Medicinal Chemistry Division, CSIR-North East Institute of Science and Technology, Jorhat 785006, India.
Steroids. 2012 Nov;77(13):1438-45. doi: 10.1016/j.steroids.2012.08.008. Epub 2012 Sep 1.
The preparation of A-ring and D-ring fused steroidal quinolines is described from one-pot reaction of steroidal β-bromovinylaldehydes and arylamines in solvent-free and catalyst-free condition under microwave irradiation. The antimicrobial activities of the compounds were tested by agar diffusion assay and broth macro dilution method. Compounds 7a, 7e and 7g-h showed promising in vitro activity when tested against fungal pathogen Aspergillus niger whereas compounds 7e-h and 7j showed promising activity when tested against fungal pathogen Candida albicans. Compounds 7c and 7f showed potent inhibition against the growth of Gram negative bacteria Pseudomonas aeruginosa and compounds 7e, 7g-h and 7j inhibited the growth of tested Gram positive bacteria Bacillus subtilis and Staphylococcus aureus.
描述了一种从甾体β-溴乙烯醛和芳胺在无溶剂和无催化剂条件下一锅反应，在微波辐射下制备 A 环和 D 环稠合甾体喹啉的方法。采用琼脂扩散法和肉汤宏观稀释法对化合物的抗菌活性进行了测试。化合物 7a、7e 和 7g-h 对真菌病原体黑曲霉表现出良好的体外活性，而化合物 7e-h 和 7j 对真菌病原体白色念珠菌表现出良好的活性。化合物 7c 和 7f 对革兰氏阴性菌铜绿假单胞菌的生长有很强的抑制作用，化合物 7e、7g-h 和 7j 抑制了革兰氏阳性菌枯草芽孢杆菌和金黄色葡萄球菌的生长。
