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  • Title: Structure-based design, synthesis, and antimicrobial activity of indazole-derived SAH/MTA nucleosidase inhibitors.
    Author: 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.
    Journal: J Med Chem; 2003 Dec 18; 46(26):5663-73. PubMed ID: 14667220.
    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.
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