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)

EI-Subbagh, H.I. and El-Kashef, H.A. and Kadi, A.A. and Abdel-Aziz, A.A.M. and Hassan, G.S. and Tettey, J.N.A. and Lehmann, J. (2008) 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). Bioorganic and Medicinal Chemistry Letters, 18 (1). pp. 72-77. ISSN 0960-894X

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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.

Author(s):EI-Subbagh, H.I., El-Kashef, H.A., Kadi, A.A., Abdel-Aziz, A.A.M., Hassan, G.S., Tettey, J.N.A. and Lehmann, J.
Item type:Article
ID code:19773
Keywords:synthesis, thiazolo[3, 2-a][1, 3]diazepine, ultra-short acting hypnotic, metabolic profile, Chemistry, Pharmacy and materia medica, Biochemistry, Organic Chemistry, Drug Discovery, Pharmaceutical Science, Molecular Medicine, Molecular Biology, Clinical Biochemistry
Subjects:Science > Chemistry
Medicine > Pharmacy and materia medica
Department:Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences
Depositing user: Strathprints Administrator
Date deposited:02 Jun 2010 19:21
Last modified:03 Jan 2019 12:24
URI:https://strathprints.strath.ac.uk/id/eprint/19773
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