2-（苯胺基）咪唑啉类作为前列环素受体拮抗剂的发现与构效关系研究[已校正]
Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists [corrected].
作者信息
Clark Robin D, Jahangir Alam, Severance Daniel, Salazar Rick, Chang Thomas, Chang David, Jett Mary Frances, Smith Steven, Bley Keith
机构信息
Department of Medicinal Chemistry, Roche Palo Alto, 3431 Hillview Avenue, Palo Alto, CA 94304, USA.
出版信息
Bioorg Med Chem Lett. 2004 Feb 23;14(4):1053-6. doi: 10.1016/j.bmcl.2003.10.070.
PMID:15013022
Abstract
On the basis of screening hits (1a,b), a series of selective, high affinity prostacyclin receptor antagonists was developed. The optimized lead compound 25d [(4,5-dihydro-1H-imidazol-2-yl)-[4-(4-isopropoxybenzyl)phenyl]amine] had analgesic activity in the rat.
摘要
基于筛选得到的活性化合物（1a，b），开发了一系列选择性高亲和力的前列环素受体拮抗剂。优化后的先导化合物25d [（4,5-二氢-1H-咪唑-2-基）-[4-（4-异丙氧基苄基）苯基]胺]在大鼠中具有镇痛活性。
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