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Rational design of phenothiazinium derivatives and photoantimicrobial drug discovery

机译:吩噻嗪鎓衍生物的合理设计和光抗菌药物的发现

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While the model for conventional antimicrobial drug discovery is based securely on singular modes and sites of action, those associated with phenothiazinium photoantimicrobial candidates are both multi factorial and variable, resulting from oxidation events due to reactive oxygen species (ROS). The effective counteraction of such species and their variable targets is clearly problematic from the point of view of microbial resistance mechanism development, and offers considerable opportunity for the use of these agents in local infection control. However, this also means that drug development cannot be carried out using similar methods to those employed for conventional agents. Furthermore, these multifactorial photoantimicrobial agents are truly broad-spectrum since they are active against bacteria, fungi, viruses and protozoa, again at variance with the targeting of conventional, single-class antimicrobials.
机译:虽然常规抗微生物药物发现的模型安全地基于单一的作用方式和作用部位,但与吩噻嗪鎓类光抗微生物候选物相关的那些作用既是多因素的又是可变的,这是由于活性氧(ROS)引起的氧化作用所致。从微生物抗性机制发展的角度来看,此类物种及其可变目标的有效对抗显然是有问题的,并且为在局部感染控制中使用这些药物提供了相当大的机会。但是,这也意味着不能使用与常规试剂相似的方法进行药物开发。此外,这些多因素光抗微生物剂真正具有广谱性,因为它们具有抗细菌,真菌,病毒和原生动物的活性,而且与传统的单类抗微生物剂的目标不同。

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