Search results for "Pyrazole"
showing 10 items of 315 documents
New 2-Methoxy Acetylenic Acids and Pyrazole Alkaloids from the Marine Sponge Cinachyrella sp.
2017
Three new 2-methoxy acetylenic acids (1–3) and a known derivative (4), in addition to three new natural pyrazole alkaloids (5–7) were isolated from an Indonesian marine sponge of the genus Cinachyrella. Compounds 5 and 6 have previously been reported as synthetic compounds. The structures of the new compounds were established on the basis of one- and two-dimensional NMR spectroscopy as well as by mass spectrometric data. The absolute configuration of the new acetylenic acid derivatives (1–3) was established by ECD spectroscopy. All isolated compounds were evaluated for their cytotoxicity against L5178Y mouse lymphoma cells. Compounds 1–4 exhibited strong activity with an IC50 value of 0.3 µ…
From isolated 1H-pyrazole cryptand anion receptors to hybrid inorganic-organic 1D helical polymeric anion receptors
2015
We report a novel 1-D helical coordination polymer formed by protonated polyamine 1H-pyrazole cryptands interconnected by Cu2+ metal ions that are able to encapsulate anionic species behaving as a multianion receptor. Switching from a monomeric receptor to a polymeric receptor is activated by metal ions and pH.
Synthesis of alkyl-5,8-dimethyl-6-phenyl-5,6-dihydropyrazolo[3,4-f] [1,2,3,5]tetrazepin-4(3H)-ones of pharmaceutical interest
2006
The multistep synthesis of two pyrazolo[3,4-f][1,2,3,5]tetrazepin-4(3H)-one derivatives, a new class of fused 1,2,3,5-tetrazepinones with potential antiproliferative activity, has been carried out. Owing to the instability of the above compounds, the last step of the synthesis was performed at -5/0 degrees C. The obtained tetrazepinones, when allowed to stand at r.t. for 24 h, afforded quantitatively 1-phenyl-3,6-dimethylpyrazolo [3,4-d][1,2,3] triazole.
Synthesis of pyrazolo[4,3-c][1,2,6]benzothiadiazocine, a new ring system as potential COX inhibitor
2012
Derivatives of the new ring system 1,4-dihydropyrazolo[4,3-c][1,2,6] benzothiadiazocin-11(10H)one 5,5-dioxide were synthesized in five or six steps in 57-66% overall yields and tested as COX inhibitors.
SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF 7-SUBSTITUTED1-ETHYL-3,4,10-TRIMETHYL-1,10-DIHYDRO-11H-PYRAZOLO(3,4-c)(1,6)BENZODIAZOCIN-11-ONE: A NEW RI…
2004
Derivatives of the title ring system of type 10 were obtained in good yield by fusion of the intermediates 12. Attempt to cyclize the acetylamino derivative 9 under Bischler-Napieralski conditions failed because of the insufficient electronic density in the position 4 of the pyrazole ring created by the adjacent carbonyl moiety. The derivatives of the new ring system, assayed as anxiolytic agents, showed no significant activity.
Synthesis of pyrazole-4-carbohydrazide derivatives of pharmaceutical interest
2003
New 1-phenylor 1-methyl-5-benzamidopyrazole-4-carbohydrazide derivatives were prepared in 70–90% yields from 1-methylor 1-phenyl-6-phenylpyrazolo[3,4-d]1,3-oxazin-4(1H)-one derivatives and hydrazine hydrate. Small quantities of the isomeric 5-aminopyrazole-4-(Nbenzoyl)hydrazides were detected in some reaction mixtures, proving that intramolecular benzoyl migration can take place in the 5-benzamidopyrazole-4-carbohydrazide molecule. The direct formation of pyrazole-4-carbohydrazides from 5-benzamidopyrazole-4-carboxylic acid ethyl esters and hydrazine hydrate was unsuccessful.
Palladium-Catalyzed Direct Arylation of Heteroaromatics with Activated Aryl Chlorides Using a Sterically Relieved Ferrocenyl-Diphosphane
2012
International audience; The palladium-catalyzed direct arylations at C3 or C4 positions of heteroaromatics are known to be more challenging than at C2 or C5 positions. Aryl chlorides are also challenging substrates for direct arylation of heteroaromatics. We observed that in the presence of a palladium-catalyst combining only 0.5 mol % of Pd(OAc)2 with the sterically relieved new ferrocenyl diphosphane Sylphos, the direct arylation at C3 or C4 of oxazoles, a benzofuran, an indole, and a pyrazole was found to proceed in moderate to high yields using a variety of electron deficient aryl chlorides. Turnover numbers up to 176 have been obtained with this catalyst. Assessment of the electron-don…
Treatment of pulmonary embolism.
2015
International audience; The treatment of pulmonary embolism is going to be deeply modified by the development of Direct Oral Anticoagulants (DOACs). There are currently three anti-Xa factors (rivaroxaban, apixaban, edoxaban) and one anti-IIa factor (dabigatran) labeled by the FDA and the EMA. All these drugs are direct anticoagulant, orally effective, without the need for adaptation to hemostasis test. As kidney excretion is involved for all of them, they are contra-indicated in patients with severe renal failure (creatinine clearance<30mL/min according to Cockcroft & Gault formula). All the anti-Xa factor drugs are metabolized by liver cytochromes and then contra-indicated in case of liver…
Antagonism by SR 48692 of mechanical responses to neurotensin in rat intestine.
1996
Abstract 1. The effects of SR 48692 on neurotensin (NT)-induced mechanical responses were investigated in rat duodenum and proximal colon by use of isometric, isovolumic preparations. 2. SR 48692 inhibited the relaxant responses to NT in duodenal circular and longitudinal muscle. It also antagonized the NT-induced contractile effects in duodenal circular muscle and in proximal colon (both muscular layers). 3. From Schild analysis and pA2 value for SR 48692 was 8.2 in tissues where NT induced relaxant effects and 7.5 in tissues where NT induced contractile effects and the slope of the regression line was not significantly different from unity, indicating competitive antagonism. 4. SR 48692 d…
Progestogens reduce thromboxane production by cultured human endothelial cells.
2011
Objectives Progestogens have been poorly studied concerning their roles in endothelial physiology. Prostanoids are vasoactive compounds, such as thromboxane A2, a potent vasoconstrictor, and prostacyclin, a vasodilator. We examined the effects of two progestogens used clinically, progesterone and medroxyprogesterone acetate, on thromboxane A2 production by cultured human umbilical vein endothelial cells (HUVEC) and investigated the role of progesterone receptors and the enzymes involved in production of thromboxane A2 and prostacyclin. Methods Cells were exposed to 1‐100 nmol/l of either progesterone or medroxyprogesterone acetate, and thromboxane A2 production was measured in culture mediu…