Substituted quinolinyl chalcones and quinolinyl pyrimidines as a new class of anti-infective agents

Frequency of tuberculosis and malaria is progressively increasing worldwide. New emerging strain of bacterium and resistance to currently available drugs make this field more conscientious and alarming. In this connection a series of substituted quinolinyl chalcones and substituted quinolinyl pyrimidines were synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37RV and antimalarial activity against NF-54 strain of Plasmodium falciparum. A comparison of structure–activity relationship reveals that different physicochemical and structural requirements exist for these two activities. Out of synthesized compounds, compound nos. 22 and 23 have shown antitubercular activity of MIC 3.12 μg/mL and were nontoxic against VERO, MBMDM cell lines and compounds 54, 55, and 56 have shown antimalarial activity of MIC 1 μg/mL.

Graphical abstractA series of substituted quinolinyl chalcones and pyrimidines have been synthesized and evaluated for antitubercular and antimalarial activity. Among all, two compounds have shown antitubercular activity of MIC 3.12 μg/mL and three compounds have shown antimalarial activity of MIC 1.0 μg/mL.Figure optionsDownload full-size imageDownload as PowerPoint slide