1402012-80-9

Upstream product

• 1122-91-4 4-bromo-benzaldehyde 
• 36449-43-1 2-(4-bromobenzylidene)hydrazine carbothioamide 
• 13178-12-6 5-(4-bromophenyl)-1,3,4-thiadiazol-2-amine 
• 392244-72-3 N-[5-(4-bromophenyl)-1,3,4-thiadiazol-2-yl]-4-chlorobutanamide 

Relevant academic research and scientific papers

Thiadiazolodiazepine analogues as a new class of neuromuscular blocking agents: Synthesis, biological evaluation and molecular modeling study

The synthesis, biological evaluation and molecular modeling study of 6,7-dihydro-[1,3,4] thiadiazolo[3,2-a][1,3]diazepine analogues as new class of neuromuscular blocking agents are described. The new compounds act via competitive mechanism with ACh which

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

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 DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS NEUROMUSCULAR BLOCKER OR SKELETAL MUSCLE RELAXANT, AND METHOD FOR THE PREPARATION

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 neuromuscular blocker or skeletal muscle relaxant.

6,7-DIHYDRO-[1,3,4]THIADIAZOLO-[3,2-A][1,3]DIAZEPIN DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS NEUROMUSCULAR BLOCKER OR SKELETAL MUSCLE RELAXANT, AND METHOD FOR THE PREPARATION

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 neuromuscular blocker or skeletal muscle relaxant.

6,7-dihydro-[1,3,4]thiadiazolo-[3,2-a][1,3]diazepin derivatives and pharmaceutical composition containing the same as neuromuscular blocker or skeletal muscle relaxant, and method for the preparation

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 neuromuscular blocker or skeletal muscle relaxant.