Design of inhibitors of Helicobacter pylori glutamate racemase as selective antibacterial agents: incorporation of imidazoles onto a core pyrazolopyrimidinedione scaffold to improve bioavailabilty.

Basarab, Gregory S; Hill, Pamela; Eyermann, Charles J; Gowravaram, Madhu; Käck, Helena; Osimoni, Ekundayo

Basarab, Gregory S; Hill, Pamela; Eyermann, Charles J; Gowravaram, Madhu; Käck, Helena; Osimoni, Ekundayo.

Affiliation

Basarab GS; Infection Innovative Medicines, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA. greg.basarab@astrazeneca.com

Bioorg Med Chem Lett ; 22(17): 5600-7, 2012 Sep 01.

Article in En | MEDLINE | ID: mdl-22877632

Subject(s)

Amino Acid Isomerases/antagonists & inhibitors; Anti-Bacterial Agents/chemistry; Anti-Bacterial Agents/pharmacology; Helicobacter pylori/drug effects; Pyrimidinones/chemistry; Pyrimidinones/pharmacology; Administration, Oral; Amino Acid Isomerases/metabolism; Animals; Anti-Bacterial Agents/administration & dosage; Anti-Bacterial Agents/pharmacokinetics; Biological Availability; Helicobacter Infections/drug therapy; Helicobacter Infections/microbiology; Helicobacter pylori/enzymology; Humans; Imidazoles/chemistry; Imidazoles/pharmacology; Mice; Models, Molecular; Pyrazoles/administration & dosage; Pyrazoles/chemistry; Pyrazoles/pharmacokinetics; Pyrazoles/pharmacology; Pyrimidinones/administration & dosage; Pyrimidinones/pharmacokinetics; Structure-Activity Relationship

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Full text: 1 Database: MEDLINE Main subject: Pyrimidinones / Helicobacter pylori / Amino Acid Isomerases / Anti-Bacterial Agents Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2012 Type: Article Affiliation country: United States

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