Synthesis and Evaluation of Novel S-alkyl Phthalimide- and S-benzyl-oxadiazole-quinoline Hybrids as Inhibitors of Monoamine Oxidase and Acetylcholinesterase.

ABSTRACT: New S-alkyl phthalimide 5a-f and S-benzyl 6a-d analogs of 5-(2-phenylquinolin-4-yl)-1,3,4-oxadiazole-2-thiol (4) were prepared by reacting 4 with N-bromoalkylphthalimide and CF₃-substituted benzyl bromides in excellent yields. Spectroscopic techniques were employed to elucidate the structures of the synthesized molecules. The inhibition activity of newly synthesized molecules toward MAO-A, MAO-B, and AChE enzymes, was also assessed. All these compounds showed activity in the submicromolar range against all enzymes. Compounds 5a and 5f were found to be the most potent compounds against MAO-A (IC₅₀ = 0.91 ± 0.15 nM) and MAO-B (IC₅₀ = 0.84 ± 0.06 nM), while compound 5c showed t

SUBMITTER: Khan BA 

PROVIDER: S-EPMC9865589 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature