There is considerable interest in the design of stable small molecule inhibitors of serine proteases and in devising tactics to enhance the specificity and potency of such reagents. A particular challenge is to design specific inhibitors of high potency without resorting to peptide functionality as a means of delivering covalent labels to the target enzyme active site. 2 4H-3, 1-Benzoxazin-4-one (1) represents an attractive lead structure for ...
