| Autor: |
McMillan, R., Bird, T., Crawley, G., Edwards, M., Girodeau, J., Kingston, J., Foster, S. |
| Zdroj: |
Agents & Actions; Sep1991, Vol. 34 Issue 1/2, p110-112, 3p |
| Abstrakt: |
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)propyl methyl ether]. ICI211965 potently inhibits LTC synthesis in murine macrophages (IC=0.0085 μ M) and its selectivity with respect to cyclo-oxygenase (>5800) is greater than any previously reported lipoxygenase inhibitor. ICI211965 also selectively inhibits LTB synthesis by human blood in vitro (IC=0.45 μ M) and rat blood ex vivo (ED=10 mg/Kg, p.o.). Methoxyalkyl thiazoles exhibit a tight structure activity relationship and resolution of a chiral member of the series demonstrates that 5-lipoxygenase inhibition resides largely in one enantiomer. Methoxyalkyl thiazoles represent the first class of agents for which 5-lipoxygenase inhibition is mediated by specific, enantioselective interaction with the enzyme. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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