Title:
NON-BETA LACTAM ANTIBIOTICS
Document Type and Number:
WIPO Patent Application WO/2016/049586
Kind Code:
A3
Abstract:
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-oxadiazole (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.
Inventors:
CHANG MAYLAND (US)
MOBASHERY SHAHRIAR (US)
SPINK EDWARD (GB)
DING DERONG (US)
TESTERO SEBASTIAN (AR)
LEEMANS ERIKA (BE)
BOUDREAU MARC A (US)
MOBASHERY SHAHRIAR (US)
SPINK EDWARD (GB)
DING DERONG (US)
TESTERO SEBASTIAN (AR)
LEEMANS ERIKA (BE)
BOUDREAU MARC A (US)
Application Number:
PCT/US2015/052474
Publication Date:
May 26, 2016
Filing Date:
September 25, 2015
Export Citation:
Assignee:
UNIV NOTRE DAME DU LAC (US)
International Classes:
C07D413/04
Foreign References:
| US20140200226A1 | 2014-07-17 | |||
| US20110086797A1 | 2011-04-14 | |||
| US20050004005A1 | 2005-01-06 | |||
| US6277872B1 | 2001-08-21 | |||
| US5179111A | 1993-01-12 |
Other References:
See also references of EP 3197888A4
Attorney, Agent or Firm:
HAUKAAS, Michael H. (5100 Eden Ave. Suite 30, Edina Minnesota, US)
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