In 2017,Okawa, Tomohiro; Aramaki, Yoshio; Yamamoto, Mitsuo; Kobayashi, Toshitake; Fukumoto, Shoji; Toyoda, Yukio; Henta, Tsutomu; Hata, Akito; Ikeda, Shota; Kaneko, Manami; Hoffman, Isaac D.; Sang, Bi-Ching; Zou, Hua; Kawamoto, Tetsuji published 《Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure》.Journal of Medicinal Chemistry published the findings.HPLC of Formula: 16982-21-1 The information in the text is summarized as follows:
A novel class of therapeutic drug candidates for heart failure, highly potent and selective GRK2 inhibitors, exhibit potentiation of β-adrenergic signaling in vitro studies. Hydrazone derivative and 1,2,4-triazole derivative were identified as hit compounds by HTS. New scaffold generation and SAR studies of all parts resulted in a 4-methyl-1,2,4-triazole derivative with an N-benzylcarboxamide moiety with highly potent activity towards GRK2, and selectivity over other kinases. In terms of subtype selectivity, these compounds showed enough selectivity against GRK1, 5, 6, 7 with almost equipotent inhibition to GRK3. The medicinal chem. efforts led to the discovery of I (GRK2 IC50 = 18 nM) which was obtained the cocrystal structure with human GRK2 and an inhibitor of GRK2 that potentiates β-adrenergic receptor (βAR)-mediated cAMP accumulation and prevents internalization of βARs in β2AR-expressing HEK293 cells treated with isoproterenol. Therefore, I appears to be a novel class of therapeutic for heart failure treatment. In the experimental materials used by the author, we found Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1HPLC of Formula: 16982-21-1)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.HPLC of Formula: 16982-21-1
Referemce:
Ester – Wikipedia,
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