Synthesis and Antibacterial Activity of a Novel Series of Acylides: 3-O-(3-Pyridyl)acetylerythromycin A Derivatives
journal contributionposted on 20.05.2003 by Tetsuya Tanikawa, Toshifumi Asaka, Masato Kashimura, Keiko Suzuki, Hiroyuki Sugiyama, Masakazu Sato, Kazuya Kameo, Shigeo Morimoto, Atsushi Nishida
Any type of content formally published in an academic journal, usually following a peer-review process.
A novel series of acylides, 3-O-(aryl)acetylerythromycin A derivatives, were synthesized and evaluated. These compounds have significant potent antibacterial activity against not only Gram-positive pathogens, including inducibly macrolide-lincosamide-streptogramin B (MLSB)-resistant and efflux-resistant strains, but also Gram-negative pathogens, such as H. influenzae. 6,9:11,12-Dicarbonate acylide 47 (FMA0122) was twice as active against H. influenzae than azithromycin, whereas it showed only moderate in vivo efficacy in mouse protection tests. However, the 11,12-carbamate acylide 19 (TEA0929), which showed potent antibacterial activity against almost all of the main causative pathogens of community-acquired pneumonia tested, exhibited excellent in vivo efficacy comparable to those of second-generation macrolides.