Article
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.
Bioorganic & medicinal chemistry - 15 Feb 2018
Degorce Sébastien L, Anjum Rana, Dillman Keith S, Drew Lisa, Groombridge Sam D, Halsall Christopher T, Lenz Eva M, Lindsay Nicola A, Mayo Michele F, Pink Jennifer H, Robb Graeme R, Scott James S, Stokes Stephen, Xue Yafeng
Abstract excerpt
We have developed a series of orally efficacious IRAK4 inhibitors, based on a scaffold hopping strategy and using rational structure based design. Efforts to tackle low permeability and high efflux in our previously reported pyrrolopyrimidine series (Scott et al., 2017) led to the identification of pyrrolotriazines which contained one less formal hydrogen bond donor and were intrinsically more lipophilic. Further...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.