-(1,3,4-Oxadiazol-2-yl)Benzamides as Antibacterial Agents against .

The Centers for Disease Control and Prevention (CDC) recognizes as an urgent-threat Gram-negative bacterial pathogen. Additionally, resistance to frontline treatment (dual therapy with azithromycin and ceftriaxone) has led to the emergence of multidrug-resistant , which has caused a global health crisis. The drug pipeline for has been severely lacking as new antibacterial agents have not been approved by the FDA in the last twenty years. Thus, there is a need for new chemical entities active against drug-resistant . Trifluoromethylsulfonyl (SOCF), trifluoromethylthio (SCF), and pentafluorosulfanyl (SF) containing -(1,3,4-oxadiazol-2-yl)benzamides are novel compounds with potent activities against Gram-positive bacterial pathogens. Here, we report the discovery of new -(1,3,4-oxadiazol-2-yl)benzamides ( and ) with highly potent activity against . Additionally, these new compounds were shown to have activity against clinically important Gram-positive bacteria, such as methicillin-resistant (MRSA), vancomycin-resistant enterococci (VRE), and (minimum inhibitory concentrations (MICs) as low as 0.25 µg/mL). Both compounds were highly tolerable to human cell lines. Moreover, showed an outstanding ability to permeate across the gastrointestinal tract, indicating it would have a high systemic absorption if used as an anti-gonococcal therapeutic.