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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and In Vitro Inhibitory Potential Towards Urease of 9-Anilinoacridines and Aciridinyl Hydrazides

Author(s): Khalid Mohammed Khan, Nosheen Akbar Rao, M. Arif Lodhi, Shahnaz Perveen, M. Iqbal Choudhary and Wolfgang Voelter

Volume 4, Issue 2, 2007

Page: [114 - 121] Pages: 8

DOI: 10.2174/157018007779422523

Price: $65

Abstract

A series of 9-anilinoacridines (1-15) and acridinyl hydrazides (16-29) with structural variations at C-9 were synthesized using an improved method, and their urease enzyme inhibitory activity was evaluated. These compounds showed varying degrees of urease inhibitory activity ranging between 19.05-135.01 μM. Out of twenty-nine compounds, eight of them (3, 4, 9, 11, 13,15, 17 and 24) were found to have a good urease inhibitory potential with IC50 values of 52.11, 64.00, 56.17, 19.05, 46.32, 101.35, 35.01, and 43.56 μM, respectively, if compared to thiourea (IC50 = 21.01 μM), used as standard.

Keywords: 9-Anilinoacridines, Acridinyl hydrazides, Urease inhibition


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