyanate / substituted benzoyl isothiocyanate in bi-molar quantity at reflux temperature. The target compounds (AR-15a to AR-55a) were synthesized as 1-chloro-3-(2-methyl-4-nitro1H-imidazole-1-yl) propane-2-on (a) was added in bi-imolar quantity to a solution of adduct (substituted-bis-piperazinyl-4-thioyl) benzamide/ chlorobenzamide in acetonitrile. The synthesized compounds were characterized by physicochemical parameters and IR, 1H NMR, Mass and elemental spectral analysis. The synthesized compounds were evaluated for their in-vitro anti-inflammatory activity using HRBC membrane stabilization method and in-vivo anti-inflammatory activity by carrageenin-induced rat paw oedema model at 20 mg/kg body weight using diclofenac and ibuprofen as standard drugs. Compounds AR-45a and AR-55a showed maximum in-vitro anti-inflammatory activity membrane stabilization at 65% and 68% protection at 200 ?/mL. However moderate to poor protection was observed by in-vivo anti-inflammatory study in carragenane induced rat hind paw edema.
KEYWORDS:
Thiazoles, nitroimidazole, piperazine, anti-inflammaory, Membrane stabilization
Cite:
Aejaz Ahmed, Khurshid I. Molvi, Gulam Javed Khan. Synthesis, characterization and anti-inflammatory activity some 1-(4-substituted)-2-(-4-(piperazine-1-yl) bis-thiazole-5-yl) 2-methyl-4-nitro-1h-imidazole-1-yl) ethanone. Asian J. Research Chem. 2017; 10(2):158-165.
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