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

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

doi:10.1016/j.bmcl.2006.10.042

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

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

Department of Chemistry

Research output: Contribution to journal › Article › peer-review

21 Citations (Scopus)

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 μM, respectively.

Original language	English
Pages (from-to)	476-481
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	2
DOIs	https://doi.org/10.1016/j.bmcl.2006.10.042
Publication status	Published - 2007 Jan 15

Bibliographical note

Funding Information:
This work was supported by Korea Institute of Science and Technology (2E18970).

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2006.10.042

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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 μM, respectively.",

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AU - Kim, Hwa Sil

AU - Kim, Yoonjee

AU - Doddareddy, Munikumar Reddy

AU - Seo, Seon Hee

AU - Rhim, Hyewhon

AU - Tae, Jinsung

AU - Pae, Ae Nim

AU - Choo, Hyunah

AU - Cho, Yong Seo

N1 - Funding Information: This work was supported by Korea Institute of Science and Technology (2E18970).

PY - 2007/1/15

Y1 - 2007/1/15

N2 - 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 μM, respectively.

AB - 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 μM, respectively.

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

Abstract

Bibliographical note

All Science Journal Classification (ASJC) codes

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