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Ding, Fa-Xiang; Shen, Hong C.; Wilsie, Larrisa C.; Krsmanovic, Mihajlo L.; Taggart, Andrew K.; Ren, Ning; Cai, Tian-Quan; Wang, Junying; Tong, Xinchun; Holt, Tom G.; Chen, Qing; Gerard Waters, M.; Hammond, Milton L.; Tata, James R.; Colletti, Steven L.
Bioorganic & medicinal chemistry letters, 06/2010, Letnik: 20, Številka: 11Journal Article
A series of pyrazolyl propionyl cyclohexenamides were discovered as full agonists for the high affinity niacin receptor GPR109A. The structure–activity relationship (SAR) studies were aimed to improve activity on GPR109A, reduce Cytochrome P450 2C8 (CYP2C8) and Cytochrome P450 2C9 (CYP2C9) inhibition, reduce serum shift and improve pharmacokinetic (PK) profiles. A series of pyrazolyl propionyl cyclohexenamides were discovered as full agonists for the high affinity niacin receptor GPR109A. The structure–activity relationship (SAR) studies were aimed to improve activity on GPR109A, reduce Cytochrome P450 2C8 (CYP2C8) and Cytochrome P450 2C9 (CYP2C9) inhibition, reduce serum shift and improve pharmacokinetic (PK) profiles.
