Hagen Schroeter

TL;DR: The design, synthesis, and structure-activity relationships (SAR) for this novel series of inhibitors along with pharmacokinetic and in vivo efficacy data for compound 9 and X-ray crystallography data for selected lead compounds cocrystallized with arginases I and II are reported.

TL;DR: Both the epicatechin glucuronides and sulfates were stable in the solid state when stored under ambient conditions and in aqueous solution when stored refrigerated.

TL;DR: The synthetic routes described here enabled the design of novel arginase inhibitors with improved potency and markedly different physico-chemical properties compared to ABH.

TL;DR: In this paper, orthogonally protected (−)-epicatechin derivatives were prepared in a regiospecific and enantioselective manner to facilitate the installation of a glucuronic acid or sulfate unit onto (−)-propane derivatives after selective removal of the methoxymethyl or p-methoxybenyzl (PMB) protecting group.

TL;DR: This is the first literature report of compounds with improved arginase inhibitory activity, relative to ABH, and represents a promising starting point for further optimization of in vitro potency and the identification of better tool molecules for in vivo investigations of the potential pathophysiological roles of arginases.