Content area
Full text
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 m/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
(ProQuest: ... denotes formula omitted.)
1. INTRODUCTION:
The piperazine is a wide-ranging class of chemical compounds, many with important pharmacological property, which contain a center piperazine functional group. Most of these agents can be classified as phenyl piperazine or benzyl piperazine, diphenylmethyl piperazine (benzhydryl piperazine), pyridinyl piperazine, pyrimidinyl piperazine or tricyclics, (With the piperazine ring attached to the heterocyclic moiety via a side chain. The developments of piperazine as an anthelmintic agent for the treatment of nematode infection have been well documented. A wide variety of piperazine derivatives and salts as original discovery of anthelmintic agent was reported. Microbial infection is associated with pain and inflammation. In general, chemotherapeutic, analgesic and anti-inflammatory agents are prescribed simultaneously for such condition. However, very few of drugs possess these activities in a single molecule. Multi-drug treatment of inflammatory conditions associated with microbial infections poses a inimitable problem especially for patients with impaired hepatic or renal functions. Thus from the pharmacoeconomic and patient compliance points of view, the monotherapy with a drug having both anti-inflammatory and antimicrobial activities is needed. Thiazoles have recent conventional attention of their diverse pharmacological properties; these include anti-inflammatory, anti-ulcer, anthelmintics, virucidal, anesthetics, antibacterial, hypoglycemic, and anticonvulsant activities. Imidazole is one of the important heterocyclic compounds in the world of medicinal chemistry and essential component...