Synthesis and In vitro Analysis of Novel Dihydroxyacetophenone Derivatives with Antimicrobial and Antitumor Activities
作者:Ana Zbancioc、Anca Miron、Cristina Tuchilus、Pincu Rotinberg、Cosmin Mihai、Ionel Mangalagiu、Gheorghita Zbancioc
DOI:10.2174/15734064113096660070
日期:2014.5.31
Herein we report a feasible study concerning the design, syntheses and in vitro antimicrobial and antitumoral
activities of some novel compounds with dihydroxyacetophenone (DA) moiety. An efficient and general method for the
preparation of diazine with dihydroxyacetophenone (DDA) skeleton under conventional thermal heating (TH), microwave
(MW) and ultrasounds (US) irradiation is presented. Antimicrobial and antitumoral tests prove that some dihydroxyacetophenone
compounds (the brominated derivatives BrDA 3) have a significant biological activity. It is also to be pointed out
that, basically all the dihydroxyacetophenone derivatives proved to have a powerful antibacterial activity against drug resistant
Gram-negative strain Pseudomonas aeruginosa ATCC 27853. Of particular interest could be the excellent antibacterial
activity of our dihydroxyacetophenone compounds against drug resistant Gram-negative strain Pseudomonas aeruginosa.
在此,我们报告了一项关于一些具有二羟基苯乙酮(DA)分子的新型化合物的设计、合成、体外抗菌和抗肿瘤活性的可行性研究。本文介绍了一种在传统热加热(TH)、微波(MW)和超声(US)辐照下制备具有二羟基苯乙酮(DDA)骨架的重氮的高效通用方法。抗菌和抗肿瘤试验证明,某些二羟基苯乙酮化合物(溴化衍生物 BrDA 3)具有显著的生物活性。还需要指出的是,基本上所有的二羟基苯乙酮衍生物都被证明对耐药性革兰氏阴性菌株铜绿假单胞菌 ATCC 27853 具有强大的抗菌活性。特别值得关注的是,我们的二羟基苯乙酮化合物对耐药革兰氏阴性假单胞菌具有极佳的抗菌活性。