392244-55-2Relevant academic research and scientific papers
Synthesis, biological evaluation and molecular modeling study of thiadiazolo[3,2-a][1,3]diazepine analogues of HIE-124 as a new class of short acting hypnotics
El-Subbagh, Hussein I.,Hassan, Ghada S.,El-Taher, Kamal E.H.,El-Messery, Shahenda M.,El-Azab, Adel S.,Abdelaziz, Alaa A.-M.,Hefnawy, Mohamed M.
, p. 237 - 247 (2016)
A new series of 6,7-dihydro-[1,3,4]thiadiazolo[3,2-a][1,3]diazepine analogues were synthesized, and biological evaluated. Compound GS-62 (33) exhibited potent in?vivo short acting hypnotic activity with onset time, duration of sleep and therapeutic index of 6.4?±?0.2, 94.8?±?5.3?min, 6.62, respectively), in comparison to thiopental sodium (6). Compounds 33 did not show any sign of acute tolerance reported with the maintenance dose of 6. Meanwhile 33 potentiated the in?vivo hypnotic effect of 6 in an equimolar amounts (0.06?mmol) combination showing an onset and duration of 7.5?±?1.3, 62.5?±?5.9?min, respectively. This combination allowed the use of lower doses of both drugs to avoid the undesirable side effects. Docking studies revealed favorable interactions and binding to BDZ binding site of the GABAAreceptor especially with Arg87, Arg149, and Thr151 amino acid residues.
6,7-DIHYDRO-[1,3,4]THIADIAZOLO-[3,2-a][1,3]DIAZEPIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS HYPNOTIC OR ANESTHETIC AGENT AND METHOD FOR THEIR PREPARATION
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Paragraph 0039; 0040, (2014/04/03)
The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as hypnotic agent or anesthetic agent.
6,7-DIYDRO-[1,3,4]THIADIAZOLO-[3,2-A][1,3]DIAZEPIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS HYPNOTIC OR ANESTHETIC AGENT AND METHOD FOR THEIR PREPARATION
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Page/Page column 11, (2012/10/18)
The present invention relates to a compound of formula (1), a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as hypnotic agent or anesthetic agent.
6,7-Dihydro-[1,3,4]thiadiazolo-[3,2-a][1,3]diazepin derivatives and pharmaceutical compositions containing the same as hypnotic or anesthetic agent and method for their preparation
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Page/Page column 6, (2012/11/07)
The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as hypnotic agent or anesthetic agent.
