Anthranilic acid replacements in a niacin receptor agonist

…, FX Ding, E Carballo-Jane, S Luell, T Ciecko…

Index: Schmidt, Darby; Smenton, Abigail; Raghavan, Subharekha; Shen, Hong; Ding, Fa-Xiang; Carballo-Jane, Ester; Luell, Silvi; Ciecko, Tanya; Holt, Tom G.; Wolff, Michael; Taggart, Andrew; Wilsie, Larissa; Krsmanovic, Mihajlo; Ren, Ning; Blom, Daniel; Cheng, Kang; McCann, Peggy E.; Waters, M.Gerard; Tata, James; Colletti, Steven Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 11 p. 3426 - 3430

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Citation Number: 14

Abstract

Niacin is an effective drug for raising HDL cholesterol. However, niacin must be taken in large doses and significant side effects are often observed, including facial flushing, loss of glucose tolerance, and liver toxicity. An anthranilic acid was identified as an agonist of the niacin receptor. In order to improve efficacy and provide structural diversity, replacements for the anthranilic acid were investigated and several compounds with improved properties ...