Exploration of beta-turn scaffolding motifs as components of sialyl Le(X) mimetics and their relevance to P-selectin

Monocyclic and bicyclic lactam units representing beta-turn surrogates were incorporated into a sialyl Le(X) structure by replacement of the natural sugar components. Low micromolar activity was found in a new P-selectin binding assay.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-10, Vol.8 (19), p.2803-2808
Hauptverfasser:	Hanessian, S, Huynh, H K, Reddy, G V, McNaughton-Smith, G, Ernst, B, Kolb, H C, Magnani, J, Sweeley, C
Format:	Artikel
Sprache:	eng
Schlagworte:	beta-Lactams - chemical synthesis beta-Lactams - chemistry beta-Lactams - metabolism Binding, Competitive Carbohydrate Conformation Carbohydrate Sequence E-Selectin - metabolism Indolizines - chemical synthesis Indolizines - chemistry Indolizines - metabolism Molecular Sequence Data Oligosaccharides - chemical synthesis Oligosaccharides - chemistry Oligosaccharides - metabolism P-Selectin - metabolism Structure-Activity Relationship Substrate Specificity
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Beschreibung
Zusammenfassung:	Monocyclic and bicyclic lactam units representing beta-turn surrogates were incorporated into a sialyl Le(X) structure by replacement of the natural sugar components. Low micromolar activity was found in a new P-selectin binding assay.
ISSN:	0960-894X
DOI:	10.1016/S0960-894X(98)00500-9