3034-57-9Relevant academic research and scientific papers
Synthesis, biological evaluation and molecular modeling study of some new thiazolodiazepine analogs as CNS active agents
Al-Rashood, Sarah T.A.,Hassan, Ghada S.,El-Messery, Shahenda M.,El-Taher, Kamal E.H.,Hefnawy, Mohamed M.,Al-Omar, Mahmmed A.,El-Subbagh, Hussein I.
supporting information, p. 445 - 453 (2016/01/09)
New derivatives of ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a][1,3]diazepin-3-carboxylate (HIE-124, 3), were synthesized as continuation to our previous patented efforts. Compounds 15 and 20 showed marginal hypnotic potency compared to 3. Compounds 15 (0.78 mmol/kg) and 20 (0.39 mmol/kg) showed remarkable 100% protection against PTZ induced convulsions with two and four fold increase in activity than sodium valproate (1.38 mmol/kg), respectively. Molecular modeling studies showed hydrogen bonding interaction between 15 and Thr56 residues at the binding site of GABAA. Superposition, flexible alignment and surface mapping of 15, 20 and diazepam supports their biological resemblance where ADMET study suggested that those compounds could be used as oral anticonvulsants.
NEW AMINOTHIAZOLES AS FBPASE INHIBITORS FOR DIABETES
-
, (2009/06/27)
Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.
4-methylthiazole derivatives, their methods of preparation and the pharmaceutical compositions in which they are present
-
, (2008/06/13)
The present invention relates to novel 4-methylthiazole derivatives, to tr methods of preparation and to the pharmaceutical compositions in which they are present. According to the invention, these derivatives have the general formula STR1 in which n is e
