Search results for "Pyrazole"
showing 10 items of 315 documents
CCDC 156982: Experimental Crystal Structure Determination
2002
Related Article: S.Kiviniemi, M.Nissinen, T.Alaviuhkola, K.Rissanen, J.Pursiainen|2001|J.Chem.Soc.,Perkin Trans.2||2364|doi:10.1039/b100775k
A new pyrazolo pyrimidine derivative inhibitor of cyclooxygenase-2 with anti-angiogenic activity
2003
In a previous study, we reported a new pyrazolo pyrimidine derivative, N(4)-benzyl-N(6),N(6)-dimethyl-1-1(tert-butyl)-1H-pyrazolo[3,4-d]pyrimidine-6,4-diamine (DPP), which inhibited potently cyclooxygenase-2 activity in intact cell assays with minor activity against cyclooxygenase-1 (IC(50)=0.9 nM for cyclooxygenase-2 versus IC(50)=59.6 nM for cyclooxygenase-1). In the present work, this behaviour was confirmed in vivo by using the 24-h zymosan-injected mouse air pouch model (ID(50)=1.36 nM/pouch for prostaglandin E(2) level). We also studied the possible beneficial effect of DPP in the angiogenesis-dependent murine air pouch granuloma and rat paw carrageenan-induced hyperalgesia models. DP…
New reaction of 1H-pyrazoles with selenium dioxide: one-pot synthesis of bis(1H-pyrazol-4-yl)selenides
2010
Abstract A novel reaction between 3- and 3,5-substituted pyrazoles with selenium dioxide proceeds with formation of bis(3R,5R′-1H-pyrazol-4-yl)selenides in high yield. On this basis, an efficient one-pot synthetic procedure has been developed. In the case of the unsubstituted pyrazole a selenonium compound has been obtained. The identity and structure of the isolated selenium derivatives have been confirmed by spectral methods and their molecular structures investigated by X-ray analysis.
Non-Classical Transformation of Benzendiazonium Hydrogen Sulfates. Access to 1,3-Dimethylisochromeno[4,3-c]pyrazol-5(1H)-one, a Potential Benzodiazep…
2013
The compound 2-((1,3-dimethyl-1H-pyrazol-5-yl)(methyl)carbamoyl)benzene-diazonium hydrogen sulfate (10) was reacted with copper sulfate and sodium chloride, in the presence of ascorbic acid as reducing agent, to afford a mixture of the chlorinated epimers 4′-chloro-2,2′,5′-trimethyl-2′,4′-dihydrospiro[isoindoline-1,3′-pyrazol]-3-one (18) and (19), the epimers 4′-hydroxy-2,2′,5′-trimethyl-2′,4′-dihydrospiro[isoindoline-1,3′-pyrazol]-3-one (20) and (21), and N-(1,3-dimethyl-1H-pyrazol-5-yl)benzamide (22). Under the foregoing conditions, diazonium salt 10 affords neither the 2-chloro-N-(1,3-dimethyl-1H-pyrazol-5-yl)-N-methylbenzamide (23) nor the tricyclic derivative 24, the classical products…
Regio- and stereoselective synthesis of spiro-heterocycles bearing the pyrazole scaffold via [3+2] cycloaddition reaction
2022
Abstract Herein we reported the utility of one-pot multicomponent based [3+2] cycloaddition reaction transformation to prepare a new two hybrids of spirooxindoles engrafted with pyrazole skeleton. Upon treatment of the electron-deficient olefins based pyrazole motif with in situ the generated azomethine ylides (AY) of sarcosine with the 6-chloro-isatin afforded spiroadducts. To enlighten the regio- and diastereo-selectivity of these spiroheterocycles, single crystal X-ray diffraction analysis was presented. Using Hirshfeld calculations, many short distance contacts such as O…H, Cl…H, N…H, H…C, C…C and Cl…S have a great impact on the molecular packing and the crystal stability of 8a and 8b. …
Raloxifene increases the capacity of serum to promote prostacyclin release in human endothelial cells: implication of COX-1 and COX-2.
2004
OBJECTIVE Prostacyclin is a potent vasodilator synthesized by two isoforms of cyclooxygenase in endothelium. The aim of this study was to investigate the effect of serum from postmenopausal women treated with raloxifene on prostacyclin production by human umbilical vein endothelial cells and on cyclooxygenases-1 and -2. DESIGN Serum was collected from 21 women receiving 60 mg/day of raloxifene, at baseline and at 3 and 6 months. Human umbilical vein endothelial cells were exposed to serum for 24 hours, and prostacyclin production was evaluated in supernatants. Selective inhibitors of cyclooxygenases-1 and -2 (SC-560 and NS-398) were used to investigate the relative contribution of each enzy…
CCDC 1471982: Experimental Crystal Structure Determination
2016
Related Article: Izabela Gryca, Joanna Palion-Gazda, Barbara Machura, Mateusz Penkala, Francesc Lloret and Miguel Julve|2016|Eur.J.Inorg.Chem.||5418|doi:10.1002/ejic.201601004
CCDC 1536511: Experimental Crystal Structure Determination
2017
Related Article: Santiago Matías Ruatta, Marcelo César Murguía, Carmen Ramírez de Arellano, Santos Fustero|2017|Tetrahedron Lett.|58|2441|doi:10.1016/j.tetlet.2017.05.029
CCDC 2102639: Experimental Crystal Structure Determination
2021
Related Article: Mohammad Shahidul Islam, Matti Haukka, Saied M. Soliman, Abdullah Mohammed Al-Majid, A.F.M.Motiur Rahman, Ahmed Bari, Assem Barakat|2022|J.Mol.Struct.|1250|131711|doi:10.1016/j.molstruc.2021.131711
CCDC 2102638: Experimental Crystal Structure Determination
2021
Related Article: Mohammad Shahidul Islam, Matti Haukka, Saied M. Soliman, Abdullah Mohammed Al-Majid, A.F.M.Motiur Rahman, Ahmed Bari, Assem Barakat|2022|J.Mol.Struct.|1250|131711|doi:10.1016/j.molstruc.2021.131711