Discovery of a New Class of Non-β-lactam Inhibitors of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity | Zendy

Peter I. O’Daniel | Zendy; Zhihong Peng | Zendy; Hualiang Pi | Zendy; Sebastián A. Testero | Zendy; Derong Ding | Zendy; Edward Spink | Zendy; Erika Leemans | Zendy; Marc A. Boudreau | Zendy; Takao Yamaguchi | Zendy; Valerie A. Schroeder | Zendy; William R. Wolter | Zendy; Leticia I. Llarrull | Zendy; Wei Song | Zendy; Elena Lastochkin | Zendy; Malika Kumarasiri | Zendy; Nuno T. Antunes | Zendy; Mana Espahbodi | Zendy; Katerina Lichtenwalter | Zendy; Mark A. Suckow | Zendy; Sergei B. Vakulenko | Zendy; Shahriar Mobashery | Zendy; Mayland Chang | Zendy

Open Access

Discovery of a New Class of Non-β-lactam Inhibitors of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity

Author(s) -

Peter I. O’Daniel,

Zhihong Peng,

Hualiang Pi,

Sebastián A. Testero,

Derong Ding,

Edward Spink,

Erika Leemans,

Marc A. Boudreau,

Takao Yamaguchi,

Valerie A. Schroeder,

William R. Wolter,

Leticia I. Llarrull,

Wei Song,

Elena Lastochkin,

Malika Kumarasiri,

Nuno T. Antunes,

Mana Espahbodi,

Katerina Lichtenwalter,

Mark A. Suckow,

Sergei B. Vakulenko,

Shahriar Mobashery,

Mayland Chang

Publication year - 2014

Publication title -

journal of the american chemical society

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 7.115

H-Index - 612

eISSN - 1520-5126

pISSN - 0002-7863

DOI - 10.1021/ja500053x

Subject(s) - linezolid , penicillin binding proteins , penicillin , staphylococcus aureus , antibiotics , chemistry , microbiology and biotechnology , in vivo , vancomycin , lactam , antibacterial activity , bacteria , biology , biochemistry , stereochemistry , genetics

Infections caused by hard-to-treat methicillin-resistant Staphylococcus aureus (MRSA) are a serious global public-health concern, as MRSA has become broadly resistant to many classes of antibiotics. We disclose herein the discovery of a new class of non-β-lactam antibiotics, the oxadiazoles, which inhibit penicillin-binding protein 2a (PBP2a) of MRSA. The oxadiazoles show bactericidal activity against vancomycin- and linezolid-resistant MRSA and other Gram-positive bacterial strains, in vivo efficacy in a mouse model of infection, and have 100% oral bioavailability.

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