title: New ultra-short acting hypnotic: synthesis, biological evaluation, and metabolic profile of ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a][1,3]diazepin-3-carboxylate (HIE-124).
abstract: Ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a][1,3]diazepin-3-carboxylate (HIE-124, 4) is a member of a new generation of ultra-short acting hypnotics. HIE-124 (4) exhibited potent in vivo activity with a rapid onset of action and a short duration of action, with no acute tolerance or noticeable side effects. The metabolic profile of 4 is also performed. HIE-124 (4) has the potential use as a preanesthetic medication, anesthesia inducer, and could be used with thiopental sodium to maintain anesthesia for longer duration.
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. subbagh@yahoo.com
authors.forename: Hussein I
authors.initials: HI
authors.lastname: El-Subbagh
authors.forename: Hassan A
authors.initials: HA
authors.lastname: El-Kashef
authors.forename: Adnan A
authors.initials: AA
authors.lastname: Kadi
authors.forename: Alaa A-M
authors.initials: AA
authors.lastname: Abdel-Aziz
authors.forename: Ghada S
authors.initials: GS
authors.lastname: Hassan
authors.forename: Justice
authors.initials: J
authors.lastname: Tettey
authors.forename: Jochen
authors.initials: J
authors.lastname: Lehmann
mesh_terms: D000818:Animals; D001381:Azepines / Q000378:metabolism* / Q000493:pharmacokinetics / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000378:metabolism* / Q000493:pharmacokinetics / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis / Q000378:metabolism* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051379:Mice; D013844:Thiazoles / Q000378:metabolism* / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: C526399:8-oxo-5,6,7,8-tetrahydro-thiazolo(3,2-a)(1,3)diazepin-3-carboxylate; D001381:Azepines; D002264:Carboxylic Acids; D006993:Hypnotics and Sedatives; D013844:Thiazoles