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).
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.
El-Subbagh
Hussein I
HI
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. subbagh@yahoo.com
El-Kashef
Hassan A
HA
Kadi
Adnan A
AA
Abdel-Aziz
Alaa A-M
AA
Hassan
Ghada S
GS
Tettey
Justice
J
Lehmann
Jochen
J
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*
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