新型CCR2拮抗剂的设计、合成及构效关系
Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.
作者信息
Kothandaraman Shankaran, Donnely Karla L, Butora Gabor, Jiao Richard, Pasternak Alexander, Morriello Gregori J, Goble Stephen D, Zhou Changyou, Mills Sander G, Maccoss Malcolm, Vicario Pasquale P, Ayala Julia M, Demartino Julie A, Struthers Mary, Cascieri Margaret A, Yang Lihu
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2009 Mar 15;19(6):1830-4. doi: 10.1016/j.bmcl.2008.12.050. Epub 2008 Dec 24.
A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found to posses potent antagonistic activity.
一系列含有取代四氢吡喃部分的新型1-氨基环戊基-3-羧酰胺已被合成，并随后评估了它们对人CCR2受体的拮抗活性。其中类似物59被发现具有强效拮抗活性。
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