6265-74-3Relevant articles and documents
Synthesis of Functionalized Pyridines via a Regioselective Oxazoline Promoted C-H Amidation Reaction
Maiden, Tracy M. M.,Swanson, Stephen,Procopiou, Panayiotis A.,Harrity, Joseph P. A.
supporting information, p. 3434 - 3437 (2016/07/26)
The first Rh-catalyzed C-H amidation of pyridines is reported. The incorporation of a substituent at the C2 position both is crucial to the success of this transformation and provides considerable scope for further elaboration of the resulting products. Among these compounds, 2-chloropyridines allow access to a selection of intermediates including a versatile azaquinazoline scaffold.
Study of synthesis and cardiovascular activity of some furoxan derivatives as potential NO-donors
Mu, Li,Feng, Si-Shen,Go, Mei Lin
, p. 808 - 816 (2007/10/03)
A series of hybrid molecules incorporating the furoxan and nicorandil moieties were designed as potential NO donors with cardiovascular and cerebrovascular activities. Thirty-six target molecules were successfully synthesized by conventional methods and characterized by infrared spectroscopy, 1H-NMR spectroscopy and high resolution mass spectra. The compounds were tested for their effects on KCl-induced contraction of rabbit thoracic aorta whose endothelium was denuded. Eight compounds were found to reduce KCl-induced contraction by more than 30% at 10 μM. All except one of these compounds are characterized by the presence of electron withdrawing groups in the phenyl ring attached via an amide or ester linkage to the furoxan moiety. The nature of the terminal carbonyl linkage (ester or amide) and the length or type of the alkyl chain bridging the two carbonyl functions have little effect on the activity. One of the active compounds, N-(4- methoxy-benzoyl)-N'-[3-methylfuroxanyl-4-carbonyl)piperazine (17i) was tested for hypotensive effects on anaesthetized rats at 1.5 mg/kg, and found to demonstrate a gradual and sustained hypotensive effect. The results suggest that the furoxannicorandil derivatives are a useful lead in the design of NO- donor compounds for hypertension.
Use of N-acyl derivatives of aminoalcohols for the manufacture of a medicament for the treatment of pathologies involving mast cells
-
, (2008/06/13)
N-acyl-derivatives of amino alcohols suitable for the therapeutic treatment of pathologies characterized by degranulation of mast cells caused by a neurogen and/or immunogenic hyperstimulation.