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Aminoglycoside Antibiotics (Paperback, Softcover reprint of the original 1st ed. 1982)
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Aminoglycoside Antibiotics (Paperback, Softcover reprint of the original 1st ed. 1982)
Series: Handbook of Experimental Pharmacology, 62
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The first useful antibiotic found by screening was streptomycin.
The late Prof. WAKSMAN started screening for antibacterial
antibiotics in 1940 and, after finding actinomycin in 1941, he and
his collaborators discovered streptomycin in 1944. This antibiotic
made a great contribution in saving human lives from tuberculosis
and acute serious infections. About 1957, after wide usage of such
antibiotics as penicillin, streptomycin, chloramphenicol,
tetracycline, and erythromycin, staphy- lococci and Gram negative
organisms resistant to all or most antibiotic drugs ap- peared in
hospital patients. The origin and treatment of such resistant
strains be- came a major topic of investigation. At that time,
kanamycin was discovered and used in the treatment of resistant
infections. It may be said that the appearance of resistant strains
stimulated a resurgence of research on new antibacterial antibiot-
ics and their derivatives. In 1965, kanamycin-resistant strains
were found in hospital patients and, undertaking the study of the
mechanisms of resistance, I found that resistant strains produce
intracellular enzymes that can transfer either the terminal phos-
phate of ATP or the acetate of acetyl-CoA to the 3' -hydroxyl or
the 6' -amino group of 2-deoxystreptamine~containing antibiotics.
These results, reported in 1967, made it possible to design new
synthetic derivatives that would inhibit the growth of kanamycin
resistant strains of microorganisms. Thus, a new research area was
opened: the development of aminoglycosides useful in the treatment
of drug-resis- tant infections.
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