Husain, S. Shaukat published the artcilep-Trifluoromethyldiazirinyl-etomidate: A Potent Photoreactive General Anesthetic Derivative of Etomidate That Is Selective for Ligand-Gated Cationic Ion Channels, Synthetic Route of 360-92-9, the publication is Journal of Medicinal Chemistry (2010), 53(17), 6432-6444, database is CAplus and MEDLINE.
We synthesized the R- and S-enantiomers of Et 1-(1-(4-(3-(trifluoromethyl)-3H-diazirin-3-yl)phenyl)ethyl)-1H-imidazole-5-carboxylate (trifluoromethyldiazirinyl-etomidate) (I), or TFD-etomidate, a novel photoactivable derivative of the stereoselective general anesthetic etomidate [R-(2-Et 1-(phenylethyl)-1H-imidazole-5-carboxylate)]. Anesthetic potency was similar to etomidate’s, but stereoselectivity was reversed and attenuated. Relative to etomidate, TFD-etomidate was a more potent inhibitor of the excitatory receptors, nAChR (nicotinic acetylcholine receptor) ((α1)2β1δ1γ1) and 5-HT3AR (serotonin type 3A receptor), causing significant inhibition at anesthetic concentrations S- but not R-TFD-etomidate enhanced currents elicited from inhibitory α1β2γ2L GABAARs by low concentrations of GABA, but with a lower efficacy than R-etomidate, and site-directed mutagenesis suggests they act at different sites. [3H]TFD-etomidate photolabeled the α-subunit of the nAChR in a manner allosterically regulated by agonists and noncompetitive inhibitors. TFD-etomidate’s novel pharmacol. is unlike that of etomidate derivatives with photoactivable groups in the ester position, which behave like etomidate, suggesting that it will further enhance our understanding of anesthetic mechanisms.
Journal of Medicinal Chemistry published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C6H10F3NO, Synthetic Route of 360-92-9.
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