title: Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists.
abstract: A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A2A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse catalepsy in mice when dosed orally.
authors.affiliation: Janssen Research & Development, LLC, Welsh and McKean Roads, PO Box 776, Spring House, PA 19477, USA. bshook@its.jnj.com
authors.forename: Brian C
authors.initials: BC
authors.lastname: Shook
authors.forename: Devraj
authors.initials: D
authors.lastname: Chakravarty
authors.forename: J Kent
authors.initials: JK
authors.lastname: Barbay
authors.forename: Aihua
authors.initials: A
authors.lastname: Wang
authors.forename: Kristi
authors.initials: K
authors.lastname: Leonard
authors.forename: Vernon
authors.initials: V
authors.lastname: Alford
authors.forename: Mark T
authors.initials: MT
authors.lastname: Powell
authors.forename: Stefanie
authors.initials: S
authors.lastname: Rassnick
authors.forename: Robert H
authors.initials: RH
authors.lastname: Scannevin
authors.forename: Karen
authors.initials: K
authors.lastname: Carroll
authors.forename: Nathaniel
authors.initials: N
authors.lastname: Wallace
authors.forename: Jeffrey
authors.initials: J
authors.lastname: Crooke
authors.forename: Mark
authors.initials: M
authors.lastname: Ault
authors.forename: Lisa
authors.initials: L
authors.lastname: Lampron
authors.forename: Lori
authors.initials: L
authors.lastname: Westover
authors.forename: Kenneth
authors.initials: K
authors.lastname: Rhodes
authors.forename: Paul F
authors.initials: PF
authors.lastname: Jackson
mesh_terms: D058917:Adenosine A2 Receptor Antagonists / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D000818:Animals; D001921:Brain / Q000378:metabolism; D002375:Catalepsy / Q000188:drug therapy; D006207:Half-Life; D006801:Humans; D007700:Kinetics; D051379:Mice; D011485:Protein Binding; D011743:Pyrimidines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D051381:Rats; D043705:Receptor, Adenosine A2A / Q000737:chemistry / Q000378:metabolism*
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D011743:Pyrimidines; D043705:Receptor, Adenosine A2A