725265-84-9Relevant academic research and scientific papers
A cyclopent-2-enecarbonyl group mimics proline at the P2 position of prolyl oligopeptidase inhibitors
Jarho, Elina M.,Ven?l?inen, Jarkko I.,Huuskonen, Juhani,Christiaans, Johannes A. M.,Garcia-Horsman, J. Arturo,Forsberg, Markus M.,J?rvinen, Tomi,Gynther, Jukka,M?nnist?, Pekka T.,Wallén, Erik A. A.
, p. 5605 - 5607 (2007/10/03)
With the aim to replace the natural amino acid proline by a proline mimetic structure, a cyclopent-2-enecarbonyl moiety was studied at the P2 position of prolyl oligopeptidase (POP) inhibitors. The cyclopent-2-enecarbonyl moiety proved to be an excellent proline mimetic at the P2 position of POP inhibitors. The replacement is particularly useful when increased lipophilicity is needed.
COMPOUNDS HAVING PROLYL OLIGOPEPTIDASE INHIBITORY ACTIVITY
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Page 22-23, (2010/02/07)
The invention provides a compound of formula (I), wherein in the formula X, R1, R2 and R3 are as defined in claim 1, or a pharmaceutically acceptable salt or ester thereof, useful as a prolyl oligopeptidase inhibitor. The compounds of formula (I) can be used for the treatment of diseases or conditions where prolyl oligopeptidase inhibitors are indicated to be effective, for example for the treatment of neurodegenerative diseases, such as Alzheimer's disease and senile dementia
