1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors.
作者信息
Coppola G M, Zhang Y L, Schuster H F, Russell M E, Hughes T E
机构信息
Metabolic and Cardiovascular Diseases Research, Novartis Institute for Biomedical Research, Summit, NJ 07901, USA.
出版信息
Bioorg Med Chem Lett. 2000 Jul 17;10(14):1555-8. doi: 10.1016/s0960-894x(00)00286-9.
Abstract
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.
摘要
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