Novel GABAA Agonist Entities: Pharmacological Investigation and Molecular Modeling Study of Thiazolo- and Thiadiazolo-[3,2-a][1,3]diazepine Analogs

Mini Rev Med Chem. 2021;21(9):1048-1057. doi: 10.2174/1389557521999201230195733.

Abstract

Thiazolo- and thiadiazolo-[3,2-a][1,3]diazepines and their patented derivatives, tested with diverse CNS pharmacological activities, constitute an important class of compounds for new drug development. Therefore, research efforts were continued to design, synthesize, and evaluate compounds for their ultra-short, short-acting hypnotic, anticonvulsant, and neuromuscular blocking activities. The present review provides a summary of the work accomplished by these heterocycles and their biological evaluation.

Keywords: Thiazolo[3,2-a][1,3]diazepines; anticonvulsants; molecular modeling studies.; neuromuscular blockers; short-acting hypnotics; thiadiazolo[3,2-a][1,3]diazepines; ultra-short-acting hypnotics.

Publication types

  • Review

MeSH terms

  • Animals
  • Anticonvulsants / chemistry
  • Anticonvulsants / pharmacology*
  • Azepines / chemistry
  • Azepines / pharmacology*
  • GABA-A Receptor Agonists / chemistry
  • GABA-A Receptor Agonists / pharmacology*
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Neuromuscular Blocking Agents / chemistry
  • Neuromuscular Blocking Agents / pharmacology*
  • Receptors, GABA-A / metabolism*
  • Thiazoles / chemistry
  • Thiazoles / pharmacology*

Substances

  • Anticonvulsants
  • Azepines
  • GABA-A Receptor Agonists
  • Neuromuscular Blocking Agents
  • Receptors, GABA-A
  • Thiazoles