Hit-to-Lead studies: The discovery of potent, orally bioavailable triazolethiol CXCR2 receptor antagonists

A Hit-to-Lead optimisation programme was carried out on the high throughput screening hit, the triazolethiol 1, resulting in the discovery of the potent, orally bioavailable triazolethiol CXCR2 receptor antagonist 45. A Hit-to-Lead programme was carried out resulting in the discovery of the potent,...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-08, Vol.13 (16), p.2625-2628
Hauptverfasser:	Baxter, Andrew, Bennion, Colin, Bent, Janice, Boden, Kerry, Brough, Steve, Cooper, Anne, Kinchin, Elizabeth, Kindon, Nicholas, McInally, Tom, Mortimore, Mike, Roberts, Bryan, Unitt, John
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Biological and medical sciences Chemokines - antagonists & inhibitors Chemokines - metabolism Chemokines - pharmacology Combinatorial Chemistry Techniques Databases, Factual Humans Immunomodulators Medical sciences Molecular Structure Pharmacology. Drug treatments Rats Receptors, Interleukin-8B - antagonists & inhibitors Receptors, Interleukin-8B - chemistry Receptors, Interleukin-8B - metabolism Structure-Activity Relationship Triazoles - chemical synthesis Triazoles - metabolism Triazoles - pharmacology
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Zusammenfassung:	A Hit-to-Lead optimisation programme was carried out on the high throughput screening hit, the triazolethiol 1, resulting in the discovery of the potent, orally bioavailable triazolethiol CXCR2 receptor antagonist 45. A Hit-to-Lead programme was carried out resulting in the discovery of the potent, orally bioavailable CXCR2 antagonist 45.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00561-4