New antibacterial agents: patent applications published in 2010.
This review summarizes patent applications from 2010 for small molecules for which there is a claim of antibacterial activity. The primary criterion for inclusion in this analysis was reporting of cellular antibacterial activity data (MICs) for at least one compound. Patent applications are reviewed according to their biological target and antibacterial class. Protein synthesis inhibitors disclosed in this period include inhibitors of the 50S ribosome subunit (oxazolidinones, macrolides/ketolides and pleuromutilins), 30S ribosome subunit (aminoglycosides and tetracyclines) and nonribosomal targets (PDF inhibitors). DNA synthesis inhibitors include inhibitors of GyrA/ParC and GyrB/ParE. Cell envelope disruptors disclosed in 2010 cover both inhibitors of cell-envelope synthesis (LpxC inhibitors, β-lactams and glycopeptides), as well as membrane disruptors (lipopeptides and polymyxins). Other antibacterial classes covered in this review include rifamycins and antibacterial peptides. Patent applications for compounds aimed at overcoming resistance mechanisms (efflux inhibitors and β-lactamase inhibitors) are also described.
AstraZeneca, Infection Innovative Medicines Unit, 35 Gatehouse Drive, Waltham, MA 02451, USA.
Suzanne S
SS
Stokes
Marshall
M
Morningstar
Helena
H
Kocis
Jeroen C
JC
Verheijen
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D024881:Drug Resistance, Bacterial; D006801:Humans; D019384:Nucleic Acid Synthesis Inhibitors / Q000494:pharmacology; D010330:Patents as Topic; D011500:Protein Synthesis Inhibitors / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D019384:Nucleic Acid Synthesis Inhibitors; D011500:Protein Synthesis Inhibitors