A series of 5-(4-substituted piperazin-1-yl)quinolin-2(1H)-one derivatives (4a-4w) has been designed as chitin synthase inhibitors and antifungal agents. The designed compounds were obtained by an environmentally benign route in four steps starting from 5-amino-3,4-dihydroquinolin-2(1H)-one which was offered by an easily achieved synthetic method. The synthesized compounds were tested for their inhibition potency against chitin synthase. Compounds 4a and 4c exhibited excellent inhibitory activity with IC₅₀ values of 0.10 mM and 0.15 mM, respectively, which is better than that of Polyoxin B whose IC₅₀ value is 0.18 mM. Compounds 4h, 4i, 4j, 4k and 4n exerted moderate inhibition potency with IC₅₀ values of 0.38, 0.36, 0.47, 0.47 and 0.37 mM, respectively. These synthesized compounds were also evaluated for their in vitro antifungal activity against Candida albicans, Crytococcus neoformans, and Aspergillus flavus. Compounds 4a, 4i and 4j exhibited the most potent antifungal activity against C. albicans with MIC of 32 μg/mL, which were similar to that of Polyoxin B. The results of antibacterial activity against selected strains showed that the designed compounds have little potency against bacteria and indicated that these compounds were chitin synthase inhibitors and have selectively antifungal activity.

一系列5-（4-取代的哌嗪-1-基）喹啉-2（1 H）-一衍生物（4a-4w）被设计为几丁质合酶抑制剂和抗真菌剂。设计的化合物是通过环境友好的方法从5个氨基3,4-二氢喹啉2（1 H）-开始的四个步骤中获得的，该步骤可通过易于实现的合成方法获得。测试合成的化合物对几丁质合酶的抑制能力。化合物4a和4c表现出优异的抑制活性，其IC ₅₀值分别为0.10 mM和0.15 mM，这优于其IC ₅₀值为0.18 mM的多聚毒素B。化合物4h，4i，4j，4k和4n表现出中等抑制效力，IC ₅₀值分别为0.38、0.36、0.47、0.47和0.37 mM。这些合成的化合物还评估了其对白色念珠菌，新型隐球菌和黄曲霉的体外抗真菌活性。化合物4a，4i和4j对白念珠菌具有最强的抗真菌活性 MIC为32μg/ mL，与多聚毒素B相似。对所选菌株的抗菌活性结果表明，所设计的化合物对细菌的效力很小，表明这些化合物是几丁质合酶抑制剂，具有选择性的抗真菌活性。