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)

  • Bioorg Med Chem Lett. 2008 Jan 1;18(1):72-7. doi: 10.1016/j.bmcl.2007.11.011.
Hussein I El-Subbagh  1 ,  Hassan A El-Kashef ,  Adnan A Kadi ,  Alaa A-M Abdel-Aziz ,  Ghada S Hassan ,  Justice Tettey ,  Jochen Lehmann
Affiliations
  • 1. Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. [email protected]
PMID: 18023180 DOI: 10.1016/j.bmcl.2007.11.011
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.

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