Jorge Esquivias

TL;DR: These studies have identified the first candidate in the triazolopyrimidine series to meet previously established progression criteria for efficacy and ADME properties, justifying further development of this compound toward clinical candidate status.

TL;DR: In vivo efficacy evaluation of two optimized THPP and Spiro leads showed how the compounds were able to reduce >2 logs bacterial cfu counts in the lungs of infected mice, and attractive in vitro and in vivo anti-tubercular profiles of both lead series are described.

TL;DR: The discovery of anti-tubercular agents inhibiting tryptophan synthase highlights the therapeutic potential of this enzyme and draws attention to the prospect of other amino acid biosynthetic pathways as future Mtb drug targets.

TL;DR: The spiro compounds were explored by a combination of traditional in-house research and open source methods, and many members of the series displayed striking potency and low toxicity, and highly promising in vivo activity in a mouse model was confirmed with one of the analogues.

TL;DR: This work demonstrates the versatility and potential of GuaB2 as an anti-tubercular drug target and identified 7 new chemical series from a high-throughput resistance-based phenotypic screen using Mycobacterium bovis BCG over-expressing Gua B2.