Open AccessDESIGN, In-silico STUDIES, SYNTHESIS, CHARACTERIZATION, AND ANTICONVULSANT ACTIVITIES OF NOVEL THIAZOLE SUBSTITUTED OXAZOLE DERIVATIVES
Author(s) -
Singagari Srilakshmi,
Raja Sundararajan
Publication year - 2022
Publication title -
rasayan journal of chemistry/rasayan journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.281
H-Index - 22
eISSN - 0976-0083
pISSN - 0974-1496
DOI - 10.31788/rjc.2022.1516762
Subject(s) - oxazole , thiazole , chemistry , potency , neurotoxicity , stereochemistry , pharmacophore , combinatorial chemistry , in vitro , organic chemistry , toxicity , biochemistry
A potent antiepileptic drug was developed by synthesizing a set of novel thiazoles substituted oxazole derivatives using multi-step synthesis. FT-IR, 1H-NMR, Mass spectroscopy, and elemental analyses are employed to confirm the structure of compounds. Molinspiration online tool was used to predict the molecular properties and molecular docking was employed to predict the antiepileptic potency of the title analogs. MES and scPTZ tests were employed to determine the antiepileptic potency of thirteen prepared novel thiazole substituted oxazole derivatives. In addition, the neurotoxicity of the compounds was also estimated using the rotarod test. Entire tested derivatives displayed varying degrees of antiepileptic and neurotoxicity potency. The pharmacological potency of prepared derivatives was compared with their chemical structures. Among fifteen tested title compounds the potent compound of this series was found to be 4-(4-(2-(4-chlorobenzylideneamino)thiazol-4-yl)benzylidene)-2-methyloxazol-5(4H)-one BTBO3 which may act as a lead molecule to find potent and safer antiepileptic drug