alpha(v)beta(3) Antagonists based on a central thiophene scaffold

A series of novel, highly potent alpha(v)beta(3) antagonists based on a thiophene scaffold and containing an acylguanidine as an Arg-mimetic is described. A number of structural features, such as cyclic versus open guanidine and a variety of lipophilic side chains, carbamates, sulfonamides and beta-...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-08, Vol.11 (15), p.2011-2015
Hauptverfasser:	Peyman, A, Scheunemann, K, Will, D W, Knolle, J, Wehner, V, Breipohl, G, Stilz, H U, Carniato, D, Ruxer, J, Gourvest, J, Auberval, M, Doucet, B, Baron, R, Gaillard, M, Gadek, T R, Bodary, S
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding Sites - drug effects Binding Sites - physiology Carbamates - chemistry Cell Adhesion - drug effects Cell Adhesion - physiology Cells, Cultured Disease Models, Animal Dose-Response Relationship, Drug Guanidine - chemistry Osteoporosis - prevention & control Parathyroidectomy Platelet Glycoprotein GPIIb-IIIa Complex - chemistry Platelet Glycoprotein GPIIb-IIIa Complex - metabolism Rats Receptors, Vitronectin - antagonists & inhibitors Receptors, Vitronectin - metabolism Sensitivity and Specificity Sulfonamides - chemistry Thiophenes - chemical synthesis Thiophenes - pharmacology Thyroidectomy
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Beschreibung
Zusammenfassung:	A series of novel, highly potent alpha(v)beta(3) antagonists based on a thiophene scaffold and containing an acylguanidine as an Arg-mimetic is described. A number of structural features, such as cyclic versus open guanidine and a variety of lipophilic side chains, carbamates, sulfonamides and beta-amino acids were explored with respect to inhibition of alpha(v)beta(3) mediated cell adhesion and selectivity versus alpha(IIb)beta(3) binding. In addition, compound 19 was found to be active in the TPTX model of osteoporosis.
ISSN:	0960-894X
DOI:	10.1016/S0960-894X(01)00357-2