SUBSTITUTED 2,4-DIAMINOQUINAZOLINES AND 2,4-DIAMINO-8-ALKYLPURINES AS ANTAGONISTS OF THE NEUROKININ-2 (NK2) RECEPTOR

被引：8
作者：
JACOBS, RT [1 ]
MAUGER, RC [1 ]
ULATOWSKI, TG [1 ]
AHARONY, D [1 ]
BUCKNER, CK [1 ]
机构：
[1] ZENECA PHARMACEUT, DEPT PHARMACOL, WILMINGTON, DE 19850 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 23期
关键词：
D O I：
10.1016/0960-894X(95)00502-K
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Modification of the heterocyclic nucleus of a lead pyrrolopyrimidine (1) found to be active as an antagonist at the neurokinin-2 (NK2) receptor is described. Compounds based on the purine nucleus (3) were found to be particularly interesting, and were modified in the C(2), C(4) and C(8) substituents to afford compounds with high potency.
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页码：2879 / 2884
页数：6
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