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Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Bioorg Med Chem. 2007 Jan 01; 15(1):365-73.BM

Abstract

T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pains. Since the withdrawal of mibefradil, a T-type calcium channel blocker, there have been a lot of efforts to develop T-type calcium channel blockers. A small molecule library of dioxoquinazoline carboxamide derivatives containing 155 compounds was designed, synthesized, and biologically evaluated for T-type calcium channel blocking activity. Among those compounds synthesized, the compound 1n shows the most potent T-type calcium current blocking activity with an IC(50) value of 1.52 microM, which is comparable to that of mibefradil.

Authors+Show Affiliations

Jo MN
Life Sciences Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
Seo HJ
No affiliation info available
Kim Y
No affiliation info available
Seo SH
No affiliation info available
Rhim H
No affiliation info available
Cho YS
No affiliation info available
Cha JH
No affiliation info available
Koh HY
No affiliation info available
Choo H
No affiliation info available
Pae AN
No affiliation info available

MeSH

AmidesCalcium Channel BlockersCalcium Channels, T-TypeCell LineDrug DesignDrug Evaluation, PreclinicalHumansMolecular StructureQuinazolinesStereoisomerismStructure-Activity Relationship

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17035033

Citation

Jo, Mi Na, et al. "Novel T-type Calcium Channel Blockers: Dioxoquinazoline Carboxamide Derivatives." Bioorganic & Medicinal Chemistry, vol. 15, no. 1, 2007, pp. 365-73.
Jo MN, Seo HJ, Kim Y, et al. Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. Bioorg Med Chem. 2007;15(1):365-73.
Jo, M. N., Seo, H. J., Kim, Y., Seo, S. H., Rhim, H., Cho, Y. S., Cha, J. H., Koh, H. Y., Choo, H., & Pae, A. N. (2007). Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. Bioorganic & Medicinal Chemistry, 15(1), 365-73.
Jo MN, et al. Novel T-type Calcium Channel Blockers: Dioxoquinazoline Carboxamide Derivatives. Bioorg Med Chem. 2007 Jan 1;15(1):365-73. PubMed PMID: 17035033.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. AU - Jo,Mi Na, AU - Seo,Hee Jeong, AU - Kim,Yoonji, AU - Seo,Seon Hee, AU - Rhim,Hyewhon, AU - Cho,Yong Seo, AU - Cha,Joo Hwan, AU - Koh,Hun Yeong, AU - Choo,Hyunah, AU - Pae,Ae Nim, Y1 - 2006/10/10/ PY - 2006/07/31/received PY - 2006/09/22/revised PY - 2006/09/23/accepted PY - 2006/10/13/pubmed PY - 2007/2/21/medline PY - 2006/10/13/entrez SP - 365 EP - 73 JF - Bioorganic & medicinal chemistry JO - Bioorg Med Chem VL - 15 IS - 1 N2 - T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pains. Since the withdrawal of mibefradil, a T-type calcium channel blocker, there have been a lot of efforts to develop T-type calcium channel blockers. A small molecule library of dioxoquinazoline carboxamide derivatives containing 155 compounds was designed, synthesized, and biologically evaluated for T-type calcium channel blocking activity. Among those compounds synthesized, the compound 1n shows the most potent T-type calcium current blocking activity with an IC(50) value of 1.52 microM, which is comparable to that of mibefradil. SN - 0968-0896 UR - https://www.unboundmedicine.com/medline/citation/17035033/Novel_T_type_calcium_channel_blockers:_dioxoquinazoline_carboxamide_derivatives_ DB - PRIME DP - Unbound Medicine ER -