Prolyl endopeptidase inhibition

The title compound, 2-(8-dimethylaminooctylthio)-6-isopropyl-3-pirydyl-2-thienyl ketone (222), a potent competitive reversible inhibitor of the enzyme PEP (prolyl endopeptidase which cleaves a variety of oligopeptides in brain and peripheral tissues217), has been synthesized218 by ["CJalkylation of the iV-desmethyl precursor 223 (equation 117). 222 crosses the BBB and inhibits brain PEP in rodents219. It is used in the study of biodistribution and activity of brain proteases by PET to evaluate the roles... 

Documented effects Essential oils from this species are used in the pharmaceutical industry to add an aroma to drugs and in the fragrance industry as an aroma fixative (Khalmatov and Kosimov 1992 Ganunerman et al. 1990). Water and MeOH extracts of the plant strongly inhibited aldose reductase activity, an enzyme associated with diabetic complications (Kasimu et al. 1998). Compounds from the plant were found to inhibit prolyl endopeptidase (PEP), an enzyme thought to be involved with learning and memory processes, and the inhibition of which may produce anti-amnesic effects (Tezuka et al. 1999). 

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