Výsledky vyhledávání - "R. M. Mcmillan"

ChemInform Abstract: Indazolinones, a New Series of Redox-Active 5-Lipoxygenase Inhibitors with Built-In Selectivity and Oral Activity

Autor: C. Delvare, R. M. Mcmillan, P. Bruneau, Martin Paul Edwards

Publikováno v: ChemInform. 22

Since the hypothetical mechanisms of hydroperoxydation of arachidonic acid by, respectively, 5-lipoxygenase (5-LPO) and cyclooxygenase (CO) involve a redox cycle, a compound which reduces 5-LPO and CO to their inactive state would give a nonselective

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f087a98cbb2f8384495e73b8cf5d971c
https://doi.org/10.1002/chin.199127164

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Are tolfenamic acid and tenidap dual inhibitors of 5-lipoxygenase and cyclo-oxygenase?

Autor: R. M. McMillan, K. E. Proudman

Publikováno v: Agents and Actions. 34:121-124

Tolfenamic acid and tenidap have been reported to be dual inhibitors of cyclo-oxygenase and 5-lipoxygenase. In this study inhibition of 5-lipoxygenase by tenidap and tolfenamic acid in plasma-free leukocyte suspensions (IC50 values = 10 microM) requi

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https://doi.org/10.1007/bf01993255

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Methoxyalkyl thiazoles: A novel series of potent, orally active and enantioselective inhibitors of 5-lipoxygenase

Autor: M. P. Edwards, S. J. Foster, J. F. Kingston, R. M. Mcmillan, J.-M. Girodeau, T. G. C. Bird, G. C. Crawley

Publikováno v: Agents and Actions. 34:110-112

Methoxyalkyl thiazoles are novel 5-lipoxygenase inhibitors which are neither redox agents nor iron chelators and are exemplified by ICI211965 [1-(3-(naphth-2-ylmethoxy)phenyl)-1-(thiazol-2-yl)prop yl methyl ether]. ICI211965 potently inhibits LTC4 sy

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https://doi.org/10.1007/bf01993252

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Selective chiral inhibitors of 5-lipoxygenase with anti-inflammatory activity

Autor: J.-M. Girodeau, S. J. Foster, R. M. Mcmillan

Publikováno v: British Journal of Pharmacology. 101:501-503

The studies described here, using enantiomers of an optically-active methoxy alkyl thiazole ICI216800 (1-methoxy-6-(naphth-2-yl-methoxyl)-1- (thiazol-2-yl)indane), provide unequivocal evidence for a specific, chiral interaction with 5-lipoxygenase. I

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https://doi.org/10.1111/j.1476-5381.1990.tb14111.x

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Approaches to Novel Anti-arthritic Drugs by Modulation of the Arachidonic Acid Cascade

Autor: John S. Shaw, R. M. Mcmillan, S. J. Foster

Publikováno v: Mechanisms and Models in Rheumatoid Arthritis

This chapter reviews several potential approaches for novel therapies, based on modulation of the arachidonic acid metabolites. It describes two approaches for discovering drugs with the efficacy, but not the side-effects, of non steroidal anti-infla

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https://doi.org/10.1016/b978-012340440-4/50046-5

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Structure and activity relationships leading to the discovery of ICI D2138, a selective, potent and orally active inhibitor of 5-lipoxygenase

Autor: G C, Crawley, T G, Bird, P, Bruneau, R I, Dowell, P N, Edwards, S J, Foster, J M, Girodeau, R M, McMillan, E R, Walker, D, Waterson

Publikováno v: Journal of lipid mediators. 6(1-3)

Structure and activity relationships of (methoxyalkyl)thiazole and 4-methoxytetrahydropyran series of 5-lipoxygenase inhibitors are reviewed. One member of the 4-methoxytetrahydropyran series, 6-([fluoro-5-(4-methoxy-3,4,5,6-tetrahydro-2H-pyran-4-yl)

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https://pubmed.ncbi.nlm.nih.gov/8395247

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Stimulation of human polymorphonuclear leukocytes by leukotriene B4 and platelet-activating factor: an ultrastructural and pharmacological study

Autor: A. G. Rossi, C. J. P. Jones, D. E. Macintyre, R. M. Mcmillan

Publikováno v: Journal of leukocyte biology. 53(2)

Human polymorphonuclear leukocytes (PMNs) stimulated by N-formylmethionyl-leucyl- phenylalanine (fMLP), leukotriene B4 (LTB4) and platelet-activating factor (PAF) showed a similar sequence of ultrastructural changes. Exposure of unstirred PMNs to die

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https://pubmed.ncbi.nlm.nih.gov/8383164

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(Methoxyalkyl)thiazoles: a new series of potent, selective, and orally active 5-lipoxygenase inhibitors displaying high enantioselectivity

Autor: R. M. Mcmillan, Pierre Andre Raymond Bruneau, John F. Kingston, T. Geoffrey C. Bird, Graham Charles Crawley, Martin Paul Edwards, Jean Marc Girodeau, S. J. Foster

Publikováno v: Journal of medicinal chemistry. 34(7)

(Methoxyalkyl)thiazoles are novel 5-lipoxygenase (5-LPO) inhibitors that are neither redox agents nor iron chelators. Consideration of a hypothetical model of the enzyme active site led to this series which is exemplified by 1-[3-(naphth-2-ylmethoxy)

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https://pubmed.ncbi.nlm.nih.gov/1648621

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