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Aminoglycoside antibiotics. 3. Epimino derivatives of neamine, ribostamycin, and kanamycin B.

Abstract：

:2',3'-Epimino analogues of neamine, ribostamycin, and kanamycin B possessing little or no intrinsic antimicrobial activity were designed to enhance the activity of kanamycin A against bacterial strains that elaborate aminoglycoside 3'-phosphotransferases. Routes were devised for their synthesis from the parent antibiotics and the 2'',3''-epimino analogue of kanamycin B also was prepared. None of these analogues was active against phosphotransferase-producing bacteria, although the kanamycin B derivatives showed very weak activity against nonresistant strains. At 8 and 32 microgram/mL, the 2',3'-epimino analogue of neamine produced a small synergistic effect on the activity of kanamycin A against a strain of Escherichia coli that produces aminoglycoside 3'-phosphotransferase II. The N3-(carbobenzyloxy) derivative of this analogue produced a small effect against the same strain, and it, as well as the 2'',3''-epimino analogue of kanamycin B, slightly enhanced the activity of kanamycin A against a strain of Proteus rettgeri that elaborates a similar enzyme.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Kumar V,Jones GS Jr,Blacksberg I,Remers WA,Misiek M,Pursiano TA

doi

10.1021/jm00175a009

subject

Has Abstract

pub_date

1980-01-01 00:00:00

pages

42-9

issue

1

eissn

0022-2623

issn

1520-4804

journal_volume

23

pub_type

杂志文章

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