Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, 388120 Gujarat, India.
Eur J Med Chem. 2011 Sep;46(9):4192-200. doi: 10.1016/j.ejmech.2011.06.022. Epub 2011 Jun 23.
A new class of β-aryloxyquinolines 3a-i and their pyrano[3,2-c]chromene derivatives 6a-r incorporating a validated molecular target has been synthesized via a nucleophilic displacement and a one-pot multicomponent reaction respectively. In vitro antimicrobial activity of the synthesized compounds were investigated against a representative panel of pathogenic strains specifically Bacillus subtilis, Clostridium tetani, Streptococcus pneumoniae, Escherichia coli, Salmonella typhi, Vibrio cholera, Aspergillus fumigatus and Candida albicans. Compounds 3c, 3e, 3g, 6f, 6l and 6q exhibited excellent antibacterial activity while compound 6p exhibited more potent antifungal activity than that of first line standard drugs. In vitro antituberculosis activity was evaluated against Mycobacterium tuberculosis H37Rv and compound 6f is emerged as the promising antimicrobial member with better antitubercular activity. Majority of the compounds appears to be better antimicrobials but poor antituberculars.
通过亲核取代和一锅多组分反应，分别合成了一类新型的β-芳氧基喹啉 3a-i 和其吡喃并[3,2-c]色烯衍生物 6a-r，其中包含了一个经过验证的分子靶标。对合成化合物进行了体外抗菌活性测试，针对枯草芽孢杆菌、破伤风梭菌、肺炎链球菌、大肠杆菌、伤寒沙门氏菌、霍乱弧菌、烟曲霉和白色念珠菌等代表性病原菌株进行了测试。化合物 3c、3e、3g、6f、6l 和 6q 表现出优异的抗菌活性，而化合物 6p 表现出比一线标准药物更强的抗真菌活性。对结核分枝杆菌 H37Rv 进行了体外抗结核活性评估，化合物 6f 是一种具有良好抗结核活性的有前途的抗菌成员。大多数化合物似乎是更好的抗菌剂，但抗结核活性较差。
