Synthesis and evaluation of dual fatty acid amide hydrolase-monoacylglycerol lipase inhibition and antinociceptive activities of 4-methylsulfonylaniline-derived semicarbazones

Autor:	Shivani Jaiswal, null Akhilesh, Ankit Uniyal, Vinod Tiwari, Senthil Raja Ayyannan
Rok vydání:	2021
Předmět:	Semicarbazones Analgesics Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Monoacylglycerol Lipases Amidohydrolases Molecular Docking Simulation Drug Discovery Molecular Medicine Humans Neuralgia Enzyme Inhibitors Molecular Biology
Zdroj:	Bioorganicmedicinal chemistry. 60
ISSN:	1464-3391
Popis:	Fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) are promising targets for neuropathic pain and other CNS disorders. Based on our previous lead compound SIH 3, we designed and synthesized a series of 4-methylsulfonylphenyl semicarbazones and evaluated for FAAH and MAGL inhibition properties. Most of the compounds showed potency towards both enzymes with leading FAAH selectivity. Compound (Z)-2-(2,6-dichlorobenzylidene)-N-(4-(methylsulfonyl)phenyl)hydrazine-1-carboxamide emerged as the lead inhibitor against both FAAH (IC
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::94e44a75972374b6c1378ae90672fa13 https://pubmed.ncbi.nlm.nih.gov/35296453 Zobrazit plný text záznamu Full Text from ScienceDirect