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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 14期

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

页码：1923 / 1928

页数：6

共 15 条

[1] SELECTIVE REDUCTION OF AROMATIC NITRO-COMPOUNDS WITH STANNOUS CHLORIDE IN NON-ACIDIC AND NON-AQUEOUS MEDIUM [J].