Picture of neon light reading 'Open'

Discover open research at Strathprints as part of International Open Access Week!

23-29 October 2017 is International Open Access Week. The Strathprints institutional repository is a digital archive of Open Access research outputs, all produced by University of Strathclyde researchers.

Explore recent world leading Open Access research content this Open Access Week from across Strathclyde's many research active faculties: Engineering, Science, Humanities, Arts & Social Sciences and Strathclyde Business School.

Explore all Strathclyde Open Access research outputs...

Strathprints

Synthesis, ultra-short acting hypnotic activity, and metabolic profile of ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a] [1,3]diazepin-3-carboxylate (HIE-124)

Kadi, A.A. and El-Kashef, H.A. and Abdel-Aziz, A.A.M. and Hassan, G. and Tettey, J.N.A. and Grant, M.H. and Lehmann, J. and El-Subbagh, H.I. (2008) Synthesis, ultra-short acting hypnotic activity, and metabolic profile of ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a] [1,3]diazepin-3-carboxylate (HIE-124). ChemInform, 39 (22). ISSN 0931-7597

Full text not available in this repository. Request a copy from the Strathclyde author

Abstract

The synthesis and biological evaluation of ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a][1,3]diazepin-3-carboxylate (HIE-124, 4), as a member of a new generation of ultra-short acting hypnotics is described. HIE-124 4 exhibited potent in-vivo activity with a very rapid onset of action and a shorter duration of action with no acute tolerance or noticeable side effects than thiopental sodium. The rat in-vivo and in-vitro metabolic profile of 4 is also described. Urine was pooled from a number of animals and analyzed using electrospray liquid chromatography mass spectrometry (ESI LC-MS). HIE-124 4 was incubated with rat-liver microsomal and rat-liver hepatocyte preparations then similarly analyzed. The only metabolic product of both in-vitro and in-vivo experiments is the carboxylic acid derivative 5. HIE-124 4 has the potential use not only as a pre-anesthetic medication and as anesthesia inducer but also has the potential to be used with thiopental sodium to maintain anesthesia for longer duration.

Item type: Article
ID code: 18402
Notes: Full version of this article published in: Archiv der Pharmazie (2008), 341 (2), pp81-89. PMID: 18214840 (This is a variant record)
Keywords: multi-membered n-heterocycles, ring closure reactions, pharmacology, medicinal chemistry, vaccines, serums, Bioengineering, Engineering (General). Civil engineering (General), Physical and Theoretical Chemistry, Library and Information Sciences, Computer Science Applications, Computer Graphics and Computer-Aided Design
Subjects: Technology > Engineering (General). Civil engineering (General) > Bioengineering
Technology > Engineering (General). Civil engineering (General)
Department: Faculty of Engineering > Bioengineering
Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences
Depositing user: Ms Ashley Urie
Date deposited: 26 Mar 2010 15:26
Last modified: 18 Oct 2017 02:16
Related URLs:
URI: https://strathprints.strath.ac.uk/id/eprint/18402
Export data:
CORE (COnnecting REpositories)