Design, synthesis, antimicrobial, anticancer evaluation, and QSAR studies of 4-(substituted benzylidene-amino)-1,5-dimethyl-2-phenyl-1,2-dihydropyrazol-3-ones

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作者
Sumit Sigroha
Balasubramanian Narasimhan
Pradeep Kumar
Anurag Khatkar
Kalavathy Ramasamy
Vasudevan Mani
Rakesh Kumar Mishra
Abu Bakar Abdul Majeed
机构
[1] Maharshi Dayanand University,Faculty of Pharmaceutical Sciences
[2] Universiti Teknologi MARA (UiTM),Collaborative Drug Discovery Research Group, Faculty of Pharmacy, Campus Puncak Alam
[3] Universiti Teknologi MARA (UiTM),Brain Research Laboratory, Faculty of Pharmacy, Campus Puncak Alam
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4-Aminoantipyrine derivatives; Antimicrobial; Anticancer; QSAR;
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摘要
A series of 4-(substituted benzylidene-amino)-1,5-dimethyl-2-phenyl-1,2-dihydropyrazol-3-ones (1–17) was synthesized and tested in vitro for its antimicrobial and anticancer potentials. The biological screening results indicated that compounds having m-chloro substituent on benzaldehyde portion showed antimicrobial potential, whereas compounds having chloro, methoxy, and hydroxyl groups showed anticancer potential. The quantitative structure activity relationship (QSAR) studies indicated the importance of topological parameter, valence first order molecular connectivity index in describing antifungal activity. The developed QSAR models, however, were statistically insignificant with reference to anticancer activity of the synthesized compounds.
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页码:3863 / 3875
页数:12
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