Design, Synthesis, and Structure− Activity Relationship Studies of Novel 2, 4, 6-Trisubstituted-5-pyrimidinecarboxylic Acids as Peroxisome Proliferator-Activated …

…, K Kiyota, S Isogai, M Iwago, T Shinozaki…

Index: Seto, Shigeki; Okada, Kyoko; Kiyota, Koichi; Isogai, Shigeki; Iwago, Maki; Shinozaki, Takehiro; Kitamura, Yoshiaki; Kohno, Yasushi; Murakami, Koji Journal of Medicinal Chemistry, 2010 , vol. 53, # 13 p. 5012 - 5024

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Citation Number: 13

Abstract

A series of novel 2, 4, 6-trisubstitutedpyrimidine-5-carboxylic acid derivatives were designed and synthesized with the intent of producing a peroxisome proliferator-activated receptor γ (PPARγ) partial agonist for antidiabetic agents. A pharmacophore-driven approach of in- house screening identified compound 7, which led to the identification of compound 9 featuring a 2, 4, 6-trisubstituted pyrimidine-5-carboxylic acid core. Structure− activity ...