Discovery, synthesis and characterization of a series of (1-alkyl-3-methyl-1H-pyrazol-5-yl)-2-(5-aryl-2H-tetrazol-2-yl)acetamides as novel GIRK1/2 potassium channel activators was written by Sharma, Swagat;Kozek, Krystian A.;Abney, Kristopher K.;Kumar, Sushil;Gautam, Nagsen;Alnouti, Yazen;David Weaver, C.;Hopkins, Corey R.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2019.Category: pyridine-derivatives This article mentions the following:
The study described the discovery and characterization of a series of 5-aryl-2H-tetrazol-3-yl acetamides as G protein-gated inwardly-rectifying potassium (GIRK) channels activators. Working from an initial hit discovered during a high-throughput screening campaign, a tetrazole scaffold was identified that shifts away from the previously reported urea-based scaffolds while remaining effective GIRK1/2 channel activators. In addition, the compounds were evaluated in Tier 1 DMPK assays and identified a (3-methyl-1H-pyrazol-1-yl)tetrahydrothiophene-1,1-dioxide head group that imparts interesting and unexpected microsomal stability compared to previously-reported pyrazole head groups. In the experiment, the researchers used many compounds, for example, 2-Fluoroisonicotinonitrile (cas: 3939-14-8Category: pyridine-derivatives).
2-Fluoroisonicotinonitrile (cas: 3939-14-8) belongs to pyridine derivatives. Pyridine has a dipole moment and a weaker resonant stabilization than benzene (resonance energy 117 kJ·mol−1 in pyridine vs. 150 kJ·mol−1 in benzene). Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one C–H in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.Category: pyridine-derivatives