Design, Synthesis, and<i>in vitro</i>Antimicrobial Activity of New Furan/Thiophene-1,3-Benzothiazin-4-one Hybrids
作者:Łukasz Popiołek、Anna Biernasiuk、Anna Malm
DOI:10.1002/jhet.2429
日期:2016.3
This study presents the design, synthesis, spectral analysis, and in vitro antimicrobial evaluation of a new series of furan/thiophene‐1,3‐benzothiazin‐4‐one hybrids (17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32). New compounds were obtained by cyclization reaction of N‐substituted furan/thiophene‐2‐carboxamide derivatives (1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16) with
本研究提出的设计,合成,频谱分析,并在一个新的系列的体外抗微生物评价呋喃/噻吩-1,3-苯并噻嗪-4-酮杂种(17,18,19,20,21,22,23,24,25,26,27,28,29,30,31,32)。由N-取代的呋喃/ -噻吩-2-羧酰胺衍生物的环化反应(得到新化合物1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16)与硫代水杨酸。使用肉汤微稀释法筛选所有合成的化合物的体外抗菌活性。九种合成化合物对革兰氏阳性菌,革兰氏阴性菌和属于假丝酵母的酵母表现出良好的活性。(MIC = 7.81–500μg/ mL),尤其是针对葡萄球菌。(MIC = 15.62–62.5μg/ ml),芽孢杆菌属。(MIC = 7.81–62.5μg/ mL),支气管博德特氏菌ATCC 4617(MIC = 62.5–125μg/ mL)和对念珠菌的抑菌活性。(MIC = 62.5–125μg/