Rakesh

TL;DR: The antitubercular efficacy of spectinamides demonstrates that synthetic modifications to classical antibiotics can overcome the challenge of intrinsic efflux pump-mediated resistance and expands opportunities for target-based tuberculosis drug discovery.

TL;DR: Overall, the addition of solubilizing and metabolically blocked outer rings did improve solubility and decrease protein binding as designed, however, the metabolic stability for compounds in this series was generally lower than desired.

TL;DR: The structure-activity relationships detailed here emphasize the need to examine efflux-mediated resistance in the design of antituberculosis drugs and demonstrate that it is possible to overcome intrinsic efflux with synthetic modification.

TL;DR: This study explores if incorporation of the outer ring elements found in first and second generation oxazolidinones into the nitroimidazole core of pretomanid can be used to improve its physicochemical and antitubercular properties.

TL;DR: Together these studies show that 9a is a nanomolar inhibitor of actively growing as well as nonreplicating M. tuberculosis grown under hypoxia.