jm015566s_si_001.pdf (379.53 kB)
Synthesis and Antibacterial Activity of Acylides (3-O-Acyl-erythromycin Derivatives): A Novel Class of Macrolide Antibiotics
journal contribution
posted on 2001-10-27, 00:00 authored by Tetsuya Tanikawa, Toshifumi Asaka, Masato Kashimura, Yoko Misawa, Keiko Suzuki, Masakazu Sato, Kazuya Kameo, Shigeo Morimoto, Atsushi NishidaIntroduction of an acyl group to the 3-O-position
of erythromycin A derivatives instead of l-cladinose led to a
novel class of macrolide antibiotics that we named “acylides”.
The 3-O-nitrophenylacetyl derivative TEA0777 showed significantly potent activity against not only erythromycin-susceptible Gram-positive pathogens but also inducibly macrolides-lincosamides-streptogramin B (MLSB)-resistant Staphylococcus aureus and efflux-resistant Streptococcus pneumoniae.
These results indicated that acylides have potential as next-generation macrolide antibiotics.