An Integrated Continuous Flow Micro-Total Ultrafast Process System (μ-TUFPS) for the Synthesis of Celecoxib and Other Cyclooxygenase Inhibitors

2019 ◽  
Vol 23 (9) ◽  
pp. 1892-1899 ◽  
Author(s):  
Vinay Kumar Sthalam ◽  
Ajay K. Singh ◽  
Srihari Pabbaraja
2020 ◽  
Vol 22 (19) ◽  
pp. 6437-6443
Author(s):  
Cheng-Kou Liu ◽  
Meng-Yi Chen ◽  
Xin-Xin Lin ◽  
Zheng Fang ◽  
Kai Guo

A catalyst-, oxidant-, acidic solvent- and quaternary ammonium salt-free electrochemical para-selective hydroxylation of N-arylamides at rt in batch and continuous-flow was developed.


Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
B Waltenberger ◽  
D Schuster ◽  
S Paramapojn ◽  
W Gritsanapan ◽  
G Wolber ◽  
...  

1988 ◽  
Vol 59 (02) ◽  
pp. 225-230 ◽  
Author(s):  
J P Maffrand ◽  
A Bernat ◽  
D Delebassée ◽  
G Defreyn ◽  
J P Cazenave ◽  
...  

SummaryThe relative importance of ADP, arachidonic acid metabolites and serotonin as thrombogenic factors was evaluated in rats by comparing, after oral administration, the effects of two inhibitors of ADP-induced platelet aggregation (ticlopidine and PCR 4099), three cyclo-oxygenase inhibitors (aspirin, triflusal and indobufen) and a selective serotonin 5HT2 receptor antagonist (ketanserin) on platelet aggregation, in four platelet-dependent thrombosis models and on bleeding time. Platelet aggregation induced by ADP and collagen was completely inhibited by ticlopidine and PCR 4099 whereas only the collagen aggregation was reduced by the cyclo-oxygenase inhibitors. Ketanserin or a depletion of platelet serotonin by reserpine did not affect platelet aggregation. Ticlopidine and PCR 4099 greatly prolonged rat tail transection bleeding time. This is probably related to their known ability to inhibit ADP-mediated platelet aggregation. In contrast, the cyclooxygenase inhibitors did not affect bleeding time at all. Reserpine and ketanserin prolonged bleeding time by interfering with the action of serotonin on the vascular wall. Ticlopidine and PCR4099 were very potent antithrombotics in all the models. Aspirin, only at a high dose, inhibited poorly thrombus formation on a silk thread in an arterio-venous shunt, suggesting that the inhibition of cyclo-oxygenase was not responsible. Triflusal was inactive in all models while indobufen slightly reduced thrombus formation in the silk thread and metallic coil models. Ketanserin and reserpine reduced thrombus only in the metallic coil model. Thrombus formation was greatly reduced in fawn-hooded rats, which lack ADP in their platelet dense granules because of a genetic storage pool deficiency. Taken together, the results obtained with the drugs and with the fawn-hooded rats support the concept that ADP plays a key role in thrombogenesis in rats.


1986 ◽  
Vol 56 (03) ◽  
pp. 263-267
Author(s):  
K D Butler ◽  
R A Shand ◽  
R B Wallis

SummaryThe effects of intravenously administered collagen on the circulatory platelet count, TxB2, 6-keto PGF1α and 51Cr-labelled platelet accumulation in the thorax have been evaluated in the guinea-pig. Administration of collagen induced a dose-related peripheral thrombocytopenia and a concomitant increase in 51Cr-labelled platelets in the thorax. There was also a transient dose-related increase in plasma TxB2 but no change in plasma 6-keto PGF1α levels.The thromboxane synthetase inhibitors tested, reduced the platelet accumulation, but only CGS 13080 significantly inhibited TxB2 production. In contrast all the cyclooxygenase inhibitors tested impaired the elevation of plasma TxB2 after collagen, but only diclofenac inhibited the 51Cr-labelled platelet accumulation.The greater effect of thromboxane synthetase inhibitors compared to cyclooxygenase inhibitors on platelet accumulation in this system cannot be completely explained by the changes measured in the circulating prostanoids.


2021 ◽  
Vol 147 (3) ◽  
pp. 04021002
Author(s):  
Wenrui Qu ◽  
Shaojie Liu ◽  
Qun Zhao ◽  
Yi Qi

2000 ◽  
Vol 627 ◽  
Author(s):  
M. E. Swanson ◽  
M. Landreman ◽  
J. Michel ◽  
J. Kakalios

ABSTRACTWhen an initially homogeneous binary mixture of granular media such as fine and coarse sand is poured near the closed edge of a “quasi-two-dimensional” Hele-Shaw cell consisting of two vertical transparent plates held a narrow distance apart, the mixture spontaneously forms alternating segregated layers. Experimental measurements of this stratification effect are reported in order to determine which model, one which suggests that segregation only occurs when the granular material contained within a metastable heap between the critical and maximum angle of repose avalanches down the free surface, or one for which the segregation results from smaller particles becoming trapped in the top surface and being removed from the moving layer during continuous flow. The result reported here indicate that the Metastable Wedge model provides a natural explanation for the initial mixed zone which precedes the formation of the layers, while the Continuous Flow model explains the observed upward moving kink of segregated material for higher granular flux rates, and that both mechansims are necessary in order to understand the observed pairing of segregated layersfor intermediate flow rates and cell separations.


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