Syntheses of lipophilic chalcones and their conformationally restricted analogues as antitubercular agents.
Lipophilic chalcones and their conformationally restricted analogues were synthesized and evaluated for their antitubercular efficacy against Mycobacterium tuberculosis H37Rv strain. Compounds 16, 24, 25a and 25c were found to be active MIC at 60, 30, 3.5 and 7.5 μg-mL(-1). In vitro cytotoxicity of compounds 16, 24, 25a, 25c and 26 in non-cancerous human epithelial kidney cell line (HEK-293) showed that most active compound 25a was approximately 2.85 times selective towards tubercular versus healthy cells whereas compound 24 was found to be 16 times selective.
Chemical Sciences Division, Central Institute of Medicinal and Aromatic Plants, PO CIMAP, Kukrail Picnic Spot Road, Lucknow 226 015, India.
Imran
I
Ahmad
Jay Prakash
JP
Thakur
Debabrata
D
Chanda
Dharmendra
D
Saikia
Feroz
F
Khan
Shivani
S
Dixit
Amit
A
Kumar
Rituraj
R
Konwar
Arvind Singh
AS
Negi
Atul
A
Gupta
D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D057809:HEK293 Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D013329:Structure-Activity Relationship
D000995:Antitubercular Agents; D047188:Chalcones