647853-30-3Relevant articles and documents
Structure-Based Design, Synthesis, and Antimicrobial Activity of Indazole-Derived SAH/MTA Nucleosidase Inhibitors
Li, Xiaoming,Chu, Sam,Feher, Victoria A.,Khalili, Mitra,Nie, Zhe,Margosiak, Stephen,Nikulin, Victor,Levin, James,Sprankle, Kelly G.,Tedder, Martina E.,Almassy, Robert,Appelt, Krzysztof,Yager, Kraig M.
, p. 5663 - 5673 (2007/10/03)
The structure-based design, synthesis, and biological activity of a novel indazole-containing inhibitor series for S-adenosyl homocysteine/methylthioadenosine (SAH/MTA) nucleosidase are described. Use of 5-aminoindazole as the core scaffold provided a structure-guided series of low nanomolar inhibitors with broad-spectrum antimicrobial activity. The implementation of structure-based methodologies provided a 6000-fold increase in potency over a short timeline (several months) and an economy of synthesized compounds.