NEW AMINOTHIAZOLYLGLYCYLCEPHALOSPORINS WITH A 1, 5-DIHYDROXY-4-PYRIDONE-2-CARBONYL GROUP

I. SYNTHESIS AND BIOLOGICAL ACTIVITY OF CEPHALOSPORIN DERIVATIVES LEADING TO MT0703

Abstract

A series of new aminothiazolylglycylcephalosporins with a mono- or dihydroxypyridonecarbonyl group at the α-amino group of the C-7 substituent have been prepared and antibacterial activity of these compounds was investigated. Among them, the compounds having a l, 5-dihydroxy-4-pyridone-2-carbonyl group showed excellent anti-pseudomonal activity. In particular, (6R, 7R)-7-[(RS)-2-(2-aminothiazol-4-yl)-2-(1, 5-dihydroxy-4-pyridone-2-carboxamido)-acetamido]-3-[[l-(2-hydroxyethyl)pyridinium-4-yl]thiomethyl]ceph-3-em-4-carboxylate(MT0703, 7g) was found to be a well balanced compound with respect to antibacterial activity.