从ATP到AZD6140：一种用于预防血栓形成的口服活性可逆P2Y12受体拮抗剂的发现。
From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.
作者信息
Springthorpe Brian, Bailey Andrew, Barton Patrick, Birkinshaw Timothy N, Bonnert Roger V, Brown Roger C, Chapman David, Dixon John, Guile Simon D, Humphries Robert G, Hunt Simon F, Ince Francis, Ingall Anthony H, Kirk Ian P, Leeson Paul D, Leff Paul, Lewis Richard J, Martin Barrie P, McGinnity Dermot F, Mortimore Michael P, Paine Stuart W, Pairaudeau Garry, Patel Anil, Rigby Aaron J, Riley Robert J, Teobald Barry J, Tomlinson Wendy, Webborn Peter J H, Willis Paul A
机构信息
AstraZeneca R&D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK.
出版信息
Bioorg Med Chem Lett. 2007 Nov 1;17(21):6013-8. doi: 10.1016/j.bmcl.2007.07.057. Epub 2007 Aug 19.
Starting from adenosine triphosphate (ATP), the identification of a novel series of P2Y(12) receptor antagonists and exploitation of their SAR is described. Modifications of the acidic side chain and the purine core and investigation of hydrophobic substituents led to a series of neutral molecules. The leading compound, 17 (AZD6140), is currently in a large phase III clinical trial for the treatment of acute coronary syndromes and prevention of thromboembolic clinical sequelae.
从三磷酸腺苷（ATP）开始，描述了一系列新型P2Y(12)受体拮抗剂的鉴定及其构效关系（SAR）的研究。对酸性侧链和嘌呤核心进行修饰，并研究疏水取代基，得到了一系列中性分子。先导化合物17（AZD6140）目前正处于一项大型III期临床试验中，用于治疗急性冠状动脉综合征和预防血栓栓塞的临床后遗症。
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