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
Letters in Drug Design & Discovery
Title: Synthesis and In Vitro Inhibitory Potential Towards Urease of 9-Anilinoacridines and Aciridinyl Hydrazides
Volume: 4 Issue: 2
Author(s): Khalid Mohammed Khan, Nosheen Akbar Rao, M. Arif Lodhi, Shahnaz Perveen, M. Iqbal Choudhary and Wolfgang Voelter
Affiliation:
Keywords: 9-Anilinoacridines, Acridinyl hydrazides, Urease inhibition
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.
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Cite this article as:
Mohammed Khan Khalid, Akbar Rao Nosheen, Arif Lodhi M., Perveen Shahnaz, Iqbal Choudhary M. and Voelter Wolfgang, Synthesis and In Vitro Inhibitory Potential Towards Urease of 9-Anilinoacridines and Aciridinyl Hydrazides, Letters in Drug Design & Discovery 2007; 4 (2) . https://dx.doi.org/10.2174/157018007779422523
DOI https://dx.doi.org/10.2174/157018007779422523 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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