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