Novel chemistries to address the challenge of antibacterial drug discovery
Among the many challenges facing drug discovery research in recent years, the search for new antibacterial agents has proved to be among the most unproductive. Many factors have contributed to this problem, but one of the key areas for improvement is the need to test compounds that are more appropriate, as it has become apparent that the screening of randomly assembled, diverse compound libraries has produced extremely low hit rates . Moreover, in-vitro screening often delivers non-drug like and non-target specific structures which tend to face serious efficacy issues in in vivo experiments later on.
To address the major challenge of antibacterial drug discovery, it is critical to access compound libraries which are capable of delivering excellent chemical starting points for completely new classes of antibacterials. A large proportion of known antibacterials have come from natural products and these compounds clearly have structures and properties which have made them a particularly rich source.
At Asinex we have developed an Antibacterial Compound Library based on unique natural product-like scaffolds which are skeletally diverse (saturated fused-, spiro- systems, macrocycles), enriched in polar functionality and which contain multiple stereocenters. The scaffolds and final compounds have been produced by utilizing stereo-controlled transformations and modern coupling reactions, generating specific structural elements inherent to antibacterials, but lacking in traditional screening libraries such as cyclic polyethers, "sugar"-like compounds and macrolactams. It is also significant that the library occupies the unique physicochemical space of known antibiotics which enhances the chances of finding high quality hits in both target specific and whole cell assays .
A wide range of chemical transformations were used for scaffold generation and scaffold decoration which allowed the introduction of higher polarity into the final compounds and the optimization of their physico-chemical profile. Moreover, a wide use of advanced stereocontrolled reactions such as stereocelective epoxidation, tandem etherification and reductive etherification enabled us to obtain target molecules containing multiple stereocenters, with a clearly defined stereo configuration.
Measured Solubility: 100% of compounds are soluble in DMSO at 10 µM, and in PBS at 10 µg/mL
Quality: min.purity of 90%, avg. of 95% (100% LC-MS, 15% NMR), stored as dry powder
ASINEX's antibacterial compound library is only available upon request, please contact us at
Tel.: +7 (495) 780 34 15, +7 (495) 780 34 10
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1. David J. Payne et al. Drugs for bad bugs: confronting the challenges of antibacterial discovery Nature Reviews Drug Discovery 6, 29-40 (January 2007)
2. O'Shea R, Moser HE, Physicochemical properties of antibacterial compounds: implications for drug discovery, J Med Chem. 2008 May 22;51(10):2871-8.