7517-19-3Relevant articles and documents
Colorimetric analysis of painting materials using polymer-supported polydiacetylene films
Trachtenberg, Alexander,Malka, Orit,Kootery, Kaviya Parambath,Beglaryan, Stella,Malferrari, Danilo,Galletti, Paola,Prati, Silvia,Mazzeo, Rocco,Tagliavini, Emilio,Jelinek, Raz
, p. 9054 - 9059 (2016)
Analysis of artworks and identification of their molecular components are of utmost importance for selecting proper conservation strategies and monitoring restoration. Accordingly, development of simple and readily applicable paint analysis assays is high
Cathepsin K inhibitors based on 2-amino-1,3,4-oxadiazole derivatives
Gontijo, Talita B.,Lima, Patrícia S.,Icimoto, Marcelo Y.,Neves, Raquel Le?o,de Alvarenga, érika C.,Carmona, Adriana K.,de Castro, Alexandre A.,Ramalho, Teodorico C.,da Silva Júnior, Eufranio N.,de Freitas, Rossimiriam P.
, (2021/02/26)
Two new series of hitherto unknown dipeptides, containing an electrophilic nitrile or a non-electrophilic 2-amino-1,3,4-oxadiazole moiety were synthesized and evaluated in vitro as Cathepsin K (Cat K) inhibitors. From 14 compounds obtained, the oxadiazole derivatives 10a, 10b, 10e, and 10g acted as enzymatic competitive inhibitors with Ki values between 2.13 and 7.33 μM. Molecular docking calculations were carried out and demonstrated that all inhibitors performed hydrogen bonds with residues from the enzyme active site, such as Asn18. The best inhibitors (10a, 10b, 10g) could also perform these bonds with Cys25, and 10a showed the most stabilizing interaction energy (?134.36 kcal mol?1) with the active cavity. For the first time, derivatives based in 2-amino-1,3,4-oxadiazole scaffolds were evaluated, and the results suggested that this core displays a remarkable potential as a building block for Cat K inhibitors.
One-pot synthesis of 1,2,4-oxadiazoles from chalcogen amino acid derivatives under microwave irradiation
Wolf, Lucas,Mayer, Jo?o C.P.,Quoos, Natália,Sauer, André C.,Schwab, Ricardo S.,Rodrigues, Oscar E.D.,Dornelles, Luciano
supporting information, (2021/06/06)
A series of sulfur- and selenium-bearing, amino acid-derived 1,2,4-oxadiazoles were obtained by a simple procedure. The method consists of EDC-promoted coupling of chalcogen amino acid derivatives with arylamidoximes in acetone, followed by solvent removal and microwave irradiation in water medium. Influence of amidoxime substituents, of the chalcogen atom and of the amino acid side chain is discussed. The results showed this to be a fast, easy and effective method to obtain these compounds, with good functional-group tolerance, potentially favouring future applications in organic synthesis.
