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Structural features and functional activities of benzimidazoles as NOD2 antagonists.

Abstract：

:NOD1 and NOD2 are pattern recognition receptors that have important roles in innate immune responses. Although their overactivation has been linked to a number of diseases, NOD2 in particular remains a virtually unexploited target in this respect, with only one structural class of antagonist reported. To gain insight into the structure-activity relationships of NOD2 antagonists, a series of novel analogs was designed and synthesized, and then screened for antagonist activity versus NOD2, and counter-screened versus NOD1. Compounds 32 and 38 were identified as potent and moderately selective NOD2 antagonists, and 33 and 42 as dual NOD1/NOD2 antagonists, with balanced activities against both targets in the low micromolar range. These data enable in-depth exploration of their structure-activity relationships and provide deeper understanding of the structural features required for NOD2 antagonism.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Guzelj S,Gobec M,Urbančič D,Mlinarič-Raščan I,Corsini E,Jakopin Ž

doi

10.1016/j.ejmech.2020.112089

subject

Has Abstract

pub_date

2020-03-15 00:00:00

pages

112089

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(20)30056-8

journal_volume

190

pub_type

杂志文章

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