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

Abstract

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 synthesised 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 No. 18, 19 have shown antitubercular activity of MIC 3.12 µg/ml and were non toxic against VERO, MBMDM cell lines and compounds 49, 50, 51 have shown antimalarial activity of MIC 1.0 µg/ml.