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Synthesis and antibacterial activity of novel 4-aryl-[1,2,3]-triazole containing macrolides

✍ Scribed by David Pereira; Prabhavathi Fernandes


Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
874 KB
Volume
21
Category
Article
ISSN
0960-894X

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✦ Synopsis


Two series of novel triazole containing 14-member macrolides having either a cladinose or a 3-pyridyl acetate group at the 3-position of the macrolide ring were synthesized. The in vitro antibacterial activities against S. aureus, S. pneumoniae, S. pyogenes and E. faecalis were determined. Macrolide 7a and the fluoroketolide 1 (CEM-101) were evaluated in vivo in murine systemic infection models. All of the macrolide analogs were less active in vitro and in vivo than the fluoroketolide 1 (CEM-101).


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In this investigation, several novel N2hydroxymethyl and N2-aminomethyl derivatives of 5-(3-chlorophenyl)-4-(4-methylphenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione and 4-(4-bromophenyl)-5-(3-chlorophenyl)-2,4-dihydro-3H-1,2,4-triazole-3thione were prepared. All synthesized compounds were screened fo