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Synthesis and SAR studies of a novel series of T-type calcium channel blockers.
Bioorg Med Chem. 2006 May 15; 14(10):3502-11.BM

Abstract

For the novel, potent, and selective T-type Ca2+ channel blockers, a series of sulfonamido-containing 3,4-dihydroquinazoline derivatives were prepared and evaluated for their blocking actions on T- and N-type Ca2+ channels. Among them, 9c (KYS05064, IC50 = 0.96 +/- 0.22 microM) was found to be as potent as Mibefradil and also showed the highest selectivity for T-type Ca2+ channel with no effect on N-type Ca2+ channel.

Authors+Show Affiliations

Park SJ
Life Sciences Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
Park SJ
No affiliation info available
Lee MJ
No affiliation info available
Rhim H
No affiliation info available
Kim Y
No affiliation info available
Lee JH
No affiliation info available
Chung BY
No affiliation info available
Lee JY
No affiliation info available

MeSH

Calcium Channel BlockersCalcium Channels, N-TypeCalcium Channels, T-TypeCell LineCells, CulturedElectrophysiologyHumansLethal Dose 50MibefradilMolecular StructureQuantitative Structure-Activity RelationshipQuinazolinesSulfonamides

Pub Type(s)

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

Language

eng

PubMed ID

16434203

Citation

Park, Seong Jun, et al. "Synthesis and SAR Studies of a Novel Series of T-type Calcium Channel Blockers." Bioorganic & Medicinal Chemistry, vol. 14, no. 10, 2006, pp. 3502-11.
Park SJ, Park SJ, Lee MJ, et al. Synthesis and SAR studies of a novel series of T-type calcium channel blockers. Bioorg Med Chem. 2006;14(10):3502-11.
Park, S. J., Park, S. J., Lee, M. J., Rhim, H., Kim, Y., Lee, J. H., Chung, B. Y., & Lee, J. Y. (2006). Synthesis and SAR studies of a novel series of T-type calcium channel blockers. Bioorganic & Medicinal Chemistry, 14(10), 3502-11.
Park SJ, et al. Synthesis and SAR Studies of a Novel Series of T-type Calcium Channel Blockers. Bioorg Med Chem. 2006 May 15;14(10):3502-11. PubMed PMID: 16434203.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and SAR studies of a novel series of T-type calcium channel blockers. AU - Park,Seong Jun, AU - Park,Sung Jun, AU - Lee,Min Joo, AU - Rhim,Hyewhon, AU - Kim,Yoonjee, AU - Lee,Jung-Ha, AU - Chung,Bong Young, AU - Lee,Jae Yeol, Y1 - 2006/01/24/ PY - 2005/12/12/received PY - 2005/12/30/revised PY - 2006/01/04/accepted PY - 2006/1/26/pubmed PY - 2006/8/9/medline PY - 2006/1/26/entrez SP - 3502 EP - 11 JF - Bioorganic & medicinal chemistry JO - Bioorg Med Chem VL - 14 IS - 10 N2 - For the novel, potent, and selective T-type Ca2+ channel blockers, a series of sulfonamido-containing 3,4-dihydroquinazoline derivatives were prepared and evaluated for their blocking actions on T- and N-type Ca2+ channels. Among them, 9c (KYS05064, IC50 = 0.96 +/- 0.22 microM) was found to be as potent as Mibefradil and also showed the highest selectivity for T-type Ca2+ channel with no effect on N-type Ca2+ channel. SN - 0968-0896 UR - https://www.unboundmedicine.com/medline/citation/16434203/Synthesis_and_SAR_studies_of_a_novel_series_of_T_type_calcium_channel_blockers_ DB - PRIME DP - Unbound Medicine ER -