1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors
4区 · 医学
Article
作者: Mary E Russell ; Gary M Coppola ; Thomas E Hughes ; Herbert F Schuster ; Y.Larry Zhang
Structure-activity relationship within a series of 1-aminoalkylisoquinoline-4-carboxylates as inhibitors of DPP-IV is described. A primary aminomethyl group is required to maintain biological activity. Substitution of the isoquinoline at the 6- and 8-positions with methoxy groups increases potency to 53 times that of the lead compound SDZ 029-576.