Fubao Huang

TL;DR: Recent clinical and preclinical studies revealed that Lp‐PLA2 inhibition showed promising therapeutic effects in diabetic macular edema and Alzheimer's disease, and novel inhibitors were identified through a fragment‐based lead discovery strategy.

TL;DR: The identification of novel sulfonamide scaffold Lp-PLA2 inhibitors derived from a relatively weak fragment and the discovery of a micromolar inhibitor with a 300-fold potency improvement clearly demonstrates the power and advantage of integrally employing fragment screening, crystal structures determination, virtual screening, and medicinal chemistry in an efficient lead discovery project.

TL;DR: The discovery of highly selective and irreversible inhibitors of lipoprotein-associated phospholipase A2 (Lp-PLA2) using a covalent-fragment-based approach and the advantage of the enol-cyclocarbamate as a new warhead in designing covalents of serine hydrolases is reported.

TL;DR: A new derivatization reagent, 2-bromo-1-[4-(dimethylamino)phenyl] ethyl ketone (BDAPE), that reacted simultaneously with phenols and aromatic acids was developed and successfully applied to analyze these microbiota-related analytes in mouse feces of a diabetic nephropathy model.

TL;DR: In this paper, Narylsulfonamide compounds represented by general formula I shown in the description, a medicinal composition adopting the compounds as active ingredients, and a use of the compounds or the medicinal composition in the preparation of medicines for treating diseases associated with Lp-PLA2 enzyme activity were described.