Identified synthesis and in-vivo study of oxidized metabolites of Rimonabant via LC-ESI-MS technique

doi:10.1016/j.molstruc.2023.137023

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Title:	Identified synthesis and in-vivo study of oxidized metabolites of Rimonabant via LC-ESI-MS technique
Authors:	Tsai, Shuo-En Chung, Cheng-Yen Li, Sin-Min Zeng, Wei-Zheng Chou, Jia-Yu Jiang, Wen-Ping Huang, Guan-Jhong Lee, Der-Yen Wong, Fung Fuh
Contributors:	China Med Univ, Sch Pharm China Med Univ, Dept Chinese Pharmaceut Sci & Chinese Med Resource China Med Univ, Inst Translat Med & New Drug Dev China Med Univ, Dept Nutr China Med Univ, Master Program Pharmaceut Manufacture Chia Nan Univ Pharm & Sci, Dept Pharm Asia Univ, Dept Food Nutr & Hlth Biotechnol China Med Univ, Grad Inst Integrated Med
Keywords:	m CPBA Rimonabant Oxidized Rimonabant metabolite 4-triazoles Pyrazoles
Date:	2024
Issue Date:	2024-12-25 11:04:47 (UTC+8)
Publisher:	ELSEVIER
Abstract:	The convenient oxidation was carried out to Rimonabant and its analogue with mCPBA for the formation of their reactive biological metabolites. The lactam oxidized Rimonabant metabolite was first successfully synthesized for demonstrating the construction and characterized by NMR spectroscopic methods and the single-crystal X-ray diffraction study. Through metabolism study of Rimonabant in vivo in mice, the lactam metabolite belongs to one of many high levels of reactive oxidized Rimonabant metabolites. On the other hand, the lactam metabolite is the most stable form in snapshot PK test and displays markedly reduced brain penetrance.
Relation:	Journal of Molecular Structure, v.1298, part.1, Article 137023
Appears in Collections:	[Offices] 456

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