Design, synthesis and SAR of a novel series of heterocyclic phenylpropanoic acids as GPR120 agonists

A novel series of 5-membered heterocycle-containing phenylpropanoic acid derivatives (I) was discovered as potent GPR120 agonists with low clearance, high oral bioavailability and in vivo antidiabetic activity in rodents. [Display omitted] A novel series of 5-membered heterocycle-containing phenylpr...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-08, Vol.27 (15), p.3272-3278
Hauptverfasser:	Zhang, Xuqing, Cai, Chaozhong, Winters, Michael, Wells, Michele, Wall, Mark, Lanter, James, Sui, Zhihua, Ma, Jingyuan, Novack, Aaron, Nashashibi, Imad, Wang, Yuanping, Yan, Wen, Suckow, Arthur, Hua, Hong, Bell, Austin, Haug, Peter, Clapper, Wilma, Jenkinson, Celia, Gunnet, Joseph, Leonard, James, Murray, William V.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological Availability Blood Glucose - analysis Blood Glucose - metabolism Diabetes Mellitus, Type 2 - blood Diabetes Mellitus, Type 2 - drug therapy Diabetes Mellitus, Type 2 - metabolism Drug Design GPR120 HEK293 Cells Heterocyclic Compounds - chemistry Heterocyclic Compounds - pharmacokinetics Heterocyclic Compounds - pharmacology Heterocyclic Compounds - therapeutic use Humans Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacokinetics Hypoglycemic Agents - pharmacology Hypoglycemic Agents - therapeutic use Mice, Inbred C57BL Phenylpropanoic acid Phenylpropionates - chemistry Phenylpropionates - pharmacokinetics Phenylpropionates - pharmacology Phenylpropionates - therapeutic use Receptors, G-Protein-Coupled - agonists Receptors, G-Protein-Coupled - metabolism Structure-Activity Relationship Type 2 diabetes
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Zusammenfassung:	A novel series of 5-membered heterocycle-containing phenylpropanoic acid derivatives (I) was discovered as potent GPR120 agonists with low clearance, high oral bioavailability and in vivo antidiabetic activity in rodents. [Display omitted] A novel series of 5-membered heterocycle-containing phenylpropanoic acid derivatives was discovered as potent GPR120 agonists with low clearance, high oral bioavailability and in vivo antidiabetic activity in rodents.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2017.06.028