Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A

Bioorganic & Medicinal Chemistry Letters
2007.0

Abstract

A urea class of high affinity niacin receptor agonists was discovered. Compound 1a displayed good PK, better in vivo efficacy in reducing FFA in mouse than niacin, and no vasodilation in a mouse model. Compound 1q demonstrated equal affinity to GPR109A as niacin.

Knowledge Graph

Similar Paper

Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A
Bioorganic & Medicinal Chemistry Letters 2007.0
Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A
Bioorganic & Medicinal Chemistry Letters 2020.0
Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A
Bioorganic & Medicinal Chemistry Letters 2008.0
Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a)
Bioorganic & Medicinal Chemistry Letters 2010.0
Discovery of coumarin-dihydroquinazolinone analogs as niacin receptor 1 agonist with in-vivo anti-obesity efficacy
European Journal of Medicinal Chemistry 2018.0
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a
Bioorganic & Medicinal Chemistry Letters 2007.0
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 2010.0
Discovery of Biaryl Anthranilides as Full Agonists for the High Affinity Niacin Receptor
Journal of Medicinal Chemistry 2007.0
Discovery of Novel Tricyclic Full Agonists for the G-Protein-Coupled Niacin Receptor 109A with Minimized Flushing in Rats
Journal of Medicinal Chemistry 2009.0
5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b
Bioorganic & Medicinal Chemistry Letters 2009.0