title: Discovery of novel and potent CRTH2 antagonists.
abstract: High throughput screening of our chemical library for CRTH2 antagonists provided a lead compound 1a. Initial optimization of the lead led to the discovery of a novel, potent and orally bioavailable CRTH2 antagonist 17.
authors.affiliation: Chemistry Research Labs, Drug Discovery Research, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan.
authors.forename: Shinji
authors.initials: S
authors.lastname: Ito
authors.forename: Tadashi
authors.initials: T
authors.lastname: Terasaka
authors.forename: Tatsuya
authors.initials: T
authors.lastname: Zenkoh
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Matsuda
authors.forename: Hisashi
authors.initials: H
authors.lastname: Hayashida
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Nagata
authors.forename: Yoshimasa
authors.initials: Y
authors.lastname: Imamura
authors.forename: Miki
authors.initials: M
authors.lastname: Kobayashi
authors.forename: Makoto
authors.initials: M
authors.lastname: Takeuchi
authors.forename: Mitsuaki
authors.initials: M
authors.lastname: Ohta
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D006168:Guinea Pigs; D057809:HEK293 Cells; D006801:Humans; D015394:Molecular Structure; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C036293:prostaglandin D2 receptor