- Synthesis of Dicyanovinyl-Substituted 1-(2-Pyridyl)pyrazoles: Design of a Fluorescent Chemosensor for Selective Recognition of Cyanide
-
A fluorescence "turn-off" probe has been designed and successfully applied to detect cyanide (CN-) based on a Michael-type nucleophilic addition reaction and intramolecular charge transfer (ICT) mechanism. For this research, a family of 3-aryl-
- Orrego-Hernández, Jessica,Portilla, Jaime
-
p. 13376 - 13385
(2017/12/15)
-
- Bidentate Directing-Enabled, Traceless Heterocycle Synthesis: Cobalt-Catalyzed Access to Isoquinolines
-
Traceless heterocycle synthesis based on transition-metal-catalyzed C-H functionalization is synthetically appealing but has been realized only in monodentate directing systems. Bidentate directing systems allow for the achievement of high catalytic reactivity without the need for a high-cost privileged ligand. The first bidentate directing-enabled, traceless heterocycle synthesis is demonstrated in the cobalt-catalyzed synthesis of isoquinolines via 2-hydrazinylpyridine-directed C-H coupling/cyclization with alkynes. Convenient directing group installation through a ubiquitously present ketone group allows synthetic elaboration for complex molecules.
- Zhou, Shuguang,Wang, Mingyang,Wang, Lili,Chen, Kehao,Wang, Jinhu,Song, Chao,Zhu, Jin
-
supporting information
p. 5632 - 5635
(2016/11/17)
-
- Synthesis and evaluation of analgesic, antiinflammatory and antiplatelet properties of new 2-pyridylarylhydrazone derivatives
-
This work describes recent results from our research program aiming at the synthesis and pharmacological evaluation of new compounds acting as antiinflammatory, analgesic and platelet antiaggregatory. In this paper the synthesis and the pharmacological profile as analgesic, antiinflammatory and anti-platelet of new functionalized 2-pyridylarylhydrazone derivatives 5a-r are discussed. This class of N-heterocyclic derivatives represents a new series of prototype candidates with analgesic and antiinflammatory properties possessing also an important anti-aggregating activity. The pharmacological results herein disclosed suggest that the anti-inflammatory and analgesic activities of these new pyridynehydrazone derivatives observed in the carrageenan pleurisy model and acetic acid writhing test, respectively, is probably due to an interference on the arachidonic acid (AA) metabolism. The most important antiinflammatory derivative 2-(2-formylfurane)pyridylhydrazone 5p presented a 79% inhibition of pleurisy at a dose of 80.1 μmol/kg. We also described the results concerning the mechanism of action of this series of N-heterocyclic derivatives in platelet aggregation which suggest a Ca2+ participation, probably by a complexation scavenger mechanism. Compound 2-(2-formylfurane)pyridylhydrazone 5p was able to complex Ca2+ in in vitro experiments at 100 μM concentration, indicating that this series of compounds can act as Ca2+ scavenger depending on the nature of the aryl moiety present at the imine subunit.
- Todeschini, Adriane R.,De Miranda, Ana Luisa P.,Da Silva, Kelly Christine M.,Parrini, Sergio C.,Barreiro, Eliezer J.
-
p. 189 - 199
(2007/10/03)
-
- Inhibiteurs mixtes des voies de la cyclooxygenase et des lipoxygenases: synthese et activite de derives hydrazoniques
-
Dual inhibitors of the cyclooxygenase and lipoxygenase pathways: synthesis and activity of hydrazone derivatives.Non-steroidal anti-inflammatory drugs (NSAIDs) act by preventing prostaglandin production.In recent years, research on non-steroid dual inhibitors of prostaglandin and leukotriene biosyntheses has been developed.These compounds should represent a new class of anti-inflammatory drugs, with a wider spectrum of activity than classical NSAIDs.The present paper reports the synthesis of hydrazone derivatives.The effect of various substitutions is studied on platelet cyclooxygenase (i.e. prostaglandin synthesis) and on leukocyte 5-lipoxygenase (i.e. leukotriene synthesis).Among the 50 tested compounds, 2 hydrazone derivatives were selected for their significant dual inhibitory potency: 2-acetylthiophene-2-thiazolylhydrazone 5g, and N-phenyl benzimidrazone 6c.Keywords - non-steroidal anti-inflammatory drugs / hydrazones / dual inhibitor / cyclooxygenase / lipoxygenase
- Ghiglieri-Bertez, Chantal,Coquelet, Claude,Alazet, Alain,Bonne, Claude
-
p. 147 - 152
(2007/10/02)
-