Picture of industrial chimneys polluting horizon

Open Access research shaping international environmental governance...

Strathprints makes available scholarly Open Access content exploring environmental law and governance, in particular the work of the Strathclyde Centre for Environmental Law & Governance (SCELG) based within the School of Law.

SCELG aims to improve understanding of the trends, challenges and potential solutions across different interconnected areas of environmental law, including capacity-building for sustainable management of biodiversity, oceans, lands and freshwater, as well as for the fight against climate change. The intersection of international, regional, national and local levels of environmental governance, including the customary laws of indigenous peoples and local communities, and legal developments by private actors, is also a signifcant research specialism.

Explore Open Access research by SCELG or the School of Law. Or explore all of Strathclyde's Open Access research...

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 1522-2667

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.