Prolyl endopeptidase inhibitors: N-acyl derivatives of L-thioproline- pyrrolidine

Kánai Károly, Erdo Sándor, Susán Edit, Fehér Miklós, Sipos Judit, Podányi Benjámin, Szappanos Andrea, Hermecz István

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

A series of N-acyl derivatives of thioproline-pyrrolidine was prepared conventionally and evaluated in vitro against rat brain prolyl endopeptidase (PEP). It is argued an the basis of pharmacophore plots that an optimum chain length exists as a result of increased population of pharmacophore space and decreased solubility on increasing the alkyl chain length.

Original languageEnglish
Pages (from-to)1701-1704
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume7
Issue number13
DOIs
Publication statusPublished - Jul 8 1997

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prolyl oligopeptidase
Protease Inhibitors
Chain length
Solubility
Derivatives
Brain
Population
Rats
thiazolidine-4-carboxylic acid
pyrrolidine
In Vitro Techniques

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Prolyl endopeptidase inhibitors : N-acyl derivatives of L-thioproline- pyrrolidine. / Károly, Kánai; Sándor, Erdo; Edit, Susán; Miklós, Fehér; Judit, Sipos; Benjámin, Podányi; Andrea, Szappanos; István, Hermecz.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 7, No. 13, 08.07.1997, p. 1701-1704.

Research output: Contribution to journalArticle

Károly, K, Sándor, E, Edit, S, Miklós, F, Judit, S, Benjámin, P, Andrea, S & István, H 1997, 'Prolyl endopeptidase inhibitors: N-acyl derivatives of L-thioproline- pyrrolidine', Bioorganic and Medicinal Chemistry Letters, vol. 7, no. 13, pp. 1701-1704. https://doi.org/10.1016/S0960-894X(97)00295-3
Károly, Kánai ; Sándor, Erdo ; Edit, Susán ; Miklós, Fehér ; Judit, Sipos ; Benjámin, Podányi ; Andrea, Szappanos ; István, Hermecz. / Prolyl endopeptidase inhibitors : N-acyl derivatives of L-thioproline- pyrrolidine. In: Bioorganic and Medicinal Chemistry Letters. 1997 ; Vol. 7, No. 13. pp. 1701-1704.
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