Novel azetidinones and their use to inhibit lactamase enzymes that destroy beta-lactam antibiotics

Abstract

Abstract COMPOUNDS OF THE FORMULA: 1-R3,3-(R1-CO-NH-),4-R2-AZETIDIN-2-ONE IIN WHICH R1 REPRESENTS AN ARYL, ARYLAKYL, OR ARYLOXYALKYL GROUP IN WHICH THE ARYL GROUP OR MOIETY MAY OPTIONALLY BE SUBSTITUTED BY ONE OR MORE ALKYL, ALKOXY, HALOACETAMIDO, NITRO OR AMINO GROUPS OR HALOGEN ATOMS AND THE ALKYL CHAIN MAY OPTIONALLY BE SUBSTITUTED BY AN AZIDO AMINO, CARBOXYL, OR ALKOXY GROUP; OR R1 REPRESENTS A GROUP (IN WHICH Z REPRESENTS H, NH2, OR N3) OF THE FOLLOWING FORMULA: THIENYL-CH(-Z)- R2 REPRESENTS A PHENYL OR NAPHTYL GROUP WHICH MAY OPTIONALLY BE SUBSTITUTED WITH ONE OR MORE ALKOXY GROUPS OR HALOGEN ATOMS; AND R3 REPRESENTS H OR AN ALKYL GROUP CONTAINING FROM 1 TO 4 CARBON ATOMS OR R3 MAY BE AN ACYL OR ALKOXY CARBONYL GROUP, AND ACID ADDITION SALTS THEREOF, THESE COMPOUNDS INHIBIT LACTAMASE ENZYMES WHICH DESTORY B-LACTAM ANTIBIOTICS.

Inventors

• 👤 J Gladych
• 👤 C Hussey

Bibliographic Details