Abstract
A new series of benzazole, thiazolidinone and azetidin-2-one derivatives incorporating to pyrazole moiety were synthesized by condensation of 1,3-diphenyl-1H-pyrazol-4-carboxaldehyde with different nucleophiles. The structures of the newly synthesized compounds were confirmed by analytical and spectral methods. Some of these compounds were evaluated for their anti-hyperglycemic and renoprotective activities. Three compounds showed remarkable anti-diabetic potency, whereas other five compounds showed significant renoprotective activity.
Highlights
Diabetes mellitus is increasing in prevalence worldwide, and its complication has grown into a public health problem
In sight of the above mentioned facts and in extension of our interest in the synthesis of heterocycles bearing pyrazole and/or thiazolidine moieties,[27,28,29,30] to discover new candidates that may be of importance in designing novel, active, selective and less toxic antidiabetic and renoprotective drugs, we present the synthesis and pharmacological evaluation of some novel structural hybrids containing both the pyrazole moiety with thiazolidin-4-one and azetidin-2-one ring systems during various linkages
Our synthetic strategy for a novel series of benzazole, thiazolidin-4-one and azetidin-2-one derivatives bearing 1,3-diphenyl-1H-pyrazole moiety is illustrated in Schemes 1-3
Summary
Diabetes mellitus is increasing in prevalence worldwide, and its complication has grown into a public health problem. There is increasing evidence that inflammation is closely involved in the pathogenesis of diabetes and associated complications.[12,13] drugs with anti-inflammatory properties such as thiazolidinediones can possibly decrease the risk of developing diabetes and diabetes-induced problems.[14,15,16]
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