title: Design, synthesis, and biological evaluation of 1,3-dioxoisoindoline-5-carboxamide derivatives as T-type calcium channel blockers.
abstract: A small molecule library of 1,3-dioxoisoindoline-5-carboxamides 4 was designed based on the pharmacophore model, synthesized and biologically evaluated as potential T-type calcium channel blockers. The most active compounds 4d and 4n show T-type calcium channel blocking activity with IC50 values of 0.93 and 0.96 microM, respectively.
authors.affiliation: Life Sciences Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
authors.forename: Hwa Sil
authors.initials: HS
authors.lastname: Kim
authors.forename: Yoonjee
authors.initials: Y
authors.lastname: Kim
authors.forename: Munikumar Reddy
authors.initials: MR
authors.lastname: Doddareddy
authors.forename: Seon Hee
authors.initials: SH
authors.lastname: Seo
authors.forename: Hyewhon
authors.initials: H
authors.lastname: Rhim
authors.forename: Jinsung
authors.initials: J
authors.lastname: Tae
authors.forename: Ae Nim
authors.initials: AN
authors.lastname: Pae
authors.forename: Hyunah
authors.initials: H
authors.lastname: Choo
authors.forename: Yong Seo
authors.initials: YS
authors.lastname: Cho
mesh_terms: D000577:Amides / Q000737:chemistry* / Q000494:pharmacology*; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology*; D020747:Calcium Channels, T-Type / Q000187:drug effects*; D002460:Cell Line; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006801:Humans; D007202:Indicators and Reagents; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D008564:Membrane Potentials / Q000187:drug effects; D020748:Mibefradil / Q000494:pharmacology; D008958:Models, Molecular; D018408:Patch-Clamp Techniques
chemical_list: C518624:1,3-dioxoisoindoline-5-carboxamide; D000577:Amides; D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type; D007202:Indicators and Reagents; D007211:Indoles; D020748:Mibefradil