2. Academic Validation
  3. Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors

Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors

  • Bioorg Med Chem Lett. 2009 Aug 1;19(15):4026-30. doi: 10.1016/j.bmcl.2009.06.027.
Manolo Rocco Sablone 1,  Maria Candida Cesta,  Alessio Moriconi,  Andrea Aramini,  Cinzia Bizzarri,  Claudia Di Giacinto,  Rosa Di Bitondo,  Isabelle Gloaguen,  Massimiliano Aschi,  Marcello Crucianelli,  Riccardo Bertini,  Marcello Allegretti
Affiliations

Affiliation

  • 1 Research Center, Dompé pha.r.ma s.p.a., via Campo di Pile, 67100, L'Aquila, Italy.
PMID: 19560921 DOI: 10.1016/j.bmcl.2009.06.027
Abstract

We reported recently the Structure-Activity Relationship (SAR) of a class of CXCL8 allosteric modulators. They invariably share a 2-arylpropionic moiety so far considered a key structural determinant of the biological activity. We show the results of recent SAR studies on a novel series of phenylacetic derivatives supported by a combined approach of mutagenesis experiments and conformational analysis. The results suggest novel insights on the fine role of the propionic/acetic chain in the modulation of CXCL8 receptors.

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