title: 5-Lipoxygenase inhibitors: convenient synthesis of 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues.
abstract: A convenient synthetic route to 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues as 5-LO inhibitors is described. This methodology enabled rapid development of structure-activity relationships (SARs) leading to improvement of pharmacological properties. Thus, new compounds with higher 5-LO inhibitory potency were discovered. The stereo-chemistry requirements of the tetrahydropyran ring are also discussed.
authors.affiliation: Pfizer Global Research & Development, Nagoya Laboratories, 5-2 Taketoyo, Aichi 470-2393, Japan. Takashi.Mano@pfizer.com
authors.forename: Takashi
authors.initials: T
authors.lastname: Mano
authors.forename: Rodney W
authors.initials: RW
authors.lastname: Stevens
authors.forename: Yoshiyuki
authors.initials: Y
authors.lastname: Okumura
authors.forename: Makoto
authors.initials: M
authors.lastname: Kawai
authors.forename: Takako
authors.initials: T
authors.lastname: Okumura
authors.forename: Minoru
authors.initials: M
authors.lastname: Sakakibara
mesh_terms: D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011714:Pyrans / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D016859:Lipoxygenase Inhibitors; D011714:Pyrans