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Discovery of Novel Small Molecule Dual Inhibitors Targeting Toll-Like Receptors 7 and 8.

Abstract：

:Endosomal toll-like receptors (TLRs) 7 and 8 recognize viral single-stranded RNAs, a class of imidazoquinoline compounds, 8-oxo-adenosines, 8-aminobenzodiazepines, pyrimidines, and guanosine analogues. Substantial evidence is present linking chronic inflammation mediated specifically by TLR7 to the progression of autoimmunity. We identified a new TLR7/8 dual inhibitor (1) and a TLR8-specific inhibitor (2) based on our previous screen targeting TLR8. Compound 1, bearing a benzanilide scaffold, was found to inhibit TLR7 and TLR8 at low micromolar concentrations. We envisioned making modifications on the benzanilide scaffold of 1 resulting in a class of highly specific TLR7 inhibitors. Our efforts led to the discovery of a new TLR8 inhibitor (CU-115) and identification of a TLR7/8 dual inhibitor (CU-72), bearing a distinct diphenyl ether skeleton, with potential for TLR7 selectivity optimization. Given the role of TLR8 in autoimmunity, we also optimized the potency of 2 and developed a new TLR8 inhibitor bearing a 1,3,4-oxadiazole motif.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Padilla-Salinas R,Anderson R,Sakaniwa K,Zhang S,Nordeen P,Lu C,Shimizu T,Yin H

doi

10.1021/acs.jmedchem.9b01201

subject

Has Abstract

pub_date

2019-11-27 00:00:00

pages

10221-10244

issue

22

eissn

0022-2623

issn

1520-4804

journal_volume

62

pub_type

杂志文章

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