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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Discovery of novel purinylthiazolylethanone derivatives as anti-Candida albicans agents through possible multifaceted mechanisms
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Discovery of novel purinylthiazolylethanone derivatives as anti-Candida albicans agents through possible multifaceted mechanisms

机译：通过可能的多方面机制发现新型嘌呤硫代吡咯基甲酮衍生物作为抗念珠菌剂药物

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8An unprecedented amount of fungal and fungal-like infections has recently brought about some of the most severe die-offs and extinctions due to fungal drug resistance. Aimed to alleviate the situation, new effort was made to develop novel purinylthiazolylethanone derivatives, which were expected to combat the fungal drug resistance. Some prepared purinylthiazolylethanone derivatives possessed satisfactory inhibitory action towards the tested fungi, among which compound 8c gave a MIC value of 1 mg/mL against C. albicans. The active molecule 8c was able to kill C. albicans with undetectable resistance as well as low hematotoxicity and cytotoxicity. Furthermore, it could hinder the growth of C. albicans biofilm, thus avoiding the occurrence of drug resistance. Mechanism research manifested that purinylthiazolylethanone derivative 8c led to damage of cell wall and membrane disruption, so protein leakage and the cytoplasmic membrane depolarization were observed. On this account, the activity of fungal lactate dehydrogenase was reduced and metabolism was impeded. Meanwhile, the increased levels of reactive oxygen species (ROS) and reactive nitrogen species (RNS) disordered redox equilibrium, giving rise to oxidative damage to fungal cells and fungicidal effect. (C) 2021 Elsevier Masson SAS. All rights reserved.
机译：8由于真菌耐药性，真菌和真菌样感染数量空前，最近导致了一些最严重的死亡和灭绝。为了缓解这种情况，人们做出了新的努力来开发新的嘌呤基噻唑烷酮衍生物，有望对抗真菌耐药性。一些制备的嘌呤基噻唑烷酮衍生物对受试真菌具有满意的抑制作用，其中化合物8c对白色念珠菌的MIC值为1 mg/mL。活性分子8c能够杀死耐药性无法检测到的白色念珠菌，并且血液毒性和细胞毒性较低。此外，它可以阻碍白色念珠菌生物膜的生长，从而避免耐药性的发生。机理研究表明，嘌呤基噻唑烷酮衍生物8c导致细胞壁损伤和细胞膜破坏，从而观察到蛋白渗漏和细胞膜去极化。因此，真菌乳酸脱氢酶活性降低，代谢受阻。同时，活性氧（ROS）和活性氮（RNS）水平的增加扰乱了氧化还原平衡，导致真菌细胞的氧化损伤和杀菌效果。（c）2021爱思唯尔马松SAS。版权所有。

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