Abstract

DESIGN, SYNTHESIS AND EVALUATION OF SOME NEW 4-AMINOBENZOIC ACID DERIVATIVES AS POTENTIAL COGNITION ENHANCER

Shashi Kant Singh, Saurabh K. Sinha and Mrunal K. Shirsat*

ABSTRACT

A series of new Schiff bases from p-amino benzoic acid has been designed, synthesized and evaluated for cognition enhancing activities through the inhibition of acetylcholinesterase (AChE) and by passive avoidance model. The results illustrated a significant cognition enhancing effect on passive avoidance test with a significant reversal of scopolamine-induced amnesia, which is comparable with standard drug rivastigmine. The in-vitro study of synthesized compounds showed maximum activity of compound-9 compared to standard drug rivastigmine, whereas its enzyme kinetic study revealed a non-competitive inhibition of acetycholinesterase (AChE), which may be attributed to a possible interaction of compound with the peripheral anionic site (PAS) of AChE and was also confirmed by molecular docking studies.

Keywords: 4-aminobenzoic acid, acetycholinesterase, passive avoidance test, rivastigmine.