Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 44, Issue 5, Pages 2081-2091Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.10.011
Keywords
Tuberculosis; Malaria; Chalcones; Pyrimidines
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Funding
- Indian Council of Medical Research (ICMR)
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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 H(37)Rv 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 mu g/mL and were nontoxic against VERO, MBMDM cell lines and compounds 54, 55, and 56 have shown antimalarial activity of MIC 1 mu g/mL. (C) 2008 Elsevier Masson SAS. All rights reserved.
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