In-vivo analgesic, anti-inflammatory and central nervous system - locomotor activities of certain synthesized 2-[(1-((phenyl amino) methyl) substituted 1H-benzoimidazol-2-yl) alkyl] isoindoline-1, 3-diones.

Abstract

Two homologous series of 1, 2-disubstituted benzimidazoles carrying isoindolines (6a-n) were synthesized by mannich  type  reaction  of  2-alkyl  benzimidazolyl  isoindoline-1,3-dione  (4a-b)  with  different    substituted aromatic primary amines (5a-g)  using formaldehyde in acid as a condensing agent. The pthalic anhydride (1) and amino acids -glycine, alanine (2a-b) fused at 180° c to give 2-(1, 3-dioxoisoindolin-2-yl) carboxylic acids (3a-b). These acids undergo cyclization with 1, 2 diaminobenzene yield (4a-b). The structures of the synthesized isoindolines were confirmed by spectral analysis. The synthesized benzimidazolyl isoindoline were screened for their in-vivo antinociceptive activities. Most of the synthesized isoindolines exhibited significant analgesic and anti-inflammatory activities. Among this isoindolines 6c, 6d, 6e, 6f, 6l, 6k, 6m, 6n were showed appreciable antinociceptive potency. The isoindolines (4a-b) and (6a-n) were screened for their in-vivo central nervous system locomotor activities. Among these tested isoindolines 4a, 4b, 6a, 6b, 6e, 6f were only shows elevated central nervous system depressant potency.