Design, synthesis and activity of thio-linked arabinofuranosyl disaccharides against mycobacterial tuberculosis (MTB) and Mycobacterium avium complex (MAC)

作者：Khare Naveen K^*; Duarte Franco J; Reynolds Robert C; Maddry Joseph A

来源：ARKIVOC, 2013, 290-315.

• Arabinofuranosyl transferases
• inhibitors
• arabinofuranose
• thio linked disaccharides
• mycobacteria
• bacterial cell walls

We report the chemical synthesis of a series of disaccharides of arabinofuranose with a glycosidic sulfur linker as mimics of the acceptor for arabinofuranosyltransferases with and without using any activator to avoid any complex reactions. These analogs were tested for in vitro activity against MTB strain H37Ra and 3 MAC clinical isolates. MICs were determined using a colorimetric microdilution broth assay. Bactericidal activity was studied with kill curves over a period of seven days. Intracellular activity against MTB H37Ra was determined in the Mono Mac 6 (MM6) human monocytic cell line.

• 出版日期2013