Medicinal Chemistry

(Jacob Rumans) #1

9.4.3.1 Antibacterials Targeting the Ribosomal 30S Subunit: Tetracyclines


The tetracyclines are closely related to the anthracycline glycoside antitumor agents.
Available since the early 1950s, they are broad-spectrum antibiotics active against a
wide variety of microorganisms, including some that either are not sensitive or are
resistant to β-lactam antibiotics. Tetracyclines interfere with protein synthesis by
inhibiting the binding of aminoacyl-tRNA to the 30S subunit of the ribosome in the
microorganisms. The release of completed peptides from the ribosome is also blocked.
The analogs include tetracycline (9.67), chlortetracycline (9.68), oxytetracycline
(9.69), demeclocycline (9.70), methacycline (9.71), doxycycline (9.72), and
minocycline (9.73).


EXOGENOUS PATHOGENS AND TOXINS 573
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