title: Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.
abstract: Niacin is an effective drug for raising HDL cholesterol and reducing coronary risks, but patients show low compliance with treatment due to severe facial flushing upon taking the drug. A series of bicyclic pyrazole carboxylic acids were synthesized and tested for their ability to activate the niacin receptor. One analog, 23, showed improved potency and lacked flushing at doses that effectively altered the lipid profile of rats.
authors: Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co, Inc, Rahway, NJ 07065-0900, USA. darbyrschmidt@verizon.net
authors: Darby
authors: D
authors: Schmidt
authors: Abigail
authors: A
authors: Smenton
authors: Subharekha
authors: S
authors: Raghavan
authors: Ester
authors: E
authors: Carballo-Jane
authors: Silvi
authors: S
authors: Lubell
authors: Tanya
authors: T
authors: Ciecko
authors: Tom G
authors: TG
authors: Holt
authors: Michael
authors: M
authors: Wolff
authors: Andrew
authors: A
authors: Taggart
authors: Larissa
authors: L
authors: Wilsie
authors: Mihajlo
authors: M
authors: Krsmanovic
authors: Ning
authors: N
authors: Ren
authors: Daniel
authors: D
authors: Blom
authors: Kang
authors: K
authors: Cheng
authors: Peggy E
authors: PE
authors: McCann
authors: M
authors: M
authors: Gerard Waters
authors: James
authors: J
authors: Tata
authors: Steven
authors: S
authors: Colletti
mesh_terms: D000818:Animals; D008076:Cholesterol, HDL / Q000378:metabolism; D050171:Dyslipidemias / Q000188:drug therapy*; D005230:Fatty Acids, Nonesterified / Q000378:metabolism; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D009525:Niacin / Q000737:chemistry / Q000494:pharmacology*; D018722:Nicotinic Agonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000378:metabolism
chemical_list: D008076:Cholesterol, HDL; D005230:Fatty Acids, Nonesterified; D000960:Hypolipidemic Agents; D018722:Nicotinic Agonists; D011720:Pyrazoles; D043562:Receptors, G-Protein-Coupled; D009525:Niacin