Synthesis and structure–activity relationships of carboxylic acid derivatives of pyridoxal as P2X receptor antagonists

KY Jung, JH Cho, JS Lee, HJ Kim, YC Kim

Index: Jung, Kwan-Young; Cho, Joong-Heui; Lee, Jung Sun; Kim, Hyo Jun; Kim, Yong-Chul Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 9 p. 2643 - 2650

Full Text: HTML

Citation Number: 5

Abstract

Carboxylic acid derivatives of pyridoxal were developed as potent P2X1 and P2X3 receptor antagonists with modifications of a lead compound, pyridoxal-5′-phosphate-6-azophenyl- 2′, 5′-disulfonate (5b, iso-PPADS). The designing strategies included the modifications of aldehyde, phosphate or sulfonate groups of 5b, which may be interacted with lysine residues of the receptor binding pocket, to weak anionic carboxylic acid groups. The ...