Quinoline-pyrimidine hybrids: synthesis, antiplasmodial activity, SAR, and mode of action studies

Journal of Medicinal Chemistry
Kamaljit SinghJan Balzarini

Abstract

For the treatment of malaria which affects nearly 200 million people each year and the continued exacerbation by the emergence of drug resistance to most of the available antimalarials, the "covalent bitherapy" suggests hybrid molecules to be the next-generation antimalarial drugs. In this investigation, new hybrids of 4-aminoquinoline and pyrimidine moieties that show antiplasmodial activity in the nM range against chloroquine-resistant as well as chloroquine-sensitive strains of Plasmodium falciparum have been prepared. Cytotoxicity evaluation and mode of action of most potent hybrid molecule have been conducted.

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Citations

Dec 8, 2015·Journal of Medicinal Chemistry·Bogdan A ŠolajaDonatella Taramelli
May 27, 2015·Journal of Agricultural and Food Chemistry·Da-Wei WangGuang-Fu Yang
Jun 27, 2015·European Journal of Medicinal Chemistry·Hardeep KaurKamaljit Singh
Jul 6, 2015·European Journal of Medicinal Chemistry·Hardeep KaurKamaljit Singh
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