The NLRP3 inflammasome is a component of the innate immune system involved in the production of pro-inflammatory cytokines. Aberrant activation by a wide range of exogenous and endogenous signals can lead to chronic, low-grade inflammation. Inhibition of the NLRP3 inflammasome with small molecules represents a potential treatment for several debilitating diseases with a large unmet medical need, including Alzheimer’s disease, Parkinson’s disease, arthritis and cancer. Despite a great deal of interest, there are currently no specific NLRP3 inflammasome inhibitors on the market. This poster will describe the medicinal chemistry approach that took a proprietary NLRP3 inhibitor and replaced a urea linker with a range of heterocycles. This bioisosteric investigation led to the discovery of a new class of small molecule NLRP3 inhibitors with improved potency and attractive lead-like characteristics. These are highly differentiated from other known NLRP3 inhibitors and offer scope for further optimisation. 

Bioisosteric approach to novel NLRP3 inflammasome inhibitors

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.