Synthesis, biological evaluation and docking studies of 4-aryloxymethyl coumarins derived from substructures and degradation products of vancomycin.

Synthesis, biological evaluation and docking studies of 4-aryloxymethyl coumarins derived from substructures and degradation products of vancomycin.
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DOI:
10.1016/j.ejmech.2013.10.047
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发表时间:
2013-12
影响因子:
6.7
通讯作者:
H. M. Revankar;M. Kulkarni;S. Joshi;U. A. More
H. M. Revankar;M. Kulkarni;S. Joshi;U. A. More
中科院分区:
医学1区
文献类型:
--
作者:
H. M. Revankar;M. Kulkarni;S. Joshi;U. A. More

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以没食子酸乙酯和N-苯甲酰酪氨酸乙酯为原料,合成了两个系列的4-芳氧甲基香豆素。没食子酸酯3a-3g和酪氨酸衍生物4 e-4j对粪肠球菌的抑制作用最强。它们也被发现对尼日尔曲霉和白色念珠菌有效。与新生霉素的比较对接研究表明比新生霉素更好的结合能力和更高的“C”评分值。
Two series of 4-aryloxymethyl coumarins derived from the reaction of 4-bromomethyl coumarins with ethyl gallate and ethyl ester of N-Benzoyl tyrosine have been synthesized. Gallate ethers3a–3gand tyrosine derivatives4e–4jwere most effective againstEntercoccus faecalis. They were also found to be effective against Aspergillus niger and Candida albicans. Comparative docking studies with novobiocin have indicated better binding ability and higher ‘C’ score values than novobiocin.