Platelet activating factor antagonist activity

Young s modulus for [CERAMICS - PffiCHANICAL PROPERTIES AND BEHAVIOR] (Vol 5) Platelet-activating factor QAE) antagonists... 

The synthetic utihty of the above transformations stems from the fact that many monoesters obtained as a result of hydrolysis may be converted to pharmaceutically important intermediates. For example, the optically active glycerol derivative (27) is a key intermediate in the production of P-blockers. Akyl derivative (25) may be converted into (5)-paraconic acid [4694-66-0] ((5)-5-oxo-3-tetrahydrofurancarboxyhc acid) that is a starting material for the synthesis of (3R)-A-factor. The unsaturated chiral cycHc monoacetate (31) is an optically active synthon for prostaglandins, and the monoester (29) is used for the synthesis of platelet activating factor (PAF) antagonists. 

Various 1.4-benzodiazepines with a five-membered heteroaromatic ring fused to the 1,2-bond, such as 17, where A represents a heteroaromatic ring, have been prepared by such methods and tested for activity on the central nervous system, as cholecystokinin antagonists and as antagonists of platelet activating factors.245... 

Ketotifen Hrreceptor antagonist, mast cell stabilizer, eosinophil inhibitor, platelet-activating factor inhibitor May inhibit eosinophil chemotaxis... 

A5. Anderson, B. O., Bensard, D. D., and Harken, A. H The role of platelet activating factor and its antagonists in shock, sepsis and multiple organ failure. Surg. Gynecol. Obstet. 172,415-424 (1991). 

D8. DeJoy, S. Q., Jeyaseelan, R., Torley, L. W., Pickett, W. C., Wissner, A., Wick, M. M., Oronsky, A. L., and Kerwar, S. S., Effect of CL 184,005, a platelet-activating factor antagonist in a murine model of Staphylococcus aureus-induced gram-positive sepsis. J. Infect. Dis. 169, 150-156... 

D22. Dirkes, K., Harris, B. H., Connolly, R. J., Schwaitzberg, S. D., Dinarello, C. A., and Gelfand, J. A., Platelet activating factor-antagonist improves survival in experimental staphylococcal septicemia. 7. Pediatr. Surg. 29, 1055-1057 (1994). 

K5. Kawamura, M Terashita, Z Imura, Y., Shino, A., and Nishikawa, K Inhibitory effect of TCV-309, a novel platelet activating factor (PAF) antagonist, on endotoxin-induced disseminated intravascular coagulation in rats Possible role of PAF in tissue factor generation. Thromb. Res. 70,281-293(1993). 

K10. Klabunde, R. E., and Calvello, C., Inhibition of endotoxin-induced microvascular leakage by a platelet-activating factor antagonist and 5-lipoxygenase inhibitor. Shock 4, 368-372 (1995). 

Platelet-activating factor is a transcriptional activator of cyclooxygenase-2. PAF induces mouse COX-2-promoter-driven luciferase activity transfected in neuroblastoma cells, such as NG108-15 or SH-SY5Y, and in NIH 3T3 cells (Fig. 33-5). The intracellular PAF antagonist BN 50730 inhibits PAF activation of this construct [41]. 

Packard, M. G., Teather, L. and Bazan, N. G. Effects of intra-striatal injections of platelet-activating factor and the PAF antagonist BN 52021 on memory. Neurobiol. Leant. Mem. 66 176-182,1996. 

Panetta, T., MarcheselH, V. L., Braquet, P., Spinnewyn, B. and Bazan, N. G. Effects of a platelet-activating factor antagonist (BN52021) on free fatty acids, diacylglycerols, polyphosphoinositides and blood flow in the gerbil brain Inhibition of ischemia-reperfusion induced cerebral injury. Biochem. Biophys. Res. Commun. 149 580-587,1987. 

Bergman described indole C-3 acylation with acid chlorides via 1-indolylzinc chloride in the absence of palladium [108]. Davidsen and co-workers synthesized 86, which is a potent antagonist of platelet activating factor-mediated effects, using this Bergman acylation sequence... 

Antagonists of Platelet-Activating Factor Chemistry, Pharmacology and Clinical Applications... 

Chapter 7 outlines the basic mechanism and treatment of emesis, and in particular, that induced by chemotherapy of cancer. Finally, the chemistry, pharmacology and clinical applications of antagonists of the platelet-activating factor (PAF), an important mediator of many physiological and pathological conditions, are reviewed in Chapter 8. 

Kurihara K, Wardlaw AJ, Moqbel R, Kay AB. (1989). Inhibition of platelet-activating factor (PAF)-induced chemotaxis and PAF binding to human eosinophils and neutrophils by the specific ginkgolide-derived PAF antagonist, BN 52021. J Allergy Clin Immunol. 83(1) 83-90. 

Lamant V, Mauco G, Braquet P, Chap H, Douste-Blazy L. (1987). Inhibition of the metabolism of platelet activating factor (PAF-acether) by three specific antagonists from Ginkgo biloba. Biochem Pharmacol. 36(17) 2749-52. 

The replacement of the polar head group of a range of piperazines by a 2-methylimidazo[4,5-f]pyridine group provided efficient orally active platelet-activating factor antagonists, for example, compounds 191-193 <1996JME487>. 

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