Abstract
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.
Keywords:
GPR120; Phenylpropanoic acid; Type 2 diabetes.
Copyright © 2017 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Biological Availability
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Blood Glucose / analysis
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Blood Glucose / metabolism
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Diabetes Mellitus, Type 2 / blood
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Diabetes Mellitus, Type 2 / drug therapy
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Diabetes Mellitus, Type 2 / metabolism
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Drug Design
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HEK293 Cells
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Heterocyclic Compounds / chemistry
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Heterocyclic Compounds / pharmacokinetics
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Heterocyclic Compounds / pharmacology
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Heterocyclic Compounds / therapeutic use
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Humans
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Hypoglycemic Agents / chemistry*
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Hypoglycemic Agents / pharmacokinetics
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Hypoglycemic Agents / pharmacology*
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Hypoglycemic Agents / therapeutic use
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Mice, Inbred C57BL
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Phenylpropionates / chemistry*
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Phenylpropionates / pharmacokinetics
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Phenylpropionates / pharmacology*
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Phenylpropionates / therapeutic use
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Receptors, G-Protein-Coupled / agonists*
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Receptors, G-Protein-Coupled / metabolism
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Structure-Activity Relationship
Substances
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Blood Glucose
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FFAR4 protein, human
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Heterocyclic Compounds
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Hypoglycemic Agents
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Phenylpropionates
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Receptors, G-Protein-Coupled
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3-phenylpropionic acid