pyocyanin

Hexyl gallate (Gallic acid hexyl ester) 是没食子酸的烷基酯衍生物，对恶性疟原虫具有很强的抗疟活性，IC50为 0.11 mM。它具有抗菌活性，通过抑制 RhlR 抑制鼠李糖脂和绿脓杆菌素的产生。

4-(tert-Butyl)-benzhydroxamic Acid is a PqsR antagonist with IC50s of 12.5 μM and 23.6 μM for E. coli and P. aeruginosa, respectively, and it reduces the production of the virulence factor pyocyanin in P. aeruginosa with an IC50 of 87.2 μM[1].

Hemipyocyanine (528-71-2) 是一种 α-淀粉酶抑制剂。

2-heptyl-3-hydroxy-4(1H)-Quinolone (Pseudomonas Quinolone Signal) 是一种铜绿假单胞菌为应对细胞密度增加而产生的一种法定人数感应信号分子。 它增加了铜绿假单胞菌中lasB 基因的表达，增加代谢物焦蓝蛋白和凝集素PA-IL 的分泌，以及增加铜绿假单胞菌种群的生物膜生产。当使用浓度为40 μM 时，它还会降低铜绿假单胞菌生长介质中的铁含量，并在硫酸铁溶液中充当一种铁螯合剂。

LasR-IN-4 是 LasR 的有效抑制剂，可抑制铜绿假单胞菌及其生物膜的形成、绿脓素和鼠李糖脂的产生。

Aeruginoic acid 是一种绿脓杆菌素生物合成的副产物并充当铁螯合剂，且具备降血压的药理活性。

PqsR-IN-2 (Compound 19) is a highly potent inhibitor of PqsR, the transcriptional regulator responsible for quorum sensing in Pseudomonas aeruginosa. It effectively suppresses pyocyanin production without causing significant cytotoxicity, making it a promising compound for therapeutic applications [1].

N-Decanoyl cyclopentylamide (C10-CPA) 在铜绿假单胞菌中作为群体感应系统las和rhl的强效抑制剂，有效干扰这些系统调控的毒力因子表达。此外，N-Decanoyl cyclopentylamide 可抑制铜绿假单胞菌的一系列关键病原因子，包括弹性蛋白酶、绿脓素和鼠李糖脂，同时阻止生物膜的形成。

RhlR antagonist 1 is a highly effective antagonist of the RhlR protein, showing an IC50 value of 26 μM. It exhibits selective antagonistic activity against RhlR, with minimal effect on LasR and PqsR. RhlR antagonist 1 strongly inhibits biofilm formation in both static and dynamic environments and reduces the production of virulence factors, such as rhamnolipid and pyocyanin, in P. aeruginosa. These characteristics make RhlR antagonist 1 a valuable tool for the development of molecules that modulate quorum sensing and control P. aeruginosa infections [1].

F-17 is a promising virulence factor inhibitor, displaying substantial inhibitory effects on biofilm formation, elastase activity, pyocyanin production, and swarming motility. Additionally, F-17 exhibits a strong binding affinity towards LasR and PqsR. Notably, F-17 does not exhibit any discernible cytotoxicity [1].

PqsR-IN-1 (Compound 18) is a potent inhibitor of PqsR, which is a transcriptional regulator involved in the quorum sensing mechanism of Pseudomonas aeruginosa. This compound effectively reduces the production of pyocyanin and exhibits minimal cytotoxicity [1].

Quorum sensing-IN-6 (compound 27) 作为一种群体感应 (QS) 抑制剂,展示出对E.coli和Pyocyanin的显著抑制效果,其IC50值分别为8 nM和106 nM.

Quorum sensing-IN-9 (Compound 7d) 通过结合 PqsR 蛋白在 Pseudomonas aeruginosa 中阻断群体感应机制。它抑制 lasB、rhlA 和 pqsA 等群体感应相关基因的表达，从而阻止毒力因子如弹性蛋白酶 (elastase)、绿脓素 (pyocyanin) 和鼠李糖脂 (rhamnolipid) 的合成。该化合物削弱 P. aeruginosa 的运动能力，抑制生物膜的形成，降低其毒力及致病性。在大蜡螟 (Galleria mellonella) 幼虫模型中，Quorum sensing-IN-9 展现出抗感染活性。

Antibacterial synergist 1 (compound 20P) is a potent inhibitor of bacterial biofilm formation. It effectively suppresses the production of pyocyanin, with an IC 50 of 8.6 μM, and inhibits biofilm formation with an IC 50 of 4.5 μM. Antibacterial synergist 1 shows promise in the research of P. aeruginosa infections [1].