ChemInform Abstract: Synthesis and Pharmacological Study of Some 3-(Pyrazol-5-yl)-quinazolin- 4(3H)-ones.

1986 ◽  
Vol 17 (52) ◽  
Author(s):  
S. PLESCIA ◽  
M. L. BAJARDI ◽  
D. RAFFA ◽  
G. DAIDONE ◽  
M. MATERA ◽  
...  
1995 ◽  
Vol 74 (02) ◽  
pp. 660-666 ◽  
Author(s):  
P Mismetti ◽  
J Reynaud ◽  
B Tardy-Poncet ◽  
S Laporte-Simitsidis ◽  
M Scully ◽  
...  

SummaryLow molecular weight heparin (LMWH) is currently prescribed for the treatment of deep vein thrombosis at the dose of 100 IU antiXa/kg twice daily or at a dose of 175 IU antiXa/kg once daily with a similar efficacy. We decided to study the chrono-pharmacology of curative dose of LMWH once daily administrated according to the one previously described with unfractionated heparin (UFH).Ten healthy volunteers participated in an open three-period crossover study according to three 24 h cycles, separated by a wash-out interval lasting 7 days: one control cycle without injection, two cycles with subcutaneous injection of 200 IU antiXa/kg of Dalteparin (Fragmin®) at 8 a.m. or at 8 p.m. Parameters of heparin activity were analysed as maximal values and area under the curve.Activated partial thromboplastin time (APTT), thrombin time (TT), prothrombin time (PT) and tissue factor pathway inhibitor (TFPI) were higher after 8 p.m. injection than after 8 a.m. injection (p <0.05) while no chrono-pharmacological variation of anti factor Xa (AXa) activity was observed. Thus the biological anticoagulant effect of 200 IU antiXa/kg of Dalteparin seems to be higher after an evening injection than after a morning injection.A chrono-therapeutic approach with LMWH, as prescribed once daily, deserves further investigation since our results suggest that a preferential injection time may optimise the clinical efficacy of these LMWH.


Author(s):  
Krishna Reddy BV ◽  
Avinash Kumar Reddy G ◽  
Sujitha V ◽  
Manasa A

DM otherwise diabetes is now a days an epidemic with the percentage of patient population rising to almost 10% of the world population. Out of all the DM complications, cataract leads the way contributing to disabilities to about 60% of diabetic population. But the pathogenesis of DM cataract is still a half-understood area of medicine there by posing a problem in the therapy. The data that we have till now gives us enough evidence to advocate the oxidative stress has a major role for the pathogenesis of DM complications like DMnephropathy, DMneuropathy, and cardiac hypertrophy, which suggests the oxidative stress is a central feature of diabetes. In the current research, the pharmacological evaluation of Fisetin for its DM based anti-cataract property was performed. This research concentrates to estimate the possible involvement of Nrf-2 / heme oxygenase (HO)-pathway in the observed therapeutic effect, if any. The data obtained in this study also indicate that the observed beneficial effects mainly due to activation of Nrf2/HO-1 pathway. These effects probably result in increased tissue anti-oxidant status as well as decreased free radical production, which ultimately responsible for the observed beneficial effects of Fisetin against hyperglycemia-induced cataract.


1991 ◽  
Vol 56 (11) ◽  
pp. 2494-2499 ◽  
Author(s):  
Maria M. Curzu ◽  
Gérard A. Pinna ◽  
Giorgio Cignarella ◽  
Daniela Barlocco ◽  
Maria Piera Demontis

We have synthesized and tested for their antiinflammatory activity a new series of 3-aryl-4,5-dihydro-4-isoxazoleacetic acids (IVa-IVg). Preliminary pharmacological results seem to indicate the 3-phenyl derivative IVa as the most interesting compound. In fact, when tested against carrageenin edema in Wistar rats, it shows antiinflammatory activity comparable to that of naproxene, taken as reference drug, though of shorter duration. All the substituted phenyl derivatives were less active (IVd-IVf) or inactive (IVb, IVc, IVg).


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