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S. Selvakumar*, I. Sudheer Babu1 and N. Chidambaranathan2
1Department of Pharmaceutical Chemistry, Sir.C.R.Reddy College of Pharmaceutical Sciences, West Godavari (Dist), Eluru - 534 007, India. 2Department of Pharmacology, K.M. College of Pharmacy,Uthangudi, Melur road, Madurai - 625 107, India.
ABSTRACT: Some new two series of 1, 2-disubstituted benzimidazolyl isoindoline derivatives (6a-n) were synthesized by mannich reaction of 2- substituted benzimidazolyl isoindolines (4a-b) with various aromatic primary amines (5a-g) with formaldehyde in acid as a condensing agent. The 2-(1,3-dioxoisoindolin-2-yl) carboxylic acids (3a-b) cyclised with 1,2 diamino benzene yield (4a-b). The pthalic anhydride (1) and amino acids (2a-b) fused at 180°C-185°C to give (3a-b). The compounds (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 and remaining isoindolines were depicted bad central nervous system depressant activity.
KEYWORDS: Benzimidazoles; benzimidazolyl isoindolines; isoindolines; central nervous system stimulant; central nervous system depressant
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