Literature DB >> 25137478

Small-molecule suppression of β-lactam resistance in multidrug-resistant gram-negative pathogens.

Christopher M Brackett1, Roberta J Melander, Il Hwan An, Aparna Krishnamurthy, Richele J Thompson, John Cavanagh, Christian Melander.   

Abstract

Recent efforts toward combating antibiotic resistance in bacteria have focused on Gram-positive bacteria; however, multidrug-resistant Gram-negative bacteria pose a significant risk to public health. An orthogonal approach to the development of new antibiotics is to develop adjuvant compounds that enhance the susceptibility of drug-resistant strains of bacteria to currently approved antibiotics. This paper describes the synthesis and biological activity of a library of aryl amide 2-aminoimidazoles based on a lead structure from an initial screen. A small molecule was identified from this library that is capable of lowering the minimum inhibitory concentration of β-lactam antibiotics by up to 64-fold.

Entities:  

Mesh:

Substances:

Year:  2014        PMID: 25137478     DOI: 10.1021/jm501050e

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  14 in total

1.  Using Small-Molecule Adjuvants to Repurpose Azithromycin for Use against Pseudomonas aeruginosa.

Authors:  Veronica B Hubble; Brittany A Hubbard; Bradley M Minrovic; Roberta J Melander; Christian Melander
Journal:  ACS Infect Dis       Date:  2018-11-29       Impact factor: 5.084

2.  Structure of the Francisella response regulator QseB receiver domain, and characterization of QseB inhibition by antibiofilm 2-aminoimidazole-based compounds.

Authors:  Morgan E Milton; C Leigh Allen; Erik A Feldmann; Benjamin G Bobay; David K Jung; Matthew D Stephens; Roberta J Melander; Kelly E Theisen; Daina Zeng; Richele J Thompson; Christian Melander; John Cavanagh
Journal:  Mol Microbiol       Date:  2017-08-16       Impact factor: 3.501

3.  Marine sponge alkaloids as a source of anti-bacterial adjuvants.

Authors:  Roberta J Melander; Hong-Bing Liu; Matthew D Stephens; Carole A Bewley; Christian Melander
Journal:  Bioorg Med Chem Lett       Date:  2016-11-09       Impact factor: 2.823

4.  Property-Guided Synthesis of Aza-Tricyclic Indolines: Development of Gold Catalysis En Route.

Authors:  Patrick M Barbour; Wei Wang; Le Chang; Kasey L Pickard; Rana Rais; Barbara S Slusher; Xiang Wang
Journal:  Adv Synth Catal       Date:  2016-03-03       Impact factor: 5.837

5.  Potentiation of Francisella Resistance to Conventional Antibiotics through Small Molecule Adjuvants.

Authors:  Matthew D Stephens; Veroncia B Hubble; Robert K Ernst; Monique L van Hoek; Roberta J Melander; John Cavanagh; Christian Melander
Journal:  Medchemcomm       Date:  2015-09-30       Impact factor: 3.597

6.  Analogue synthesis reveals decoupling of antibiofilm and β-lactam potentiation activities of a lead 2-aminoimidazole adjuvant against Mycobacterium smegmatis.

Authors:  Sara E Martin; Catherine M Nguyen; Randall J Basaraba; Christian Melander
Journal:  Chem Biol Drug Des       Date:  2018-05-12       Impact factor: 2.817

7.  Anti-biofilm activity of quinazoline derivatives against Mycobacterium smegmatis.

Authors:  Karlie E Cox; Christian Melander
Journal:  Medchemcomm       Date:  2019-05-23       Impact factor: 3.597

8.  Small Molecule Potentiation of Gram-Positive Selective Antibiotics against Acinetobacter baumannii.

Authors:  Sara E Martin; Roberta J Melander; Christopher M Brackett; Alison J Scott; Courtney E Chandler; Catherine M Nguyen; Bradley M Minrovic; Sarah E Harrill; Robert K Ernst; Colin Manoil; Christian Melander
Journal:  ACS Infect Dis       Date:  2019-04-26       Impact factor: 5.084

9.  Second Generation Modifiers of Colistin Resistance Show Enhanced Activity and Lower Inherent Toxicity.

Authors:  Christopher M Brackett; Robert E Furlani; Ryan G Anderson; Aparna Krishnamurthy; Roberta J Melander; Samuel M Moskowitz; Robert K Ernst; Christian Melander
Journal:  Tetrahedron       Date:  2016-06-23       Impact factor: 2.457

10.  Augmenting the Activity of Macrolide Adjuvants against Acinetobacter baumannii.

Authors:  Veronica B Hubble; Kyle R Bartholomew; Alexander W Weig; Sara M Brackett; Samantha L Barlock; Anne E Mattingly; Ansley M Nemeth; Roberta J Melander; Christian Melander
Journal:  ACS Med Chem Lett       Date:  2020-08-12       Impact factor: 4.345

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.