A set of 17 novel ketolides bearing an aryltetrazolyl-substituted alkyl side chain were synthesized and evaluated for their antibacterial activities, which the aryltetrazolyl group was selected to replace the hetero-aryl moiety of the side chain in telithromycin for designing new compounds. The synthesis of aryltetrazolyl alkylamines was reported in detail. The antibacterial activities of new ketolides were evaluated against a number of pathogens including macrolide-resistant organisms by using telithromycin as the reference. Many of the evaluated compounds exhibited remarkable activities against both erythromycinsusceptible and erythromycin-resistant organisms such as Staphylococcus aureus (except S. aureus AD-08), Pseudomonas aeruginosa and Escherichia coli. Among these, the compound 11e exhibited excellent antibacterial potency against all the strains in comparison with others.
Design, Synthesis and Antibacterial Activity of Novel Ketolides Bearing an Aryltetrazolyl-Substituted Alkyl Side Chain. -A series of novel C-11,12 cyclic carbamate ketolides (17 examples) are synthesized from clarithromycin and evaluated for their antibacterial activities. Derivatives (I), the most active compound, exhibits excellent antibacterial potency against all the strains studied. -(SONG, Q.-L.; GUO, B.-Q.; ZHANG, W.; LAN, P.; SUN, P.-H.; CHEN*, W.-M.; J. Antibiot. 64 (2011) 8, 571-581, http://dx.doi.org/10.
Antibiotics U 1200Synthesis and Antibacterial Activities of (9S)-3-O-Descladinose-6-O-methyl--3-oxo-12-(Δ 2 -pyrazolinyl)-12-dehydroxy-21-demethyl-9-dihydroerythromycin A. -A 10-step synthesis of title compound (I) from clarithromycin is presented. This product is active against macrolide-sensitive S. aureus and Staphylococcus epidermidis in vitro and also shows a higher activity against macrolide-resistant S. aureus 5676 than erythromycin and clarithromycin. -(WANG, Y.-T.; HU, L.; CHEN*, W.-M.; HU, A.-X.; SONG, Q.-L.; GUAN, D.; Lett.
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