New antibacterial agents: patent applications published in 2011

Area of Science:

• Medicinal Chemistry
• Drug Discovery
• Microbiology

Background:

• The rise of antibiotic resistance necessitates the development of novel antibacterial agents.
• Small molecules represent a promising avenue for new antibacterial therapies.
• Patent literature provides insights into emerging antibacterial research and development.

Purpose of the Study:

• To review and categorize small-molecule antibacterial patent applications published in 2011.
• To identify novel antibacterial compounds and their reported biological targets.
• To assess the landscape of antibacterial drug discovery based on patent filings.

Main Methods:

• Systematic review of 101 patent applications from 2011 disclosing small-molecule antibacterials.
• Analysis of compounds for reported bacterial growth inhibition and lack of fungal/mammalian toxicity.
• Categorization of compounds based on biological targets and/or antibacterial classes.

Main Results:

• Identified various antibacterial classes including protein synthesis inhibitors (targeting 50S/30S ribosomal subunits), DNA synthesis inhibitors (topoisomerase ligands), and cell envelope inhibitors (synthesis and membrane disruption).
• Covered inhibitors targeting cell division, fatty acid biosynthesis, and compounds with unknown targets.
• Included compounds designed to overcome resistance mechanisms, such as efflux and beta-lactamase inhibitors.

Conclusions:

• Patent applications in 2011 revealed diverse strategies for developing small-molecule antibacterials.
• The reviewed patents highlight ongoing innovation in targeting various bacterial pathways and addressing resistance.
• This analysis provides a snapshot of the antibacterial drug discovery landscape in 2011.