Catarzi, Daniela; Varano, Flavia; Vigiani, Erica; Calenda, Sara; Melani, Fabrizio; Varani, Katia; Vincenzi, Fabrizio; Pasquini, Silvia; Mennini, Natascia; Nerli, Giulia; Dal Ben, Diego; Volpini, Rosaria; Colotta, Vittoria published an article in 2022. The article was titled ã?-Heteroaryl Substituted Amino-3,5-Dicyanopyridines as New Adenosine Receptor Ligands: Novel Insights on Structure-Activity Relationships and Perspectivesã? and you may find the article in Pharmaceuticals.Application of 16982-21-1 The information in the text is summarized as follows:
A new set of amino-3,5-dicyanopyridines I [R = [(1H-imidazol-2-yl)methyl]sulfanyl, [(1H-imidazol-2-yl)methyl]amino, etc.; R1 = amino, pyrroldino, cyclopentylamino, etc.; R2 = 2-furyl, Ph, etc] was synthesized and biol. evaluated at the adenosine receptors (ARs). This chem. class was particularly versatile, as small structural modifications was influence not only affinity and selectivity, but also the pharmacol. profile. Thus, in order to deepen the structure-activity relationships (SARs) of this series, different substituents were evaluated at the diverse positions on the dicyanopyridine scaffold I. In general, the herein reported compounds show nanomolar binding affinity and interact better with both the human (h) A1 and A2A ARs than with the other subtypes. Docking studies at hAR structure were performed to rationalize the observed affinity data. Of interest are compounds I [R1 = amino, R2 = 2-furyl, 2-thiophenyl; R = [(1H-imidazol-2-yl)methyl]sulfanyl], which was considered as pan ligands as binding all the ARs with comparable nanomolar binding affinity (A1AR: 1, Ki = 9.63 nM; 5, Ki = 2.50 nM; A2AAR: 1, Ki = 21 nM; 5, Ki = 24 nM; A3AR: 1, Ki = 52 nM; 5, Ki = 25 nM; A2BAR: 1, EC50 = 1.4 nM; 5, EC50 = 1.12 nM). Moreover, these compounds I showed a partial agonist profile at all the ARs. This combined AR partial agonist activity could lead us to hypothesize a potential effect in the repair process of damaged tissue that would be beneficial in both wound healing and remodeling. In addition to this study using Ethyl 2-amino-2-thioxoacetate, there are many other studies that have used Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Application of 16982-21-1) was used in this study.
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Application of 16982-21-1
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