Hit-to-lead studies: the discovery of potent, orally bioavailable triazolethiol CXCR2 receptor antagonists

Andrew Baxter; Colin Bennion; Janice Bent; Kerry Boden; Steve Brough; Anne Cooper; Elizabeth Kinchin; Nicholas Kindon; Tom McInally; Mike Mortimore; Bryan Roberts; John Unitt

doi:10.1016/s0960-894x(03)00561-4

Hit-to-lead studies: the discovery of potent, orally bioavailable triazolethiol CXCR2 receptor antagonists

Bioorg Med Chem Lett. 2003 Aug 18;13(16):2625-8. doi: 10.1016/s0960-894x(03)00561-4.

Authors

Andrew Baxter¹, Colin Bennion, Janice Bent, Kerry Boden, Steve Brough, Anne Cooper, Elizabeth Kinchin, Nicholas Kindon, Tom McInally, Mike Mortimore, Bryan Roberts, John Unitt

Affiliation

¹ AstraZeneca R&D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK. andrew.jg.baxter@astrazeneca.com

PMID: 12873480
DOI: 10.1016/s0960-894x(03)00561-4

Abstract

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.

MeSH terms

Administration, Oral
Animals
Chemokines / antagonists & inhibitors
Chemokines / metabolism
Chemokines / pharmacology
Combinatorial Chemistry Techniques
Databases, Factual
Humans
Molecular Structure
Rats
Receptors, Interleukin-8B / antagonists & inhibitors*
Receptors, Interleukin-8B / chemistry
Receptors, Interleukin-8B / metabolism
Structure-Activity Relationship
Triazoles / chemical synthesis
Triazoles / metabolism
Triazoles / pharmacology*

Substances

Chemokines
Receptors, Interleukin-8B
Triazoles