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 H(37)R(V) 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 microg/mL and were nontoxic against VERO, MBMDM cell lines and compounds 54, 55, and 56 have shown antimalarial activity of MIC 1 microg/mL.
Sharma
Moni
M
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
Chaturvedi
Vinita
V
Manju
Y K
YK
Bhatnagar
Shalini
S
Srivastava
Kumkum
K
Puri
S K
SK
Chauhan
Prem M S
PM
D000818:Animals; D000890:Anti-Infective Agents / Q000737:chemistry*; D047188:Chalcones / Q000737:chemistry* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology; D011804:Quinolines / Q000737:chemistry; D013329:Structure-Activity Relationship
D000890:Anti-Infective Agents; D047188:Chalcones; D011743:Pyrimidines; D011804:Quinolines