Inhibitors of oleamide hydrolase

Details Inhibitors of oleamide hydrolase Inhibitors of oleamide hydrolase

1999-01-05

2000-08-01

Carr, Deborah D.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514552, 514613, 514623, 514627, 514628, A01N 3706

Patent

active

060967846

ABSTRACT:
Inhibitors of oleamide hydrolase, responsible for the hydrolysis of an endogenous sleep-inducing lipid (1, cis-9-octadecenamide) were designed and synthesized. The most potent inhibitors possess an electrophilic carbonyl group capable of reversibly forming a (thio) hemiacetal or (thio) hemiketal to mimic the transition state of a serine or cysteine protease catalyzed reaction. In particular, the tight binding .alpha.-keto ethyl ester 8 (1.4 nM) and the trifluoromethyl ketone inhibitor 12 (1.2 nM) were found to have exceptional inhibitory activity. In addition to the inhibitory activity, some of the inhibitors displayed agonist activity which resulted in the induction of sleep in laboratory animals.

REFERENCES:
Chem abstr of Koutek et al, Journal of Biological Chemistry, vol. 269, No. 37, pp. 22937-22940, 121:221790, 1994.
Chem. abstr. of JP-01086884, 111:193095, 1989.

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