Bollenbach, Maud; Nemska, Simona; Wagner, Patrick; Camelin, Guillaume; Daubeuf, Francois; Obrecht, Adeline; Villa, Pascal; Rognan, Didier; Bihel, Frederic; Bourguignon, Jean-Jacques; Schmitt, Martine; Frossard, Nelly published an article in 2021, the title of the article was Design, synthesis and biological evaluation of arylpyridin-2-yl guanidine derivatives and cyclic mimetics as novel MSK1 inhibitors. An application in an asthma model.Category: imidazoles-derivatives And the article contains the following content:
In order to identify new MSK1 inhibitors, a screening of a library of low mol. weight compounds was performed, and the results highlighted the I [R = phenyl] ( IC50~18μM) as a starting hit for structure-activity relationship study. Derivatives, homologues and rigid mimetics of I [R = Ph, 2-furanyl, 3-pyridine, etc.] were designed, and all synthesized compounds were evaluated for their inhibitory activity towards MSK1. Among them, the non-cytotoxic 2-aminobenzimidazole was the most potent at inhibiting significantly: (i) MSK1 activity, (ii) the release of IL-6 in inflammatory conditions in vitro (IC50~2μM) and (iii) the inflammatory cell recruitment to the airways in a mouse model of asthma. The experimental process involved the reaction of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one(cas: 40644-16-4).Category: imidazoles-derivatives
The Article related to arylpyridinyl guanidine preparation msk1 inhibitor antiasthmatic cytotoxicity sar, msk1, pyridine-2-yl guanidine, asthma, inflammation, kinase inhibitors, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Category: imidazoles-derivatives
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem