ACS Medicinal Chemistry Letters p. 233 - 237 (2018)
Update date:2022-08-03
Topics:
Ni, Shuaishuai
Li, Baoli
Chen, Feifei
Wei, Hanwen
Mao, Fei
Liu, Yifu
Xu, Yixiang
Qiu, Xiaoxi
Li, Xiaokang
Liu, Wenwen
Hu, Linghao
Ling, Dazheng
Wang, Manjiong
Zheng, Xinyu
Zhu, Jin
Lan, Lefu
Li, Jian
Diapophytoene desaturase (CrtN) is a potential novel target for intervening in the biosynthesis of the virulence factor staphyloxanthin. In this study, 38 1,4-benzodioxan-derived CrtN inhibitors were designed and synthesized to overwhelm the defects of leading compound 4a. Derivative 47 displayed superior pigment inhibitory activity, better hERG inhibitory properties and water solubility, and significantly sensitized MRSA strains to immune clearance in vitro. Notably, 47 displayed excellent efficacy against pigmented S. aureus Newman, Mu50 (vancomycin-intermediate MRSA, VISA), and NRS271 (linezolid-resistant MRSA, LRSA) comparable to that of linezolid and vancomycin in vivo.
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