title: Anthranilic acid replacements in a niacin receptor agonist.
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 were identified.
authors.affiliation: Department of Medicinal Chemistry, Merck & Co., Rahway, NJ 07065, USA. darbyrschmidt@verizon.net
authors.forename: Darby
authors.initials: D
authors.lastname: Schmidt
authors.forename: Abigail
authors.initials: A
authors.lastname: Smenton
authors.forename: Subharekha
authors.initials: S
authors.lastname: Raghavan
authors.forename: Hong
authors.initials: H
authors.lastname: Shen
authors.forename: Fa-Xiang
authors.initials: FX
authors.lastname: Ding
authors.forename: Ester
authors.initials: E
authors.lastname: Carballo-Jane
authors.forename: Silvi
authors.initials: S
authors.lastname: Luell
authors.forename: Tanya
authors.initials: T
authors.lastname: Ciecko
authors.forename: Tom G
authors.initials: TG
authors.lastname: Holt
authors.forename: Michael
authors.initials: M
authors.lastname: Wolff
authors.forename: Andrew
authors.initials: A
authors.lastname: Taggart
authors.forename: Larissa
authors.initials: L
authors.lastname: Wilsie
authors.forename: Mihajlo
authors.initials: M
authors.lastname: Krsmanovic
authors.forename: Ning
authors.initials: N
authors.lastname: Ren
authors.forename: Daniel
authors.initials: D
authors.lastname: Blom
authors.forename: Kang
authors.initials: K
authors.lastname: Cheng
authors.forename: Peggy E
authors.initials: PE
authors.lastname: McCann
authors.forename: M Gerard
authors.initials: MG
authors.lastname: Waters
authors.forename: James
authors.initials: J
authors.lastname: Tata
authors.forename: Steven
authors.initials: S
authors.lastname: Colletti
mesh_terms: D001682:Biological Availability; D009525:Niacin / Q000378:metabolism*; D011955:Receptors, Drug / Q000378:metabolism*; D062367:ortho-Aminobenzoates / Q000737:chemistry*
chemical_list: D011955:Receptors, Drug; D062367:ortho-Aminobenzoates; C031385:anthranilic acid; D009525:Niacin