DHFR

DHFR-targeted antibacterial drugs have been used successfully for forty years. The development of widespread bacterial resistance to DHFR-based drugs such as trimethoprim has severely reduced their utility for treating infections. In its DHFR program, Trius is using structural biology to understand changes in molecular recognition that lead to resistance and to design new DHFR-based antibacterial that circumvent resistance. Our efforts have yielded multiple series of novel compounds with excellent antibacterial potency, selectivity and spectrum that include strains resistant to trimethoprim. We are optimizing these leads with the goal of providing a novel wide spectrum antibacterial agent that addresses the current clinical need.