Steven Park, Riccardo Russo, Landon Westfall, Riju Shrestha, Matthew Zimmerman, Veronique Dartois, Natalia Kurepina, Barry Kreiswirth, Eric Singleton, Shao-Gang Li, Nisha Mittal, Yong-Mo Ahn, Joseph Bilotta, Kristie L Connolly, Ann E Jerse, Joel S Freundlich, David S Perlin
Drug-resistant Neisseria gonorrhoeae is a serious global health concern. New drugs are needed that can overcome existing drug resistance and limit the development of new resistances. Here, we describe the small molecule tricyclic pyrimidoindole JSF-2414 [8-(6-fluoro-8-(methylamino)-2-((2-methylpyrimidin-5-yl)oxy)-9H-pyrimido[4,5-b]indol-4-yl)-2-oxa-8-azaspiro[4.5]decan-3-yl)methanol], which was developed to target both ATP-binding regions of DNA gyrase (GyrB) and topoisomerase (ParE). JSF-2414 displays potent activity against N...
August 16, 2022: Antimicrobial Agents and Chemotherapy