Electric Literature of C8H8N2OOn June 1, 2020, Sekioka, Ryuichi; Honda, Shugo; Akashiba, Hiroki; Yarimizu, Junko; Mitani, Yasuyuki; Yamasaki, Shingo published an article in Bioorganic & Medicinal Chemistry. The article was 《Optimization and biological evaluation of imidazopyridine derivatives as a novel scaffold for γ-secretase modulators with oral efficacy against cognitive deficits in Alzheimer′s disease model mice》. The article mentions the following:
Gamma-secretase modulators (GSMs) selectively lower amyloid-β42 (Aβ42) and are therefore potential disease-modifying drugs for Alzheimer′s disease (AD). Here, we report the discovery of imidazopyridine derivatives as GSMs with oral activity on not only Aβ42 levels but also cognitive function. Structural optimization of the biphenyl group and pyridine-2-amide moiety of compound 1a greatly improved GSM activity and rat microsomal stability, resp. 5-{8-[(3,4′-Difluoro[1,1′-biphenyl]-4-yl)methoxy]-2-methylimidazo[1,2-a]pyridin-3-yl}-N-methylpyridine-2-carboxamide (1o)(I) showed high in vitro potency and brain exposure, induced a robust reduction in brain Aβ42 levels, and exhibited undetectable inhibition of cytochrome P 450 enzymes. Moreover, compound 1o showed excellent efficacy against cognitive deficits in AD model mice. These findings suggest that compound 1o is a promising candidate for AD therapeutics. The results came from multiple reactions, including the reaction of 2-Methylimidazo[1,2-a]pyridin-8-ol(cas: 79707-11-2Electric Literature of C8H8N2O)
2-Methylimidazo[1,2-a]pyridin-8-ol(cas: 79707-11-2) belongs to imidazoles.Imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies.
Electric Literature of C8H8N2O However, the application of imidazoles is not limited to the field of peptides and peptidomimetics.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem