title: Hit-to-Lead studies: the discovery of potent, orally bioavailable thiazolopyrimidine CXCR2 receptor antagonists.
abstract: A Hit-to-Lead optimisation programme was carried out on a high throughput screening hit, the thiazolopyrimidine 1, resulting in the discovery of the potent, orally bioavailable CXCR2 antagonist 29.
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: Anne
authors.initials: A
authors.lastname: Cooper
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Kinchin
authors.forename: Kerry
authors.initials: K
authors.lastname: Moakes
authors.forename: John
authors.initials: J
authors.lastname: Unitt
authors.forename: Alan
authors.initials: A
authors.lastname: Wallace
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004353:Drug Evaluation, Preclinical / Q000379:methods; D022781:Hepatocytes / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D008861:Microsomes / Q000187:drug effects / Q000378:metabolism; D015394:Molecular Structure; D011743:Pyrimidines / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D023063:Receptors, Interleukin-8B / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D011743:Pyrimidines; D023063:Receptors, Interleukin-8B; D013844:Thiazoles