J. Med. Chem

Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors

A El-Tayeb, A Qi, RA Nicholas, CE Müller

Index: El-Tayeb, Ali; Qi, Aidong; Nicholas, Robert A.; Mueller, Christa E. Journal of Medicinal Chemistry, 2011 , vol. 54, # 8 p. 2878 - 2890

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Citation Number: 25

Abstract

ABSTRACT: A large series of derivatives and analogues of the uracil nucleotides UMP, UDP, and UTP with modifications in various positions of the uracil moiety and/or the phosphate groups were synthesized and evaluated at human P2Y2, P2Y4, and P2Y6 receptors. 2--(Ar) alkylthio substitution of UMP and UDP was best tolerated by the P2Y2 receptor. 2-Phenethylthio-UMP (13e) showed an EC50 value of 1.3 μM at P2Y2 and> 70- ...