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Design, Synthesis And Biological Evaluation Of Novel Cannabinoid Antagonist, Abha Verma
Design, Synthesis And Biological Evaluation Of Novel Cannabinoid Antagonist, Abha Verma
University of New Orleans Theses and Dissertations
This study was aimed at the development of novel CB1 cannabinoid receptor antagonists that may have clinical applications for the treatment of cannabinoid and psychostimulant addiction. The rationale for the design for our target was to incorporate a bioisosteric 1,2,3-triazole ring into the vicinal diaryl group revealed in the prototypical antagonist/inverse agonist SR141716 (Rimonabant) that was presumed to interact with a unique region in the CB1 receptors. Based on our preliminary results we identified a novel series of 1,2,3-triazole ester and keto derivatives as lead compounds for biological evaluation. Here in the design rationale, synthesis and CB1 receptor affinity for …