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.

journal_name

Bioorg Med Chem Lett

authors

El-Subbagh HI,El-Kashef HA,Kadi AA,Abdel-Aziz AA,Hassan GS,Tettey J,Lehmann J

doi

10.1016/j.bmcl.2007.11.011

subject

Has Abstract

pub_date

2008-01-01 00:00:00

pages

72-7

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)01320-0

journal_volume

18

pub_type

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