Enantioselective synthesis and antielastase activity of 1,3,4-trisubstituted and 3,4-disubstituted β-lactam antibiotics

Abstract The synthesis and elastase inhibitory properties of 1,3,4-trisubstituted and 3,4-disubstituted 2-azetidinones are described. Nine of the synthesized derivatives showed elastase inhibitory activities and four of them were specific against human leukocyte elastase (HLE). 2-Deioxy-2-dithianyl-3,4;5,6-di- O -isopropylidene- D -2-glucosyl group attached to the β-lactam nitrogen atom is related to the specificity against HLE.