Vascular adhesion protein-1(VAP-1) is an amine oxidase, also known as semicarbazide sensitive amine oxidase(SSAO), which especially exists in human plasma, and it is thought to be an attractive therapeutic target for various inflammatory diseases including diabetes complications (diabetic nephropathy, retinopathy and so on).In our VAP-1 inhibitor program, subsequent structural modifications following high-throughput screening of our compound library resulted in the discovery of a novel series of thiazole derivatives showing potent inhibitory activity with <50nM IC50 values in rat. Moreover, treatment with selected compounds exhibited significant effects on ocular permeability in STZ induced diabetic rats. Synthesis, SAR and pharmacological properties of the thiazole derivatives will be presented.

Design, synthesis and biological evaluation of novel thiazole derivatives as vascular adhesion pretein-1 inhibitors

243rd National Meeting (2012)

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