A new class of antibiotics to fight bacteria such as methicillin-resistant Staphylococcus aureus and other drug-resistant bacteria that threaten public health has been discovered by a team of chemists. The new class, called oxadiazoles, was discovered in silico (by computer) screening and has shown promise in the treatment of MRSA in mouse models of infection. MRSA has become a global public-health problem since the 1960s because of its resistance to antibiotics. Read More
Peter I. O’Daniel, Zhihong Peng, Hualiang Pi, Sebastian 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 Vakulenko, Shahriar Mobashery, Mayland Chang. Discovery of a New Class of Non-β-lactam Inhibitors of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity. Journal of the American Chemical Society, 2014; 136 (9): 3664 DOI: 10.1021/ja500053x
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.