Synthetic Route of C6H13NOIn 2017 ,《Structure-Affinity Relationships and Structure-Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists》 was published in Journal of Medicinal Chemistry. The article was written by Xia, Lizi; de Vries, Henk; Lenselink, Eelke B.; Louvel, Julien; Waring, Michael J.; Cheng, Leifeng; Pahlen, Sara; Petersson, Maria J.; Schell, Peter; Olsson, Roine I.; Heitman, Laura H.; Sheppard, Robert J.; IJzerman, Adriaan P.. The article contains the following contents:
The synthesis and biol. evaluation of a series of 1,2-diarylimidazol-4-carboxamide derivatives, e.g. I, developed as CB1 receptor antagonists is reported. These were evaluated in a radioligand displacement binding assay, a [35S]GTPγS binding assay, and in a competition association assay that enables the relatively fast kinetic screening of multiple compounds The compounds show high affinities and a diverse range of kinetic profiles at the CB1 receptor and their structure-kinetic relationships (SKRs) were established. Using the recently resolved hCB1 receptor crystal structures, a modeling study was performed that sheds light on the crucial interactions for both the affinity and dissociation kinetics of this family of ligands. Evidence is provided that, next to affinity, addnl. knowledge of binding kinetics is useful for selecting new hCB1 receptor antagonists in the early phases of drug discovery. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Synthetic Route of C6H13NO)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Synthetic Route of C6H13NO
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