| Autor: |
Veken, P. Van der, Senten, K., Kertesz, I., Meester, I. De, Lambeir, A.-M., Maes, M.-B., Scharpe, S., Haemers, A., Augustyns, K. |
| Zdroj: |
Journal of Medicinal Chemistry; March 2005, Vol. 48 Issue: 6 p1768-1780, 13p |
| Abstrakt: |
The feasibility of the fluoro-olefin function as a peptidomimetic group in inhibitors for dipeptidyl peptidase IV and II (DPP IV and DPP II) is investigated by evaluation of N-substituted Gly-Ψ[CF&dbd;C]pyrrolidines, Gly-Ψ[CF&dbd;C]piperidines, and Gly-Ψ[CF&dbd;C](2-cyano)pyrrolidines. Of this later class, the (Z)- and (E)-fluoro-olefin analogues were prepared and chemical stability in comparison with the parent amide was checked. Most of these compounds exhibited a strong binding preference toward DPP II with IC50 values in the low micromolar range, while only low DPP IV inhibitory potential is seen. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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