Design, In-Silico Studies, Synthesis, Characterization, and Anticonvulsant Activities of Novel Thiazolidin-4-One Substituted Thiazole Derivatives

Abstract

A series of novel thiazolidine-4-one substituted thiazoles were prepared using multi-step synthesis and screened for their antiepileptic potency. The chemical nature of the prepared derivatives was confirmed using FT-IR, elemental analyses, Mass spectroscopy, and 1H-NMR. Molecular properties and antiepileptic potency of the novel thiazoles were predicted using in-silico models such as molinspiration online tool and molecular docking, respectively. In-vivo antiepileptic potency of the entire title compounds was determined using MES and scPTZ method. Additionally, the rotorod test was employed to determine the neurotoxicity of the synthesized derivatives. Entire title analogs displayed -varying degrees of antiepileptic and neurotoxicity potency. The pharmacological potency of tested compounds was compared with their chemical structures. 2-(4-Nitrophenyl)-3-(4-((4-phenylthiazol-2-ylimino)methyl)phenyl) thiazolidin-4-one (PTT6) was found to be the very active derivative of this series among thirteen tested derivatives. Thus, this analog may act as a lead molecule to find potent and safer antiepileptic drugs.