Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays

被引：29

作者：

Campbell, RM ^{[1
]}

Cartwright, C ^{[1
]}

Chen, W ^{[1
]}

Chen, Y ^{[1
]}

Duzic, E ^{[1
]}

Fu, JM ^{[1
]}

Loveland, M ^{[1
]}

Manning, R ^{[1
]}

McKibben, B ^{[1
]}

Pleiman, CM ^{[1
]}

Silverman, L ^{[1
]}

Trueheart, J ^{[1
]}

Webb, DR ^{[1
]}

Wilkinson, V ^{[1
]}

Witter, DJ ^{[1
]}

Xie, XB ^{[1
]}

Castelhano, AL ^{[1
]}

机构：

[1] Cadus Pharmaceut Corp, Tarrytown, NY 10591 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(99)00398-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Evaluation of a biased "library" of pyrrolo[2,3-d]pyrimidines using yeast-based functional assays expressing human A(1)- and A(2a)-adenosine receptors, led to the A(1) selective antagonist 4b. A direct correlation between yeast functional activity and binding data was established. Practical compounds with polar residues at C-4 of the pyrrolopyrimidine system required H-bond donor functionality for high potency. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2413 / 2418

页数：6

共 17 条

[1] Canine mast cell adenosine receptors: Cloning and expression of the A(3) receptor and evidence that degranulation is mediated by the A(2B) receptor [J].