title: Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore.
abstract: Structures containing the (R)-3-amino-3-methyl piperidine unit as a new pharmacophore moiety have been shown to possess moderate inhibitory activity for DPP-4 with good pharmacokinetics profile. One of these compounds was found to have good oral bioavailability and PK/PD profile in ZF-rat.
authors.affiliation: Drug Research Division, Dainippon Sumitomo Pharma Co., Ltd, Konohana-ku, Osaka, Japan. yukihiro-nishio@ds-pharma.co.jp
authors.forename: Yukihiro
authors.initials: Y
authors.lastname: Nishio
authors.forename: Hidenori
authors.initials: H
authors.lastname: Kimura
authors.forename: Shinya
authors.initials: S
authors.lastname: Tosaki
authors.forename: Eiji
authors.initials: E
authors.lastname: Sugaru
authors.forename: Mutsuko
authors.initials: M
authors.lastname: Sakai
authors.forename: Masakuni
authors.initials: M
authors.lastname: Horiguchi
authors.forename: Yumi
authors.initials: Y
authors.lastname: Masui
authors.forename: Michiko
authors.initials: M
authors.lastname: Ono
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Nakagawa
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Nakahira
mesh_terms: D000818:Animals; D018819:Dipeptidyl Peptidase 4 / Q000737:chemistry* / Q000378:metabolism; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008862:Microsomes, Liver / Q000378:metabolism; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: C556340:(R)-3-amino-3-methylpiperidine; D054873:Dipeptidyl-Peptidase IV Inhibitors; D010880:Piperidines; D011744:Pyrimidinones; D018819:Dipeptidyl Peptidase 4