当前位置： SCI文献检索 > INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS期刊下所有文献 > Identification and bioevaluation of SRI-12742 as an antimicrobial agent against multidrug-resistant Acinetobacter baumannii.

Identification and bioevaluation of SRI-12742 as an antimicrobial agent against multidrug-resistant Acinetobacter baumannii.

Abstract：

:Multidrug-resistant Acinetobacter baumannii (MDR-Ab) is one of the most significant nosocomial pathogens that is being increasingly isolated in healthcare settings worldwide. Owing to its inherent drug-resistant nature, coupled with its ability to readily acquire resistance to other antibiotic classes, there is a real dearth of antibiotics available to treat infections with MDR-Ab. A commercially available library was screened against MDR-Ab BAA-1605 to identify novel inhibitory molecules. The selectivity index of a hit was tested against Vero cells and in vitro efficacy was profiled against a panel of clinical MDR-Ab. The bacteriostatic or bactericidal nature was determined by time-kill experiments, and synergy with clinically approved drugs was determined by the chequerboard method. Additionally, in vivo efficacy was measured in a murine neutropenic A. baumannii thigh infection model. SRI-12742 was identified as a potent active hit, with a minimum inhibitory concentration (MIC) of 4 mg/L against BAA-1605. Its activity was then profiled against a MDR-Ab clinical strain panel (MICs 4 mg/L to >64 mg/L). SRI-12742 exhibited concentration-dependent bactericidal activity and caused an ca. 16 log10 CFU/mL reduction at 10 × MIC in 24 h, which is comparable with minocycline. In a murine neutropenic thigh infection model of A. baumannii infection, SRI-12742 reduced CFU counts by ca. 0.9 log10 CFU, which is comparable with polymyxin B. In addition, SRI-12742 synergised with all classes of antibiotics tested. SRI-12742 exhibits all of the criteria necessary to be positioned as a novel lead with potential to be deployed for the treatment of infections caused by MDR-Ab.

journal_name

Int J Antimicrob Agents

journal_title

International journal of antimicrobial agents

authors

Shukla M,Soni I,Matsuyama K,Tran T,Tanga M,Gong L,Chopra S

doi

10.1016/j.ijantimicag.2018.02.018

subject

Has Abstract

pub_date

2018-07-01 00:00:00

pages

22-27

issue

1

eissn

0924-8579

issn

1872-7913

pii

S0924-8579(18)30056-6

journal_volume

52

pub_type

杂志文章

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