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Non-beta lactam antibiotics

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posted on 2022-01-16, 00:00 authored by Derong Ding, Edward Spink, Erika Leemans, Marc Boudreau, Mayland ChangMayland Chang, Sebastian Testero, Shahriar MobasheryShahriar Mobashery
The invention provides a newly discovered oxadiazole class of antibiotics. The oxadiazoles impair cell-wall biosynthesis and exhibit activities against the Gram-positive bacteria such as the bacterium Staphylococcus aureus, including methicillin-resistant S. aureus (MRSA) and vancomycin-resistant and linezolid-resistant S. aureus. For example, 5-(1H-indol-5-yl)-3-(4-(4-(trifluoromethyl)phenoxy)phenyl)-1,2,4-oxadiazo- le (antibiotic 75b) was efficacious in a mouse model of MRSA infection, exhibiting a long half-life, a high volume of distribution, and low clearance. Antibiotic 75b antibiotic is bactericidal and is orally bioavailable. This class of antibiotics can be used as a therapeutic agent against infections by Gram-positive bacteria such as MRSA.

History

Patent Number

US 10662164 B2

Other Application

15/513,892

Inventor

Mayland Chang Shahriar Mobashery Edward Spink Derong Ding Sebastian Testero Erika Leemans Marc Boudreau

Inventor from Local Institution

Mayland Chang Shahriar Mobashery Edward Spink Derong Ding Sebastian Testero Erika Leemans Marc Boudreau

Assignee

University of Notre Dame du Lac

Date Modified

2022-02-04

Language

  • English

Claims

9

Prior Publication Number

US 2019/0127340 A1

Cooperative Patent Classification Codes

C07D 271/06 (20130101); C07D 271/107 (20130101); C07F 9/65318 (20130101); C07D 413/04 (20130101); A61P 31/04 (20180101); C07D 471/04 (20130101)

Contributor

Mayland Chang|Shahriar Mobashery|Edward Spink|Derong Ding|Sebastian Testero|Erika Leemans|Marc Boudreau

International Patent Classification Codes

A61K 31/4245 (20060101); C07D 271/107 (20060101); C07D 271/06 (20060101); C07D 471/04 (20060101); C07D 413/04 (20060101); C07F 9/653 (20060101)

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