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Antibiotics are substances that inhibit the growth of

microorganisms (anti-metabolites) or their replication


(a bacteriostatic effect). They were traditionally
obtained by extracting them fromculturesof microbes.
However, most drugs on the market today
aresemisyntheticderivatives of natural products.
In the late 1920s, while working in a London hospital,
Alexander Flemingobserved a mold overtaking a
culture of staphylococcus bacteria he was growing in his
laboratory.
He extracted juices from the mold and, in 1929,
reported that the extract, which he called penicillin, had
antiseptic (anti-infectious) activity.

The fungus was subsequently identified


asPenicillium notatum(now calledPenicillium
chrysogenum).
It was not until the 1940s that penicillin was put into
clinical use. Howard W. Florey, professor of pathology
at Oxford's Sir William Dunn School of Pathology, and
Ernst B. Chainare credited with culturing the fungus
and producing the first significant quantities of
penicillin for treating bacterial infections.
In 1945 Fleming, Florey, and Chain received the
Nobel Prize in physiology or medicine"for the
discovery of penicillin and its curative effect in various
infectious diseases."

-Lactam Antibiotics
A variety of penicillins have been produced by the fermentation
of Penicillium chrysogenum in the presence of different nutrients.
Penicillin G predominates when the culture medium is rich in
phenylacetic acid, whereas the incorporation of phenoxyacetic acid
favors penicillin V (phenoxymethylpenicillin).
Semisynthetic penicillins, such as ampicillin and amoxicillin, are
prepared by replacing the aromatic side chain of biosynthetically
derived penicillins with other chemical groups.
All penicillins are -lactam antibiotics and have the same
mechanism of action: They inhibit bacterial cell wall biosynthesis .
Bacterial cell walls differ from mammalian cell walls and are
therefore attractive targets for antibiotics. Bacterial cell walls
contain -lactam receptors , known as penicillin-binding proteins
(PBPs).

Figure 2. The -lactam ring.

PENCILINE-G

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