DSpace at KIST: Design, synthesis, and biological evaluation of 1,3-dioxoisoindoline-5-carboxamide derivatives as T-type calcium channel blockers

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Design, synthesis, and biological evaluation of 1,3-dioxoisoindoline-5-carboxamide derivatives as T-type calcium channel blockers

Authors: Kim, Hwa Sil; Kim, Yoonjee; Doddareddy, Munikumar Reddy; Seo, Seon Hee; Rhim, Hyewhon; Tae, Jinsung; Pae, Ae Nim; Choo, Hyunah; Cho, Yong Seo

Issue Date: 2007-01-15

Publisher: PERGAMON-ELSEVIER SCIENCE LTD

Citation: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.17, no.2, pp.476 - 481

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 mu M, respectively. (c) 2006 Elsevier Ltd. All rights reserved.

Keywords: CA2+ CHANNELS; ETHOSUXIMIDE; PAIN; CA2+ CHANNELS; ETHOSUXIMIDE; PAIN; T-type calcium channel blockers; 1,3-dioxoisoindoline-5-carboxamides; pharmacophore model

ISSN: 0960-894X

URI: https://pubs.kist.re.kr/handle/201004/134733

DOI: 10.1016/j.bmcl.2006.10.042

Appears in Collections:: KIST Article > 2007

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