Novel pyrazole–pyrazoline hybrids endowed with thioamide as antimalarial agents: their synthesis and 3D-QSAR studies. (August 2015)

• Record Type: Journal Article
• Authors: Marella, Akranth; Shaquiquzzaman, Mohammad; Akhter, Mymoona; Verma, Garima; Alam, Mohammad Mumtaz
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 30:Number 4(2015:Aug.)
• Page Start: 597
• Page End: 606
• Publication Date: 2015-08
• Subjects: Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2014.958081
• Languages: English
• ISSNs: 1475-6366

Abstract

<abstract> <title>Abstract</title> <p>One of the most viable options to tackle the growing resistance to the antimalarial drugs is hybrid molecules. It involves combination of different scaffolds in one frame that may lead to compounds with diverse biological profiles. In this context, new hybrids of three different scaffolds <italic>viz</italic> pyrazole, pyrazoline and thiosemicarbazone moiety were incorporated into one single compound and evaluated for their <italic>in vitro</italic> schizontocidal activity against the CQ-sensitive 3D7 strain of <italic>Plasmodium falciparum</italic>. Compounds with significant <italic>in vitro</italic> antimalarial activity were further evaluated for cytotoxicity against VERO cell lines. The best active compound <bold>48</bold> exhibited an IC₅₀ of 1.13 µM. The <italic>in vitro</italic> results were further validated by quantitative structure–activity relationship (QSAR).</p> </abstract>