KKL-40 是一种小分子抑制剂,专门针对反式转录过程,能够有效抑制甲氧西林敏感和耐药的金黄色葡萄球菌 (S. aureus),以及包括耐万古霉素的屎肠球菌、枯草芽孢杆菌和化脓性链球菌在内的其他革兰氏阳性病原体。KKL-40 与人类抗菌肽 LL-37 协同作用可抑制金黄色葡萄球菌,但与达托霉素、卡那霉素或红霉素等其他抗生素之间没有协同效应。反式转录是一种极端的重新编码形式,KKL-40 能抑制该过程,同时对 HeLa 细胞无毒。
CAY10711 is a substituted diamine that produces rapid bactericidal activity against both Gram-positive and Gram-negative bacteria, including methicillin-resistant S. aureus (MRSA) and stationary-phase bacteria. It displays MIC99 values of 2.9, 11.5, 2.9, and 2.9 μM against S. aureus RN4220, P. aeruginosa PAO1, E. coli ANS1, and MRSA 10082B, respectively. CAY10711 reduces biofilm formation and promotes biofilm dispersal in P. aeruginosa. It is synergistic with kanamycin and has limited adverse effects against mammalian cells or C. elegans development, survival, or reproduction.