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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 multifactorial 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. This review concentrates on the use of the phenothiazinium class as exemplar photoantimicrobials, due to their pre-eminence in the field and considers the various criteria required for successful activity against microbes. These include alicyclic fusion, chalcogen substitution, benzo[a] fusion and the heavy atom effect, to decrease aggregation, improve ROS production and extend absorption wavelength, as well as conventional approaches, such as increasing cationic character to improve microbial selectivity/targeting. © 2016 Elsevier Ltd
机译：尽管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位点，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）引起的氧化事件所致。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所用方法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。由于其在本领域的杰出地位，本综述着重将吩噻嗪鎓类用作示例性光抗菌剂，并考虑了成功开展抗微生物活动所需的各种标准。这些方法包括脂环式融合，硫族元素取代，苯并[a]融合和重原子效应，以减少聚集，提高ROS的产生并延长吸收波长，以及常规方法，例如增加阳离子特性以改善微生物的选择性/靶向性。 ©2016爱思唯尔有限公司

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    Wainwright, M; McLean, A;

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