Regioselective Synthesis of Pyrazolyl-pyrimidine Hybrids of Pharmacological Interest

Synthesis DOI: 10.1055/s-0040-1707948 The regioselective synthesis of twenty novel [3-substituted 5-hydroxy-5-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-1-yl][6-aryl-(2-methylthio)pyrimidin-4-yl]methanones from the cyclocondensation reactions of new 6-aryl-2-(methylthio)pyrimidine-4-carbohydrazides with 4-substituted 1,1,1-trifluorobut-3-en-2-ones is reported. Human acetylcholinesterase (HsAChE) and butyrylcholinesterase (HsBChE) inhibition tests were performed on selected products in order to explore the possible pharmacological applications of these compounds. Two compounds showed significant and selective inhibitory activity for BChE. [...] © Georg Thieme Verlag Stuttgart · New YorkArticle in Thieme eJournals: Table of contents  |  Abstract  |  Full text

Source: Synthesis - May 11, 2020 Category: Chemistry Authors: Camargo, Adriano F. Marangoni, M ário A. de Moraes, Paulo A. Nogara, Pablo A. Afolabi, Blessing A. Bencke, Carlos E. Rocha, Jo ão B. T. Bonacorso, Helio G. Martins, Marcos A. P. Zanatta, Nilo Tags: paper Source Type: research