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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

The Antibiotics in the Chemical Space

Author(s): Maxime Gualtieri, Francoise Baneres-Roquet, Philippe Villain-Guillot, Martine Pugniere and Jean-Paul Leonetti

Volume 16 , Issue 3 , 2009

Page: [390 - 393] Pages: 4

DOI: 10.2174/092986709787002628

Price: $65


Ensuring the availability of new antibiotics to eradicate resistant pathogens is a critical issue, but very few new antibacterials have been recently commercialized. In an effort to rationalize their discovery process, the industry has utilized chemical library and high-throughput approaches already applied in other therapeutical areas to generate new antibiotics. This strategy has turned out to be poorly adapted to the reality of antibacterial discovery. Commercial chemical libraries contain molecules with specific molecular properties, and unfortunately systemic antibacterials are more hydrophilic and have more complex structures. These factors are critical, since hydrophobic antibiotics are generally inactive in the presence of serum. Here, we review how the skewed distribution of systemic antibiotics in chemical space influences the discovery process.

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