N-(3-(4-Hydroxyphenyl)-propenoyl)-amino acid tryptamides as SIRT2 inhibitors

  • Bioorg Med Chem Lett. 2007 May 1;17(9):2448-51. doi: 10.1016/j.bmcl.2007.02.023.
Päivi H Kiviranta  1 ,  Jukka Leppänen ,  Valtteri M Rinne ,  Tiina Suuronen ,  Olga Kyrylenko ,  Sergiy Kyrylenko ,  Erkki Kuusisto ,  Anu J Tervo ,  Tomi Järvinen ,  Antero Salminen ,  Antti Poso ,  Erik A A Wallén
Affiliations
  • 1. Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, 70211 Kuopio, Finland. [email protected]
PMID: 17329104 DOI: 10.1016/j.bmcl.2007.02.023
Abstract

A series of N-(3-(4-hydroxyphenyl)-propenoyl)-amino acid tryptamides was based on a previously reported new SIRT2 Inhibitor from our group, and it was designed to study if the molecular size of the compound could be reduced. The most potent compounds, N-(3-(4-hydroxyphenyl)-propenoyl)-2-aminoisobutyric acid tryptamide and N-(3-(4-hydroxyphenyl)-propenoyl)-L-alanine tryptamide, were equipotent, 30% smaller in molecular weight, and slightly more selective (SIRT2/SIRT1) than the parent compound.

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