Document Report Card

ID: ALA1144886

Journal: J Med Chem

Title: Structure-based design, synthesis, and antimicrobial activity of indazole-derived SAH/MTA nucleosidase inhibitors.

Authors: Li X, Chu S, Feher VA, Khalili M, Nie Z, Margosiak S, Nikulin V, Levin J, Sprankle KG, Tedder ME, Almassy R, Appelt K, Yager KM.

Abstract: 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.

CiteXplore: 14667220

DOI: 10.1021/jm0302039