2000-07-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学
1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors
4区 · 医学
Article
作者: Mary E Russell ; Thomas E Hughes ; Y.Larry Zhang ; Herbert F Schuster ; Gary M Coppola
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.