The Antibiotics in the Chemical Space

Authors: Gualtieri, Maxime; Baneres-Roquet, Francoise; Villain-Guillot, Philippe; Pugniere, Martine; Leonetti, Jean-Paul

Source: Current Medicinal Chemistry, Volume 16, Number 3, January 2009 , pp. 390-393(4)

Publisher: Bentham Science Publishers

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Abstract:

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.

Document Type: Research article

DOI: http://dx.doi.org/10.2174/092986709787002628

Affiliations: 1: CNRS, UMR 5236, CPBS, 4 Bd Henri IV, CS 69033, F-34965 Montpellier, France.

Publication date: 2009-01-01

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Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.