首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and identification of beta-aryloxyquinolines and their pyrano(3,2-c)chromene derivatives as a new class of antimicrobial and antituberculosis agents.
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Synthesis and identification of beta-aryloxyquinolines and their pyrano(3,2-c)chromene derivatives as a new class of antimicrobial and antituberculosis agents.

机译:β-芳氧基喹啉及其吡喃(3,2-c)苯二甲基衍生物作为一类新型的抗微生物剂和抗结核剂的合成与鉴定。

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摘要

A new class of beta-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.
机译:分别通过亲核置换和一锅多组分反应合成了新型的β-芳氧基喹啉3a-i及其吡喃并[3,2-c]色烯衍生物6a-r,其中包含经过验证的分子靶标。研究了合成的化合物对代表性菌株的致病菌株的体外抗菌活性,所述菌株包括枯草芽孢杆菌,破伤风梭菌,肺炎链球菌,大肠杆菌,鼠伤寒沙门氏菌,霍乱弧菌,烟曲霉和白色念珠菌。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。评估了针对结核分枝杆菌H37Rv的体外抗结核活性,化合物6f成为具有更好抗结核活性的有希望的抗微生物成员。该化合物的大多数似乎是更好的抗菌剂,但抗结核药较差。

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