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

Abstract：

:This SAR study has shown that the salicylanilide is the pharmacophore for inhibition of the bacterial 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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Hlasta DJ,Demers JP,Foleno BD,Fraga-Spano SA,Guan J,Hilliard JJ,Macielag MJ,Ohemeng KA,Sheppard CM,Sui Z,Webb GC,Weidner-Wells MA,Werblood H,Barrett JF

doi

10.1016/s0960-894x(98)00326-6

subject

Has Abstract

pub_date

1998-07-21 00:00:00

pages

1923-8

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960894X98003266

journal_volume

8

pub_type

杂志文章

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