Synthesis, biological evaluation and molecular modeling study of some new thiazolodiazepine analogs as CNS active agents.

@article{AlRashood2016SynthesisBE,
  title={Synthesis, biological evaluation and molecular modeling study of some new thiazolodiazepine analogs as CNS active agents.},
  author={Sarah T A Al-Rashood and G. S. Hassan and S. El-Messery and Kamal E H El-Taher and M. Hefnawy and M. A. Al-Omar and H. El-Subbagh},
  journal={Bioorganic & medicinal chemistry letters},
  year={2016},
  volume={26 2},
  pages={
          445-453
        }
}
  • Sarah T A Al-Rashood, G. S. Hassan, +4 authors H. El-Subbagh
  • Published 2016
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 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 (0.78mmol/kg) and 20 (0.39mmol/kg) showed remarkable 100% protection against PTZ induced convulsions with two and four fold increase in activity than sodium valproate (1.38mmol/kg), respectively. Molecular modeling studies showed hydrogen… CONTINUE READING
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