title: Hit-to-lead studies: the discovery of potent, orally bioavailable triazolethiol CXCR2 receptor antagonists.
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.
authors.affiliation: AstraZeneca R&D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK. andrew.jg.baxter@astrazeneca.com
authors.forename: Andrew
authors.initials: A
authors.lastname: Baxter
authors.forename: Colin
authors.initials: C
authors.lastname: Bennion
authors.forename: Janice
authors.initials: J
authors.lastname: Bent
authors.forename: Kerry
authors.initials: K
authors.lastname: Boden
authors.forename: Steve
authors.initials: S
authors.lastname: Brough
authors.forename: Anne
authors.initials: A
authors.lastname: Cooper
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Kinchin
authors.forename: Nicholas
authors.initials: N
authors.lastname: Kindon
authors.forename: Tom
authors.initials: T
authors.lastname: McInally
authors.forename: Mike
authors.initials: M
authors.lastname: Mortimore
authors.forename: Bryan
authors.initials: B
authors.lastname: Roberts
authors.forename: John
authors.initials: J
authors.lastname: Unitt
mesh_terms: D000284:Administration, Oral; D000818:Animals; D018925:Chemokines / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D016208:Databases, Factual; D006801:Humans; D015394:Molecular Structure; D051381:Rats; D023063:Receptors, Interleukin-8B / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D018925:Chemokines; D023063:Receptors, Interleukin-8B; D014230:Triazoles