Revised Structure of Penicillazine and Preparation, Bioactivities of Penicillazine Derivatives

The structure of penicillazine has been revised on the basis of hydrolysis reaction. Its absolute stereochemistry has been confirmed by X-ray diffraction using copper radiation. Eight new penicillazine derivatives (1-8) were prepared and some of them showed higher levels of activity than penicillazine against α-glucosidase and Human DNA topoisomerase I.