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A total synthesis approach of CS-E oligosaccharides was established and a series of derivatives were synthesized. These oligosaccharides were evaluated for a glycosaminoglycan (GAG)-binding protein interaction against cytokines, midkine, and pleiotrophin, by surface-plasmon resonance (SPR) assay. The binding epitopes of oligosaccharides to midkine were mapped using a saturation transfer difference (STD) NMR technique. The groups on the reducing end contributed to binding affinity, and should not be ignored in biological assays. These findings contribute to the structure and activity relationship research and a foundation of understanding that will underpin potential future optimization of this class of oligosaccharides as pharmaceutical agents. [ABSTRACT FROM AUTHOR]

A series of novel 4″-O-desosaminyl clarithromycin derivatives with 11, 12-arylalkyl side chains was synthesized by coupling 6-deoxy-desosamine donors (18, 19) with 4″-OH of compounds 5a–c. The activities of the target compounds were tested against a series of macrolide-sensitive and macrolide-resistant pathogens. Some of them showed activities against macrolide sensitive and resistant pathogens, and compounds 21d and 21e displayed significant improvement of activities against resistant pathogens. [ABSTRACT FROM AUTHOR]

A series of novel 5-O-(4′,6′-O-dimodified)-mycaminose 14-membered ketolides were assessed for their in vitro antibacterial activities against a panel of sensitive and resistant pathogens. Compound 1 and compound 2, two ester analogs, showed the best antibacterial activities against several macrolide-sensitive and macrolide-resistant strains. These results indicated that introducing ester to 6-OH and a small volume ether substituent to the 4-OH of mycaminose could improve the antibacterial activities of ketolides. [ABSTRACT FROM AUTHOR]

During the process of icogenin analog research, we obtained two cytotoxic steroids: compound4and compound6casually. Theirin vitroantitumor activities were tested by the standard MTT assay. The results disclosed that compound4(IC50 = 3.65–6.90 μM) showed potential antitumor activities against HELA, KB cell lines and compound6(IC50 = 2.40–9.05 μM) showed potential antitumor activities against HELA, BGC-823, KB, A549, HCT-8 cell lines. [ABSTRACT FROM PUBLISHER]

Some novel josamycin derivatives bearing an arylalkyl-type side chain were designed and synthesized. By HWE or Wittig reaction, 16-aldehyde group of josamycin analogs were converted into unsaturated carbonyl compounds. They were evaluated for theirin vitroantibacterial activities against a panel of respiratory pathogens.8band8eexhibited comparable activities against a panel of respiratory pathogens, especially to resistant ones in the series of desmycarosyl josamycin analogs. Among of all the target molecules,21showed the best antibacterial activities. [ABSTRACT FROM PUBLISHER]

In order to simplify the synthesis of OSW-1's disaccharide side chain and explore the structure–activity relationship of OSW-1, three 16α-O-maltose OSW-1 analogs carrying three maltose side chains bearing different protections were designed and synthesized. [ABSTRACT FROM PUBLISHER]