Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors

ArticleinBioorganic & medicinal chemistry letters 19(15):4437-40 · June 2009with10 Reads
Impact Factor: 2.42 · DOI: 10.1016/j.bmcl.2009.05.048 · Source: PubMed


    The synthesis and biochemical evaluation of novel cyanothiazolidine inhibitors of dipeptidyl peptidase 4 (DPP4) is described. Their main structural feature is a constrained bicyclic core that prevents the intramolecular formation of inactive cyclic species. The inhibitors show good to moderate biochemical potency against DPP4 and display distinct selectivity profiles towards DPP7, DPP8 and DPP9 depending on their substitution.