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Title: | Synthesis and Toxicity Evaluation of Some N4 -Aryl Substituted 5-Trifluoromethoxyisatin-3-thiosemicarbazones |
Authors: | Pervez, Humayun Saira, Naveeda Iqbal, Mohammad S. Yaqub, Muhammad Khan, Khalid Mohammed |
Keywords: | isatin; 5-trifluoromethoxyisatin; thiosemicarbazones; 5-trifluoromethoxyisatin 3-thiosemicarbazones; toxicity |
Issue Date: | 22-Jul-2011 |
Publisher: | Molecules |
Citation: | Pervez, Humayun, et al. "Synthesis and toxicity evaluation of some N 4-aryl substituted 5-trifluoromethoxyisatin-3-thiosemicarbazones." Molecules 16.8 (2011): 6408-6421. |
Abstract: | A series of twenty one N4 -aryl substituted 5-trifluoromethoxyisatin-3- thiosemicarbazones 3a-3u was synthesized by the reaction of trifluoromethoxyisatin 1 with different arylthiosemicarbazides 2 in aqueous ethanol (50%), containing a few drops of acetic acid. Their structures were established on the basis of analytical (CHN) and spectral (IR, 1 H-NMR, EIMS) data. All the synthesized compounds were evaluated for their toxicity potential by a brine shrimp lethality bioassay. Ten compounds i.e., 3a, 3e, 3i-3l and 3n-3q proved to be active in this assay, displaying promising toxicity (LD50 = 1.11 × 10−5 M − 1.80 × 10−4 M). Amongst these, 3k, 3n and 3o were found to be the most active ones (LD50 = 1.11 × 10−5 M − 1.43 × 10−5 M). Compound 3k showed the highest activity with a LD50 value of 1.11 × 10−5 M and can, therefore, be used as a lead for further studies. Structure-activity relationship (SAR) studies revealed that the presence of strong inductively electron-attracting trifluoromethoxy substituent at position-5 of the isatin moiety played an important role in inducing or enhancing toxic potentiality of some of the synthesized compounds. |
URI: | http://202.142.177.21/handle/123456789/2246 |
Appears in Collections: | Chemistry Department |
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