Cyclic urea derivatives as potent NK1 selective antagonists.: Part II:: Effects of fluoro and benzylic methyl substitutions
Cyclic urea derivatives as potent NK1 selective antagonists.: Part II:: Effects of fluoro and benzylic methyl substitutions
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DOI：
10.1016/j.bmcl.2005.10.072
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发表时间：
2006-02-15
影响因子：
2.7
通讯作者：
Shih, NY
中科院分区：
文献类型：
--
作者：
Shue, HJ;Chen, X;Shih, NY
本发明描述了一系列作为有效的NK 1受体拮抗剂的新型五元脲衍生物。取代的4-氟基团在苯环和引入的α-甲基基团在苄基的位置，以提高效力和持续时间的体内活性的影响进行了讨论。鉴定了几种具有高亲和力和持续体内活性的化合物。(c)2005爱思唯尔有限公司保留所有权利。
A series of novel five-membered urea derivatives as potent NK1 receptor antagonists is described. The effects of substitution of a 4-fluoro group at the phenyl ring and the introduction of an alpha-methyl group at the benzylic position to improve potency and duration of in vivo activity are discussed. Several compounds with high affinity and sustained in vivo activity were identified. (c) 2005 Elsevier Ltd. All rights reserved.