Synthesis Characterization and Pharmacological Evaluation of Some Novel Trisubstituted Thiazole Derivatives

Author(s)

Aejaz, A., Molvi, K.I., Khan, J.G.

Author's Affiliation

Abstract

Sets of trisubstituted thiazoles (AR-11a-AR-53a) were synthesized by reaction of substituted N-(morpholino/methoxyphenylpiperazin/methylpiperazine-1-yl-4-thiazol-5-carbonyl) benzamide (3) with (1-chloro-3-(2-methyl-4-nitro1H-imidazole-1-yl) propane-2-one), respectively. The (3) were synthesized by nucleophilic addition of benzoyl isothiocyanate /substituted benzoyl isothiocyanate and morpholino/methoxyphenylpiperazin/methylpiperazine-1-yl-4-thiazol-5-carbonyl in equimolar quantity at reflux temperature. The selected synthesized compounds from (AR-11a-AR-53a) were screened for their in vivo anti-inflammatory activity in carrageen in-induced rat hind paw oedema model at three graded doses employed at 10, 20 and 40 mg/kg body weight using Diclofenac sodium (10 mg/kg, 75 %) and ibuprofen (20 mg/kg, 74%) drug while other compounds were screened at single grad dose of 20 mg/kg. Among all the tested compounds AR-21a, AR-31a, AR-12a and AR-42a showed maximum anti-inflammatory activity of 70% protection at 20 mg/kg and 56% protection at 40 mg/kg to inflamed paw, while other compounds showed Moderate to less protection at 10 mg/kg, 20 mg/kg & 40 mg/kg to inflamed paw.

Keywords

Thiazoles, Nitroimidazole, Inflammation, Anti-Inflammatory Activity

Cite This Article

Aejaz, A., Molvi, K.I., Khan, J.G. (2015). Synthesis Characterization and Pharmacological Evaluation of Some Novel Trisubstituted Thiazole Derivatives, International Journal for Pharmaceutical Research Scholars (IJPRS), 4(2), 425-437.