Bioorganic and Medicinal Chemistry Letters p. 3426 - 3430 (2010)
Update date:2022-08-04
Topics:
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
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 were identified.
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