Structural hybridization of three aminoglycoside antibiotics yields a potent broad-spectrum bactericide that eludes bacterial resistance enzymes

被引：13

作者：

Maianti, Juan Pablo ^{[1
]}

Hanessian, Stephen ^{[1
]}

机构：

[1] Univ Montreal, Dept Chem, CP 6128 Succ Ctr Ville, Montreal, PQ H3C 3J7, Canada

来源：

MEDCHEMCOMM | 2016年 / 7卷 / 01期

基金：

加拿大自然科学与工程研究理事会;

关键词：

16S RIBOSOMAL-RNA; CRYSTAL-STRUCTURE; A-SITE; ANTIBACTERIAL ACTIVITY; MECHANISMS; GENES; PAROMOMYCIN; INSIGHTS; STAPHYLOCOCCI; COMPLEXES;

D O I：

10.1039/c5md00429b

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Vast numbers of prevalent aminoglycoside-modifying enzymes undermine the clinical use of aminoglycoside antibiotics. We present the design and synthesis of a potent broad-spectrum bactericidal aminoglycoside based on available X-ray co-crystal structures within the ribosomal binding-site. The resulting antibiotic displays broad protection of its functional groups from inactivation by clinically relevant resistance enzymes.

引用

页码：170 / 176

页数：7

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