Novel desosamine-modified 14- and 15-membered macrolides without antibacterial activity (CROSBI ID 185024)
Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija
Podaci o odgovornosti
Palej Jakopović, Ivana ; Bukvić Krajačić, Mirjana ; Matanović Škugor, Maja ; Štimac, Vlado ; Pešić, Dijana ; Vujasinović, Ines ; Alihodžić, Sulejman ; Čipčić Paljetak, Hana ; Kragol, Goran
engleski
Novel desosamine-modified 14- and 15-membered macrolides without antibacterial activity
Novel modifications of the desosamine sugar of 14- and 15-membered antibacterial macrolides, in which the desosamine was fused with N-substituted-1, 3- oxazolidin-2-ones, were developed in order to completely suppress antibacterial activity and make them promising agents for other biological targets. The synthesis of such bicyclic desosamine derivatives, especially 1, 3-oxazolidin-2-one formation, was optimized and conducted under mild conditions without a need for protection/deprotection steps for other functional groups. A focused series of novel desosamine- modified macrolide derivatives was prepared and their antibacterial activities tested. It was shown that these macrolide derivatives do not possess any residual antibacterial activity.
macrolide; 1; 3-Oxazolidin-2-one; N-alkylations; Antibacterial activity
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Podaci o izdanju
22 (10)
2012.
3527-3530
objavljeno
0960-894X
10.1016/j.bmcl.2012.03.076