Non-steroid and non-prostanoid inhibitors of steroid and prostag

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Aldehyde doai

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435184, 435190, A01N 3500, A61K 3111

Patent

active

054399432

ABSTRACT:
Compounds such as 1-(4'-nitrophenyl)-2-propen-1-ol are disclosed which are non-steroidal mechanism-based inactivators of rat liver 3.alpha.-hydroxysteroid dehydrogenase. The corresponding ketones are time dependent inactivators of cyclooxygenase (PGH.sub.2 -synthase).

REFERENCES:
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Penning et al. (1984) Biochem. J. 222, 601-611.
Penning et al. (1983) Proc. Natl. Acad. Sci., U.S.A. 80, 4504-4508.
Penning et al. (1987) Biochem. Biophys. Res. Comm. 142(2), 646-652.
MacInnes et al., Allylic Inhibitors of Alcohol Dehydrogenase, Journal of the Chemical Society Perkin Transaction 1, 1981, 1103-1108.
Covey et al., Biochemistry 1986, 25, 7288.
Ricigliano et al. Biochem. J. 1989, 262, 139.
Lawate and Covey, J. Med. Chem. 1990, 33, 2319-2321.

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