Naslov
Novel desosamine-modified 14- and 15-membered macrolides without antibacterial activity

Autori
Palej Jakopović, Ivana ; Bukvić Krajačić, Mirjana ; Matanović Škugor, Maja ; Štimac, Vlado ; Pešić, Dijana ; Vujasinović, Ines ; Alihodžić, Sulejman ; Čipčić Paljetak, Hana ; Kragol, Goran

Izvornik
Bioorganic & medicinal chemistry letters (0960-894X) 22 (2012), 10; 3527-3530

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
macrolide; 1; 3-Oxazolidin-2-one; N-alkylations; Antibacterial activity

Sažetak
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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA