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Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Facile synthesis of antimalarial 1,2-disubstituted 4-quinolones from 1,3-bisaryl-monothio-1,3-diketones
Ajjampura C Vinayaka1, Maralinganadoddi P Sadashiva, Xianzhu Wu
1Department of Studies in Chemistry, University of Mysore, Manasagangothri, Mysore 570006, India. mpsadashiva@gmail.com rangappaks@yahoo.com.
Abstract:
A new strategy was developed to synthesize 1,2-disubstituted 4-quinolones in good yield starting from 1,3-bisaryl-monothio-1,3-diketone substrates. The synthesized compounds were evaluated for antimalarial activity using Plasmodium falciparum strains. All compounds, except for two, showed good activity. Of these, seven compounds exhibited an excellent antimalarial activity (IC50, <2 μM). More importantly, all seven compounds were equally effective in inhibiting the growth of both chloroquine-sensitive and chloroquine-resistant strains. The cytotoxicity assessment using carcinoma and non-carcinoma human cell lines revealed that almost all synthesized compounds were minimally cytotoxic (IC50, >50 μM).
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