Discovery of coumarin-dihydroquinazolinone analogs as niacin receptor 1 agonist with in-vivo anti-obesity efficacy

Autor:	L. Ravithej Singh, Koneni V. Sashidhara, Akanksha Upadhyay, Gopala Reddy Palanati, Kamakshi Sikka, Mohammad Imran Siddiqi, Ajeet Kumar, Sampa Gupta, Prem N. Yadav
Rok vydání:	2018
Předmět:	0301 basic medicine Agonist Male Models Molecular medicine.drug_class Pharmacology Receptors Nicotinic Diet High-Fat 01 natural sciences Receptors G-Protein-Coupled 03 medical and health sciences chemistry.chemical_compound Mice Structure-Activity Relationship In vivo Coumarins Drug Discovery medicine Niacin receptor 1 Animals Obesity Receptor Quinazolinones Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Organic Chemistry General Medicine Glucose Tolerance Test Coumarin Small molecule 0104 chemical sciences Mice Inbred C57BL 030104 developmental biology chemistry Anti obesity Anti-Obesity Agents
Zdroj:	European journal of medicinal chemistry. 152
ISSN:	1768-3254
Popis:	In this study, we presented rational designing and synthesis of coumarin-dihydroquinazolinone conjugates to evaluate their agonist activity at GPR109a receptor. Among the synthesized small molecule library, compound 10c displayed robust agonist action at GPR109a with EC50
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6dddafca3f5bc3cab6ad9205430c754d https://pubmed.ncbi.nlm.nih.gov/29709786 Zobrazit plný text záznamu Full Text from ScienceDirect