In 2022,Awalt, Jon Kyle; Nguyen, Anh T. N.; Fyfe, Tim J.; Thai, Bui San; White, Paul J.; Christopoulos, Arthur; Jorg, Manuela; May, Lauren T.; Scammells, Peter J. published an article in Journal of Medicinal Chemistry. The title of the article was 《Examining the Role of the Linker in Bitopic N6-Substituted Adenosine Derivatives Acting as Biased Adenosine A1 Receptor Agonists》.Synthetic Route of C6H15NO The author mentioned the following in the article:
The adenosine A1 receptor is a therapeutic target based on its ability to provide cardioprotection during episodes of myocardial ischemia and reperfusion injury. However, the clin. translation of A1R agonists has been hindered by dose-limiting adverse effects (bradycardia and hypotension). Previously, we demonstrated that the bitopic agonist VCP746 (1), consisting of an adenosine pharmacophore linked to an allosteric moiety, can stimulate cardioprotective A1R signaling effects in the absence of unwanted bradycardia. This study maps the structure-activity relationships of 1 through modifications to the linker moiety. Derivatives differing in the flexibility, length, and nature of the linker were assessed, which revealed that the linker is tolerant of several modifications including added rigidity. Ligands featuring 1,4-disubstituted 1,2,3-triazoles were the most biased of the novel analogs but also displayed sub-nanomolar potency in a cAMP accumulation assay at the A2BR. To our knowledge, 10 is the most potent A2BR agonist published to date. In the experimental materials used by the author, we found 6-Aminohexan-1-ol(cas: 4048-33-3Synthetic Route of C6H15NO)
6-Aminohexan-1-ol(cas: 4048-33-3) may be used along with glutaric acid to generate poly(ester amide)s with excellent film- and fiber forming properties. It can undergo cyclization over copper supported on γ-alumina and magnesia to form hexahydro-1H-azepine.Synthetic Route of C6H15NO
Referemce:
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Alcohols – Chemistry LibreTexts