ChemInform Abstract: N‐3‐Substituted Pyrimidinones as Potent, Orally Active, AT1 Selective Angiotensin II Receptor Antagonists.

Abstract

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Vasoactive Thiomethyl-Pyrimidines: Promising Drug Candidates with Vascular Activity

“…1,4 It can be observed that Prazosin, Terazosin and Doxazosin have a pyrimidine ring in their chemical structures. 4 In fact, pyrimidines and their oxo-derivatives are described in the literature as presenting a wide array of biological activities such as antitumor, 6,7 interferon inducer, 8 antiviral, 9 anti-hipertensive, 10 hypoglycemic, 11 anticonvulsant, 12 antinociceptive, 13,14 and anti-inflammatory. 15 Pyrimidine or pyrimidinone rings can be synthesized in several ways.…”

“…This whole process may take two days of laboratory work for the preparation of one product. [9][10][11]14,18 These findings encouraged us to search new ways to perform these reactions and to evaluate the biological activity of these heterocyclic derivatives.…”

Synthesis of 2-(Arylselanyl)benzo[b]chalcogenophenes via Intramolecular Cyclization of Vinyl Selenides

“…Sartans are a new class of antihypertensive drugs acting as Ang II receptor antagonists. Examples of thiophene-containing sartan derivatives are milfasartan (E), which has reached the phase I of clinical trials, 8 and eprosartan (F), marketed in some countries under the tradename Teveten ® , used in the treatment of arterial hypertension (…”

Microwave-Assisted Copper-Powder-Catalyzed Synthesis of Pyrimidinones from β-Bromo α,β-Unsaturated Carboxylic Acids and Amidines

“…[1][2][3][4][5][6][7] Fu and co-workers have shown that 2-bromocycloalk-1-enecarboxylic acids couple and cyclize with amidine hydrochlorides in the presence of copper(I) iodide to give bicyclic pyrimidinones. 8 A similar coupling and cyclization of 2-bromocyclohex-1-enecarboxylic acid with amidine hydrochlorides to give bicyclic pyrimidinones can be induced by a magnetite (Fe 3 O 4 ) nanoparticlesupported copper(I) catalyst.…”

“…Because the pyrimidinone ring plays an important role as a basic scaffold component in numerous biologically active compounds, many pyrimidinone-containing compounds have been synthesized and tested for biological activity. [1][2][3][4][5][6][7] Fu and co-workers have shown that 2-bromocycloalk-1-enecarboxylic acids couple and cyclize with amidine hydrochlorides in the presence of copper(I) iodide to give bicyclic pyrimidinones. 8 A similar coupling and cyclization of 2-bromocyclohex-1-enecarboxylic acid with amidine hydrochlorides to give bicyclic pyrimidinones can be induced by a magnetite (Fe 3 O 4 ) nanoparticlesupported copper(I) catalyst.…”