Novel inhibitors of bacterial two-component systems with gram positive antibacterial activity: Pharmacophore identification based on the screening hit closantel

被引:63
作者
Hlasta, DJ [1 ]
Demers, JP [1 ]
Foleno, BD [1 ]
Fraga-Spano, SA [1 ]
Guan, JH [1 ]
Hilliard, JJ [1 ]
Macielag, MJ [1 ]
Ohemeng, KA [1 ]
Sheppard, CM [1 ]
Sui, ZH [1 ]
Webb, GC [1 ]
Weidner-Wells, MA [1 ]
Werblood, H [1 ]
Barrett, JF [1 ]
机构
[1] RW Johnson Pharmaceut Res Inst, Raritan, NJ 08869 USA
关键词
D O I
10.1016/S0960-894X(98)00326-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This SAR study has shown that the salicylanilide is the pharmacophore for inhibition of the bacteria! two-component system. Hydrophobic substituents improve the potency of inhibitors in this series; however, hydrophobicity is not the sole determinant for inhibition; structural and electronic requirements also exist. Closantel (1) was found to inhibit a two-component system and to have antibacterial activity against drug resistant S. aureus and E. faecium, (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1923 / 1928
页数:6
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