RESUMO
A series of carbosilane dendrimers uniformly functionalized with sialyl lactose moieties (Neu5Ac alpha2-->3Gal beta1-->4Glc) was systematically synthesized, and biological evaluations for anti-influenza virus activity using the glycodendrimers were performed. The results suggested that the glycodendrimers had unique biological activities depending on the form of their core frame, and Dumbbell(1)6-amide type glycodendrimer 7 showed particularly strong inhibitory activities against human influenza viruses [A/PR/8/34 (H1N1) and A/Aichi/2/68 (H3N2)]. The results suggested that the structure-activity relationship (SAR) on the glycolibrary against various influenza viruses was observed, and dumbbell-shaped dendrimers as supporting carbohydrate moieties were found to be the most suitable core scaffolds in this study.
Assuntos
Antivirais/química , Antivirais/farmacologia , Vírus da Influenza A/efeitos dos fármacos , Silanos/química , Silanos/farmacologia , Animais , Antivirais/síntese química , Linhagem Celular , Dendrímeros/síntese química , Dendrímeros/química , Dendrímeros/farmacologia , Cães , Eritrócitos/citologia , Eritrócitos/virologia , Hemaglutinação/efeitos dos fármacos , Hemólise/efeitos dos fármacos , Humanos , Vírus da Influenza A Subtipo H1N1/efeitos dos fármacos , Vírus da Influenza A Subtipo H1N1/patogenicidade , Vírus da Influenza A Subtipo H3N2/efeitos dos fármacos , Vírus da Influenza A Subtipo H3N2/patogenicidade , Vírus da Influenza A/patogenicidade , Influenza Humana/tratamento farmacológico , Rim/citologia , Rim/virologia , Lactose/química , Estrutura Molecular , Ácido N-Acetilneuramínico/química , Silanos/síntese química , Relação Estrutura-AtividadeRESUMO
An efficient synthesis of a series of carbosilane dendrimers uniformly functionalized with sialyl alpha(2-->3) lactose (Neu5Acalpha(2-->3)Galbeta(1-->4)Glcbeta1-->) moieties was accomplished. The results of a preliminary study on biological responses against influenza virus hemagglutinin, using the sialyl lactose clusters showed unique biological activities on the basis of the structure-activity relationship according to the carbosilane scaffolds.
