The first amphenichol was
chloramphenichol, that is a natural product isolated from Streptomyces in
the 1940s. Several chemical derivatives nad analogues have been prepared, but
with a few exceptions the antibacterial activity was rsignificantly reduced.
Nonetheless a few interesting compounds have been developed, including: Azidamfenicol,
Chloramphenicol, Florfenicol, Thiamphenicol.
Mechanism of action
Amphenicols acts by inhibiting the peptidyl transferase reaction the step at which the peptide bond is formed on bacterial ribosomes. The spectrum of activity includes most Gram-positive and Gram-negative bacteria, and also extends to chlamydiae and rickettsiae, strictly intracellular bacteria that cause a variety of infections, including trachoma, psittacosis, and typhus. Resistance when it occurs is usually due to bacterial enzymes that acetylate the two hydroxyl groups.
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