Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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, Wolfgang Voelter.

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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Article Details

VOLUME: 4
ISSUE: 2
Year: 2007
Page: [114 - 121]
Pages: 8
DOI: 10.2174/157018007779422523
Price: $58