1333495-01-4Relevant academic research and scientific papers
Synthesis and biological evaluation of some N4-substituted 5-nitroisatin-3-thiosemicarbazones
Pervez, Humayun,Manzoor, Nazia,Yaqub, Muhammad,Nasim, Faiz-Ul-Hassan,Khan, Khalid M.
, p. 2251 - 2262 (2012)
A series of 5-nitroisatin-3-thiosemicarbazones 2a-2l was synthesised and evaluated for selected biological activities. The brine shrimp lethality bioassay was carried out to study their in vitro cytotoxicity potential and besides, their antifungal, phytotoxic and urease inhibitory effects were also investigated. Only compound 2j proved to be active in the brine shrimp assay exhibiting LD50 value 1.16 × 10-3 M. Compounds 2a and 2d displayed moderate antifungal activity (50 and 40%, respectively) against M. canis. Similarly, compound 2l exhibited moderate activity (40%) against the fungal strain, A. flavus. In phytotoxicity assay, all the synthesised compounds including the reference point 2m showed weak to moderate (20-60%) activity at the highest tested concentrations (1,000 μg and 500 μg/ml, respectively). In urease inhibition assay, compounds 2a, 2i and 2k proved to be potent inhibitors demonstrating pronounced inhibition with IC50 values 0.440, 0.901 and 27.880 μM, respectively. These compounds may act as leads for further studies. Springer Science+Business Media, LLC 2011.
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.
