Jonathan Thomas Seal

TL;DR: A novel series of quinoline isoxazole BET family bromodomain inhibitors shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine in vivo endotoxaemia model.

TL;DR: A phenyl dimethyl isoxazole chemotype resulting from a focused fragment screen has been rapidly optimized through structure-based design, leading to a sulfonamide series showing anti-inflammatory activity in cellular assays.

TL;DR: The discovery, synthesis and biological evaluation of a novel series of 7-isoxazoloquinolines is described and several analogs are shown to increase ApoA1 expression within the nanomolar range in the human hepatitis cell line HepG2.

TL;DR: Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy are described in this article, where the authors discuss the use of such compounds in therapy.

TL;DR: The X-ray crystal structure-directed optimisation of a novel weak fragment ligand with a pan-second bromodomain (BD2) bias, to potent and highly BD2 selective inhibitors is described.