Novel coumarinic derivatives were synthesized and tested for their inhibitory potency toward α-CT and HLE. Cycloalkyl esters and amides were found to be essentially inactive on both enzymes. On the opposite, aromatic esters strongly inactivated α-CT whereas HLE was less efficiently inhibited with dichlorophenyl ester derivatives (kinact/KI= 4000M− 1 s− 1 for 36). Representative examples of amide, ester, thioester and ketone derivatives were prepared ...
