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)

H.I. EI-Subbagh, H.A. El-Kashef, A.A. Kadi, A.A.M. Abdel-Aziz, G.S. Hassan, J.N.A. Tettey, J. Lehmann

Research output: Contribution to journalArticle

12 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)72-77
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number1
DOIs
Publication statusPublished - 1 Jan 2008

Keywords

  • synthesis
  • thiazolo[3
  • 2-a][1
  • 3]diazepine
  • ultra-short acting hypnotic
  • metabolic profile

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