1. Academic Validation
  2. 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)

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

Affiliation

  • 1 Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. subbagh@yahoo.com
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-129451
    睡眠剂