Letters in Drug Design & Discovery

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


Synthesis and Urease Inhibitory Properties of Some New N4-Substituted 5-Nitroisatin-3-thiosemicarbazones

Author(s): Humayun Pervez, Nazia Manzoor, Muhammad Yaqub, Ajmal Khan, Khalid Mohammed Khan, Faiz-ul-Hassan Nasim, M. Iqbal Choudhary.


A series of seventeen N4-substituted 5-nitroisatin-3-thiosemicarbazones 2a-2q has been synthesized and screened for in vitro urease inhibitory activities. Compounds 2a-2d, 2g, 2i, 2j and 2q were found to be potent inhibitors of the enzyme. Of these, 2c exhibited a potent inhibitory activity with IC50 value 16.4 μM and may act as a lead molecule for further studies. Structure-activity relationship studies revealed that electronic effects of the substituents play an important role in the urease inhibitory potential of the synthetic compounds.

Keywords: 5-Nitroisatin, Thiosemicarbazones, Urease Inhibition

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Article Details

Year: 2010
Page: [102 - 108]
Pages: 7
DOI: 10.2174/157018010790225840
Price: $58