Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): A potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate

Journal of Medicinal Chemistry

Volumn 53, Issue 6, 2010, Pages 2666-2670

  Shen, Hong C ^a   Ding, Fa Xiang ^a   Raghavan, Subharekha ^a   Deng, Qiaolin ^a   Luell, Silvi ^a   Forrest, Michael J ^a   Carballo Jane, Ester ^a   Wilsie, Larissa C ^a   Krsmanovic, Mihajlo L ^a   Taggart, Andrew K ^a   Wu, Kenneth K ^a   Wu, Tsuei Ju ^a   Cheng, Kang ^a   Ren, Nina ^a   Cai, Tian Quan ^a   Chen, Qing ^a   Wang, Junying ^a   Wolff, Michael S ^a   Tong, Xinchun ^a   Holt, Tom G ^a   Waters, M Gerard ^a   Hammond, Milton L ^a   Tata, James R ^a   Colletti, Steven L ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [[3 [3 (5 HYDROXYPYRIDIN 2 YL) 1,2,4 OXADIAZOL 5 YL] 2,2 DIMETHYLPROPANOYL]AMINO]CYCLOHEX 1 ENE 1 CARBOXYLIC ACID; CARBOXYLIC ACID DERIVATIVE; CYCLOHEXENE DERIVATIVE; G PROTEIN COUPLED RECEPTOR; MK 6892; NICOTINIC ACID; PROTEIN GPR109A; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DISTRIBUTION VOLUME; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG STRUCTURE; DRUG SYNTHESIS; EXPERIMENTAL DOG; FLUSHING; MOUSE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; VASODILATATION;

ANIMALS; AREA UNDER CURVE; BINDING, COMPETITIVE; CARBOXYLIC ACIDS; CHO CELLS; CRICETINAE; CRICETULUS; CYCLOHEXANECARBOXYLIC ACIDS; CYCLOHEXENES; DOGS; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; FATTY ACIDS, NONESTERIFIED; HUMANS; METABOLIC CLEARANCE RATE; MICE; MICE, INBRED C57BL; MICE, KNOCKOUT; MODELS, CHEMICAL; MOLECULAR STRUCTURE; OXADIAZOLES; RATS; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, NICOTINIC; STRUCTURE-ACTIVITY RELATIONSHIP; VASODILATION;

EID: 77949868548     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100022r     Document Type: Article

References (20)

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