title: Structure-based design, synthesis, and antimicrobial activity of purine derived SAH/MTA nucleosidase inhibitors.
abstract: The structure-based design, synthesis, and biological activity of novel inhibitors of S-adenosyl homocysteine/methylthioadenosine (SAH/MTA) nucleosidase are described. Using 6-substituted purine and deaza purines as the core scaffolds, a systematic and structure guided series of modifications provided low nM inhibitors with broad-spectrum antimicrobial activity.
authors.affiliation: Department of Medicinal Chemistry, Quorex Pharmaceuticals, Carlsbad, CA 92008, USA.
authors.forename: Martina E
authors.initials: ME
authors.lastname: Tedder
authors.forename: Zhe
authors.initials: Z
authors.lastname: Nie
authors.forename: Stephen
authors.initials: S
authors.lastname: Margosiak
authors.forename: Shaosong
authors.initials: S
authors.lastname: Chu
authors.forename: Victoria A
authors.initials: VA
authors.lastname: Feher
authors.forename: Robert
authors.initials: R
authors.lastname: Almassy
authors.forename: Krzysztof
authors.initials: K
authors.lastname: Appelt
authors.forename: Kraig M
authors.initials: KM
authors.lastname: Yager
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006710:Homocysteine / Q000037:antagonists & inhibitors / Q000378:metabolism; D009699:N-Glycosyl Hydrolases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011683:Purine-Nucleoside Phosphorylase / Q000037:antagonists & inhibitors / Q000378:metabolism; D011687:Purines / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D011687:Purines; D006710:Homocysteine; D011683:Purine-Nucleoside Phosphorylase; C021784:5'-methylthioadenosine phosphorylase; D009699:N-Glycosyl Hydrolases