Synthesis and biological evaluation of some N4-substituted 5-nitroisatin-3-thiosemicarbazones
Identifieur interne : 000D12 ( Main/Exploration ); précédent : 000D11; suivant : 000D13Synthesis and biological evaluation of some N4-substituted 5-nitroisatin-3-thiosemicarbazones
Auteurs : Humayun Pervez [Pakistan] ; Nazia Manzoor [Pakistan] ; Muhammad Yaqub [Pakistan] ; Faiz-Ul-Hassan Nasim [Pakistan] ; Khalid M. Khan [Pakistan, États-Unis]Source :
- Medicinal Chemistry Research [ 1054-2523 ] ; 2012-09-01.
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Abstract
Abstract: 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.
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DOI: 10.1007/s00044-011-9745-7
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Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, 75270, Karachi</wicri:regionArea><wicri:noRegion>Karachi</wicri:noRegion></affiliation><affiliation wicri:level="1"><country wicri:rule="url">États-Unis</country></affiliation></author></analytic><monogr></monogr><series><title level="j">Medicinal Chemistry Research</title><title level="j" type="abbrev">Med Chem Res</title><idno type="ISSN">1054-2523</idno><idno type="eISSN">1554-8120</idno><imprint><publisher>Springer-Verlag</publisher><pubPlace>New York</pubPlace><date type="published" when="2012-09-01">2012-09-01</date><biblScope unit="volume">21</biblScope><biblScope unit="issue">9</biblScope><biblScope unit="page" from="2251">2251</biblScope><biblScope unit="page" to="2262">2262</biblScope></imprint><idno type="ISSN">1054-2523</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">1054-2523</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>5-Nitroisatin</term><term>Antifungal</term><term>Cytotoxicity</term><term>Phytotoxicity</term><term>Thiosemicarbazones</term><term>Urease inhibition</term></keywords></textClass><langUsage><language ident="en">en</language></langUsage></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Abstract: 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. 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Khan</name><name sortKey="Manzoor, Nazia" sort="Manzoor, Nazia" uniqKey="Manzoor N" first="Nazia" last="Manzoor">Nazia Manzoor</name><name sortKey="Nasim, Faiz Ul Hassan" sort="Nasim, Faiz Ul Hassan" uniqKey="Nasim F" first="Faiz-Ul-Hassan" last="Nasim">Faiz-Ul-Hassan Nasim</name><name sortKey="Yaqub, Muhammad" sort="Yaqub, Muhammad" uniqKey="Yaqub M" first="Muhammad" last="Yaqub">Muhammad Yaqub</name></country><country name="États-Unis"><noRegion><name sortKey="Khan, Khalid M" sort="Khan, Khalid M" uniqKey="Khan K" first="Khalid M." last="Khan">Khalid M. Khan</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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