Indole is one of the most ubiquitous privileged structure in the field of medicinal chemistry. Indole derivatives are particularly well represented in natural products, amine GPCR ligands, enzyme inhibitors, DNA and nucleotides interfering compounds. Isosteric replacement of carbon by nitrogen often results in increased activity or selectivity, metabolic stabilization and better pharmacokinetics (increased solubility, oral activity, longer half-life). However, synthetic difficulties have hampered the development of azaindoles, and more specifically, of 4 and 7-azaindoles. In collaboration with Provence Technologies, which has developed new methodologies for the synthesis of functionalized azaindoles (www.azaindole.com), Chem-X-Infinity has delivered a library built upon original 4 and 7-azaindole acidic intermediates.

Examples of active azaindole compounds include many kinase inhibitors and GPCR antagonists. The scaffold is so small that it could be useful in any research domain and could be considered as a good surrogate for indole to improve pharmacokinetic properties or to insure patentability. It is noticeable that more than 44 % of the compounds are predicted to be CNS by our model developed with CIPF.

Details and scientific references can be found in the azaindole library brochure.

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