Synthesis and pharmacological evaluation of second-generation phosphatidic acid derivatives as lysophosphatidic acid receptor ligands

GG Durgam, R Tsukahara, N Makarova…

Index: Durgam, Gangadhar G.; Tsukahara, Ryoko; Makarova, Natalia; Walker, Michelle D.; Fujiwara, Yuko; Pigg, Kathryn R.; Baker, Daniel L.; Sardar, Vineet M.; Parrill, Abby L.; Tigyi, Gabor; Miller, Duane D. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 3 p. 633 - 640

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Citation Number: 51

Abstract

Short-chain phosphatidic acid derivatives, dioctanoyl glycerol pyrophosphate (DGPP 8: 0, 1) and phosphatidic acid 8: 0 (PA 8: 0, 2), were previously identified as subtype-selective LPA1 and LPA3 receptor antagonists. Recently, we reported that the replacement of the phosphate headgroup by thiophosphate in a series of fatty alcohol phosphates (FAP) improves agonist as well as antagonist activities at LPA GPCR. Here, we report the ...