强效非腈类二肽基二肽肽酶IV抑制剂。
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.
作者信息
Simpkins Ligaya M, Bolton Scott, Pi Zulan, Sutton James C, Kwon Chet, Zhao Guohua, Magnin David R, Augeri David J, Gungor Timur, Rotella David P, Sun Zhong, Liu Yajun, Slusarchyk William S, Marcinkeviciene Jovita, Robertson James G, Wang Aiying, Robl Jeffrey A, Atwal Karnail S, Zahler Robert L, Parker Rex A, Kirby Mark S, Hamann Lawrence G
机构信息
Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543-5400, USA.
出版信息
Bioorg Med Chem Lett. 2007 Dec 1;17(23):6476-80. doi: 10.1016/j.bmcl.2007.09.090. Epub 2007 Oct 1.
The synthesis and structure-activity relationships of novel dipeptidyl peptidase IV inhibitors replacing the classical cyanopyrrolidine P1 group with other small nitrogen heterocycles are described. A unique potency enhancement was achieved with beta-branched natural and unnatural amino acids, particularly adamantylglycines, linked to a (2S,3R)-2,3-methanopyrrolidine based scaffold.
本文描述了用其他小氮杂环取代经典氰基吡咯烷P1基团的新型二肽基肽酶IV抑制剂的合成及其构效关系。与基于(2S,3R)-2,3-亚甲基吡咯烷的骨架相连的β-支链天然和非天然氨基酸，尤其是金刚烷基甘氨酸，实现了独特的活性增强。
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