SYNTHESIS AND BETA-LACTAMASE INHIBITORY ACTIVITY OF OARYLTHIOETHYL-1,2,3-TRIAZOL-4-YL)-METHYLENE]PENAM SULFONES

The synthesis of beta-lactamase inhibitory activity of a series of sod ium ioethyl-1,2,3-triazol-4-yl)methylene]penicillanate 1,1-dioxides ar e described. Their activity was compared with tazobactam and sulbactam . The Z-isomers were more active than the E-isomers. The in vitro acti vity of the Z-isomers of the phenylthiadiazole derivatives (13a and 15 a) was better than sulbactam against the tested beta P-lactamases and comparable to tazobactam especially against TEM-2 and cephalosporinase . But their synergistic activity with five antibiotics was inferior to tazobactam.