Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists

A series of 2-dialkylamino-4-phenylpyrimidines (7) was designed and synthesized as CRF(1) antagonists. SAR studies of this series resulted in the discovery of potent and selective antagonists 7b and 7n bearing a 4-(2,4,6-trisubstituted-phenyl) ring and a bulky 2-(N-bis(cyclopropane)methyl-N-propyl)a...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 14; no. 9; pp. 2083 - 2086
Main Authors:	Huang, Charles Q, Grigoriadis, Dimitri E, Liu, Zhengyu, McCarthy, James R, Ramphal, John, Webb, Thomas, Whitten, Jeffrey P, Xie, Michael Y, Chen, Chen
Format:	Journal Article
Language:	English
Published:	England 03-05-2004
Subjects:	Animals CHO Cells Cricetinae Drug Design Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Rats Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors Structure-Activity Relationship
Online Access:	Get full text
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Summary:	A series of 2-dialkylamino-4-phenylpyrimidines (7) was designed and synthesized as CRF(1) antagonists. SAR studies of this series resulted in the discovery of potent and selective antagonists 7b and 7n bearing a 4-(2,4,6-trisubstituted-phenyl) ring and a bulky 2-(N-bis(cyclopropane)methyl-N-propyl)amino group.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2004.02.053