Narayanan, Sanju’s team published research in Bioorganic & Medicinal Chemistry in 2016 | CAS: 56602-33-6

((1H-Benzo[d][1,2,3]triazol-1-yl)oxy)tris(dimethylamino)phosphonium hexafluorophosphate(V)(cas: 56602-33-6) is a peptide coupling reagent. Can be used in the preparation of phenyl esters of amino acids which have been shown to be valuable as blocked derivatives of amino acids in the field of peptide synthesis.Category: triazoles

In 2016,Narayanan, Sanju; Maitra, Rangan; Deschamps, Jeffery R.; Bortoff, Katherine; Thomas, James B.; Zhang, Yanyan; Warner, Keith; Vasukuttan, Vineetha; Decker, Ann; Runyon, Scott P. published 《Discovery of a novel small molecule agonist scaffold for the APJ receptor》.Bioorganic & Medicinal Chemistry published the findings.Category: triazoles The information in the text is summarized as follows:

The apelinergic system includes a series of endogenous peptides apelin, ELABELA/TODDLER and their 7-transmembrane G-protein coupled apelin receptor (APJ, AGTRL-1, APLNR). The APJ receptor is an attractive therapeutic target because of its involvement in cardiovascular diseases and potentially other disorders including liver fibrosis, obesity, diabetes, and neuroprotection. To date, pharmacol. characterization of the APJ receptor has been limited due to the lack of small mol. functional agonists or antagonists. Through focused screening we identified a drug-like small mol. agonist hit 1 with a functional EC50 value of 21.5 ± 5 μM and binding affinity (Ki) of 5.2 ± 0.5 μM. Initial structure-activity studies afforded compound 22 having a 27-fold enhancement in potency and the first sub-micromolar full agonist with an EC50 value of 800 ± 0.1 nM and Ki of 1.3 ± 0.3 μM. Preliminary SAR, synthetic methodol., and in vitro pharmacol. characterization indicate this scaffold will serve as a favorable starting point for further refinement of APJ potency and selectivity. The experimental part of the paper was very detailed, including the reaction process of ((1H-Benzo[d][1,2,3]triazol-1-yl)oxy)tris(dimethylamino)phosphonium hexafluorophosphate(V)(cas: 56602-33-6Category: triazoles)

((1H-Benzo[d][1,2,3]triazol-1-yl)oxy)tris(dimethylamino)phosphonium hexafluorophosphate(V)(cas: 56602-33-6) is a peptide coupling reagent. Can be used in the preparation of phenyl esters of amino acids which have been shown to be valuable as blocked derivatives of amino acids in the field of peptide synthesis.Category: triazoles

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics