UK-18,892: Resistance to Modification by Aminoglycoside-Inactivating Enzymes

Author:

Andrews R. J.1,Brammer K. W.1,Cheeseman H. E.1,Jevons S.1

Affiliation:

1. Pfizer Central Research, Pfizer Ltd., Sandwich, Kent, United Kingdom

Abstract

UK-18,892, a new semisynthetic aminoglycoside, was active against bacteria possessing aminoglycoside-inactivating enzymes, with the exception of some known to possess AAC(6′) or AAD(4′) enzymes. This activity has been rationalized by using cell-free extracts of bacteria containing known inactivating enzymes, where it was shown that UK-18,892 was not a substrate for the APH(3′), AAD(2″), AAC(3), and AAC(2′) enzymes. It was also demonstrated that UK-18,892 protected mice against lethal infections caused by organisms possessing aminoglycoside-inactivating enzymes.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Reference12 articles.

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3. Mechanisms of antibiotic resistance in bacteria. Annu;Benveniste R.;Rev. Biochem.,1973

4. Aminoglycoside resistance in bacteria mediated by gentamicin acetyl transferase II, an enzyme modifying the 2'-amino group of aminoglycoside antibiotics;Chevereau M.;Biochemistry,1974

5. Cox D. A. K. Richardson and B. C. Ross. 1977. The aminoglycosides p. 1-90. In P. Sammes (ed.) Topics in antibiotic chemistry vol. 1. Ellis Horwood Ltd. England.

Cited by 5 articles. 订阅此论文施引文献 订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献

1. The potential for discovery and development of improved aminoglycosides;The American Journal of Medicine;1986-06

2. Aminoglycoside research 1975-1985: prospects for development of improved agents;Antimicrobial Agents and Chemotherapy;1986-04

3. Enzymatic Modification of Aminoglycoside Antibiotics in Gentamicin-Resistant Gram-Negative Bacteria;Zentralblatt für Bakteriologie, Mikrobiologie und Hygiene. 1. Abt. Originale. A, Medizinische Mikrobiologie, Infektionskrankheiten und Parasitologie;1984-08

4. Effect on the renal function of UK 18892;Journal of Antimicrobial Chemotherapy;1980

5. Chapter 11 Antibiotics;Annual Reports in Medicinal Chemistry;1979

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