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

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

Volume: 7 Issue: 2

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

Affiliation:

Keywords: 5-Nitroisatin, Thiosemicarbazones, Urease Inhibition

Abstract: 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.

Cite this article as:

Pervez Humayun, Manzoor Nazia, Yaqub Muhammad, Khan Ajmal, Khan Mohammed Khalid, Nasim Faiz-ul-Hassan and Choudhary Iqbal M., Synthesis and Urease Inhibitory Properties of Some New N4-Substituted 5-Nitroisatin-3-thiosemicarbazones, Letters in Drug Design & Discovery 2010; 7 (2) . https://dx.doi.org/10.2174/157018010790225840