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Tetracyclic indolines as a novel class of β-lactam-selective resistance-modifying agent for MRSA.

Abstract：

:Antibiotic-resistant bacterial infections have seen a marked increase in recent years, while antibiotic discovery has waned. Resistance-modifying agents (RMA) offer an intriguing alternative strategy to fight against resistant bacteria. Here we report the discovery, antibiotic profiling, and structure-activity relationships of a novel class of RMAs, tetracyclic indolines. These selectively potentiate β-lactam antibiotics in methicillin-resistant Staphylococcus aureus (MRSA) without antibacterial or β-lactamase inhibitory activity on their own. The most potent analogue, 6a, showed strong potentiation of amoxicillin/clavulanic acid in a variety of hospital-acquired and community-acquired MRSA strains with low mammalian toxicity. These compounds may be further developed to extend the clinic life span of β-lactam antibiotics.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Zhu Y,Cleaver L,Wang W,Podoll JD,Walls S,Jolly A,Wang X

doi

10.1016/j.ejmech.2016.09.034

subject

Has Abstract

pub_date

2017-01-05 00:00:00

pages

130-142

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30764-4

journal_volume

125

pub_type

杂志文章

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