Design, synthesis and structure–activity relationships of zwitterionic spirocyclic compounds as potent CCR1 antagonists

A series of zwitterionic spirocyclic compounds were synthesised. In vitro data revealed that these compounds were potent CCR1 antagonists. In particular, 2, 4, 11 and 20 inhibited CCR1 mediated chemotaxis of THP-1 cells in a functional assay.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-07, Vol.23 (14), p.4026-4030
Hauptverfasser:	Hossain, Nafizal, Ivanova, Svetlana, Timén, Åsa Sjöholm, Bergare, Jonas, Mussie, Tesfaledet, Bergström, Lena
Format:	Artikel
Sprache:	eng
Schlagworte:	Antagonists Cell Line, Tumor chemotaxis Chemotaxis - drug effects Drug Design Humans Protein Binding Receptors, CCR1 - antagonists & inhibitors Receptors, CCR1 - metabolism Spiro Compounds - chemical synthesis Spiro Compounds - chemistry Spiro Compounds - pharmacology Structure-Activity Relationship structure-activity relationships zwitterions
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Beschreibung
Zusammenfassung:	A series of zwitterionic spirocyclic compounds were synthesised. In vitro data revealed that these compounds were potent CCR1 antagonists. In particular, 2, 4, 11 and 20 inhibited CCR1 mediated chemotaxis of THP-1 cells in a functional assay.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2013.05.087