Design and synthesis of novel spirocyclic carboxylic acids as potent and orally bioavailable DGAT1 inhibitors and their biological evaluation

Autor:	Summon Koul, Suresh Kurhade, Sandeep Bhosale, Keshav Naik, Videsh Salunkhe, Sudhir Ravula, Prasad Punde, Ravikumar Velayutham, Atul Tiwari, Daniela Ahl, Srividya Malkapuram, Vamsi Mudagala, Amol Raje, Dhananjay Umrani, Suhas Tambe, Poonam Patil, Umesh Singh, Debnath Bhuniya, Narayanan Hariharan, Kasim Mookhtiar
Rok vydání:	2021
Předmět:	Oxadiazoles Organic Chemistry Clinical Biochemistry Carboxylic Acids Pharmaceutical Science Biochemistry Disease Models Animal Mice Drug Design Drug Discovery Molecular Medicine Animals Diacylglycerol O-Acyltransferase Enzyme Inhibitors Molecular Biology Triglycerides
Zdroj:	Bioorganicmedicinal chemistry letters. 62
ISSN:	1464-3405
Popis:	A series of novel spirocyclic DGAT1 inhibitors containing the oxadiazole motif were designed and synthesized for biological evaluation. Several compounds exhibited potent diacylglycerol acyltransferase 1 (DGAT1) inhibitory activity. Optimization of the series led to the identification of five lead compounds 8, 9, 10, 11 and 12 that showed excellent in-vitro activity with IC
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8687566935fcb2ba4d51bfa986746836 https://pubmed.ncbi.nlm.nih.gov/35189320 Zobrazit plný text záznamu Full Text from ScienceDirect