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Updated: Jun 28, 2025

Forward Genetic Approaches in Chlamydia trachomatis
Published on: October 23, 2013
4-Chloroisocoumarins as Chlamydial Protease Inhibitors and Anti-Chlamydial Agents
Matthew J A Phillips1, Wilhelmina M Huston2, Andrew M McDonagh1
1School of Mathematical and Physical Sciences, Faculty of Science, University of Technology Sydney, Sydney, NSW 2007, Australia.
Abstract:
4-Chloroisocoumarin compounds have broad inhibitory properties against serine proteases. Here, we show that selected 3-alkoxy-4-chloroisocoumarins preferentially inhibit the activity of the conserved serine protease High-temperature requirement A of Chlamydia trachomatis. The synthesis of a new series of isocoumarin-based scaffolds has been developed, and their anti-chlamydial properties were investigated. The structure of the alkoxy substituent was found to influence the potency of the compounds against High-temperature requirement A, and modifications to the C-7 position of the 3-alkoxy-4-chloroisocoumarin structure attenuate anti-chlamydial properties.
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