TY - JOUR
T1 - 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)
AU - EI-Subbagh, H.I.
AU - El-Kashef, H.A.
AU - Kadi, A.A.
AU - Abdel-Aziz, A.A.M.
AU - Hassan, G.S.
AU - Tettey, J.N.A.
AU - Lehmann, J.
PY - 2008/1/1
Y1 - 2008/1/1
N2 - 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.
AB - 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.
KW - synthesis
KW - thiazolo[3
KW - 2-a][1
KW - 3]diazepine
KW - ultra-short acting hypnotic
KW - metabolic profile
UR - http://dx.doi.org/10.1016/j.bmcl.2007.11.011
U2 - 10.1016/j.bmcl.2007.11.011
DO - 10.1016/j.bmcl.2007.11.011
M3 - Article
SN - 0960-894X
VL - 18
SP - 72
EP - 77
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 1
ER -