脂溶性查耳酮及其构象限制类似物的合成作为抗结核药物。
Syntheses of lipophilic chalcones and their conformationally restricted analogues as antitubercular agents.
机构信息
Chemical Sciences Division, Central Institute of Medicinal and Aromatic Plants, PO CIMAP, Kukrail Picnic Spot Road, Lucknow 226 015, India.
出版信息
Bioorg Med Chem Lett. 2013 Mar 1;23(5):1322-5. doi: 10.1016/j.bmcl.2012.12.096. Epub 2013 Jan 9.
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.
合成了亲脂性查耳酮及其构象受限类似物，并评估了它们对结核分枝杆菌 H37Rv 株的抗结核功效。发现化合物 16、24、25a 和 25c 的 MIC 活性分别为 60、30、3.5 和 7.5μg-mL(-1)。在非癌细胞人上皮肾细胞系（HEK-293）中，化合物 16、24、25a、25c 和 26 的体外细胞毒性显示，最活性化合物 25a 对结核细胞的选择性约为对健康细胞的 2.85 倍，而化合物 24 的选择性则为 16 倍。
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