4-hydroxythiazole inhibitors of 5-lipoxygenase.

doi:10.1002/CHIN.199152183

Paper

4-hydroxythiazole inhibitors of 5-lipoxygenase.

Published Jul 1, 1991 · F. A. Kerdesky, J. Holms, Jimmie L. Moore

Journal of medicinal chemistry

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36

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0

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Abstract

4-Hydroxythiazoles have been identified as potent inhibitors of 5-lipoxygenase in vitro exhibiting IC50's of less than 1 microM. An investigation of structure-activity relationships showed that the most potent inhibitors of this series are the 5-phenyl derivatives. The corresponding thiazolidin-4-one analogues were found to be relatively inactive. The 4-hydroxythiazoles were active inhibitors against 5-lipoxygenase in both intact rat polymorphonuclear leukocytes and human whole blood. The compounds were also selective inhibitors of 5-lipoxygenase, displaying only weak activity against other related enzymes, cyclooxygenase and 12- and 15-lipoxygenase.

In Vitro Study

Study Snapshot

4-hydroxythiazoles are potent inhibitors of 5-lipoxygenase, showing selective activity against this enzyme and weak activity against related enzymes.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Paper

4-hydroxythiazole inhibitors of 5-lipoxygenase.

References

Citations

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