Molecules, Vol. 29, Pages 1519: 4-Chloroisocoumarins as Chlamydial Protease Inhibitors and Anti-Chlamydial Agents

Molecules, Vol. 29, Pages 1519: 4-Chloroisocoumarins as Chlamydial Protease Inhibitors and Anti-Chlamydial Agents
Molecules doi: 10.3390/molecules29071519
Authors:
Matthew J. A. Phillips
Wilhelmina M. Huston
Andrew M. McDonagh
Tristan Rawling

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.

Source: Molecules - March 28, 2024 Category: Chemistry Authors: Matthew J. A. Phillips Wilhelmina M. Huston Andrew M. McDonagh Tristan Rawling Tags: Article Source Type: research