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Structural features and functional activities of benzimidazoles as NOD2 antagonistsGuzelj, Samo ...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.Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 190, Mar. 2020, str. 1-15)Type of material - article, component partPublish date - 2020Language - englishCOBISS.SI-ID - 4874097
Author
Guzelj, Samo |
Gobec, Martina, 1983- |
Urbančič, Dunja, farmacevtka |
Mlinarič-Raščan, Irena |
Corsini, Emanuela, pharmacist |
Jakopin, Žiga
Topics
Citokini |
Imunski odziv |
Farmacevtska kemija |
Receptorji (medicina) |
NOD2 antagonist |
NOD1 antagonist |
NF-kB activationImmunomodulation |
Interleukin-8Tumor |
necrosis factor-[alpha]
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Author | Guzelj, Samo ... |
Title | Structural features and functional activities of benzimidazoles as NOD2 antagonists |
Publication date | 2020-03-29 |
COBISS.SI-ID | 4874097 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
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Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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Database name | Field | Year |
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Guzelj, Samo | 52379 |
Gobec, Martina, 1983- | 32034 |
Urbančič, Dunja, farmacevtka | 34512 |
Mlinarič-Raščan, Irena | 12443 |
Corsini, Emanuela, pharmacist | ![]() |
Jakopin, Žiga | 26496 |
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