502881-14-3Relevant academic research and scientific papers
5-Nitroisatin-derived thiosemicarbazones: Potential antileishmanial agents
Pervez, Humayun,Manzoor, Nazia,Yaqub, Muhammad,Khan, Khalid Mohammed
, p. 628 - 632 (2014/12/11)
A series of 29 previously reported N4-substituted 5-nitroisatin-3-thiosemicarbazones 2-30 has been screened for leishmanicidal potential. Compounds 2-4, 7, 8, 10-13, 15-19, 21, 23, 24, 26, 28 and 30 exhibited good to excellent antileishmanial activities with IC50 values ranging from 0.44±0.02 to 32.38±0.66μg/mL. Of these, 5, 7, 19 and 28 proved to be the most active antileishmanial agents, displaying activities with IC50 values 1.78±0.35, 0.44±0.02, 1.91±0.04 and 4.28±0.75μg/mL, respectively, which were even better than the standard drug, pentamidine (IC50=5.09±0.04μg/mL). This study presents the first example of exhibition of leishmanicidal potential by isatin-thiosemicarbazones and as such furnishes a solid basis for further research on these compounds to develop more potent antileishmanial agents.
Synthesis and urease inhibitory properties of some new N 4-substituted 5-nitroisatin-3-thiosemicarbazones
Pervez, Humayun,Manzoor, Nazia,Yaqub, Muhammad,Khan, Ajmal,Khan, Khalid Mohammed,Nasim, Faiz-Ul-Hassan,Choudhary, M. Iqbal
experimental part, p. 102 - 108 (2011/01/13)
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.
