取代哌嗪类化合物作为新型二肽基肽酶IV抑制剂
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.
作者信息
Brockunier Linda L, He Jiafang, Colwell Lawrence F, Habulihaz Bahanu, He Huaibing, Leiting Barbara, Lyons Kathryn A, Marsilio Frank, Patel Reshma A, Teffera Yohannes, Wu Joseph K, Thornberry Nancy A, Weber Ann E, Parmee Emma R
机构信息
Department of Medicinal Chemistry, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2004 Sep 20;14(18):4763-6. doi: 10.1016/j.bmcl.2004.06.065.
Incorporation of a fluorophenyl beta-amino amide moiety into piperazine screening lead 2 has resulted in the discovery of a structurally novel series of potent and selective DP-IV inhibitors. Simplification of the molecule and incorporation of multiple fluorine atoms on the phenyl ring has provided low molecular weight analogs such as compound 32, which is a 19nM DP-IV inhibitor with >4000-fold selectivity over QPP.
将氟苯基β-氨基酰胺部分引入哌嗪筛选先导化合物2，从而发现了一系列结构新颖的强效且选择性的二肽基肽酶-IV（DP-IV）抑制剂。分子的简化以及在苯环上引入多个氟原子，得到了低分子量类似物，如化合物32，它是一种二肽基肽酶-IV抑制剂，对喹啉蛋白酶（QPP）的选择性大于4000倍，抑制活性为19nM。
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