| 摘要 |
<p>6-(1-Carbamoyl-1-hydroxymethyl)penicillanic acid derivatives of the formula:
<CHEM>
wherein
n is 0, 1 or 2;
R is hydrogen, a radical group forming an ester hydrolyzable under physiological conditions, or an acyloxymethyl or 1-(acyloxy)ethyl radical derived from a conventional betalactam antibiotic; and
R<1> and R<2> are taken separately and are each independently for example, hydrogen, (C1-C4)alkyl, (C5-C6)cycloalkyl, phenyl benzyl or one of said groups substituted by methyl, hydroxy, (C1-C2)alkoxy, -COOR<3>, or -CONR<3>R<4>; or
R<1> and R<2> are taken together with the nitrogen to which they are attached to form for example, a pyrrolidine, piperidine, perhydroazepine, morpholine 4-[formyl, (C1-C4)alkyl, phenyl benzyl, pyridyl or 2-hydroxyethyl]piperazine, indoline, isoindoline, 1,2,3,4-tetrahydroquinoline or 1,2,3,4-tetrahydroisoquinoline ring system, or one of said ring systems substituted by methyl, hydroxy, hydroxymethyl, carboxy, carbamoyl, -COOR<3> or -CONR<3>R<4>.
<??>The compounds are useful as antibacterial agents and/or betalactamase inhibitors. </p> |
