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Synthesis and SAR study of T-type calcium channel blockers. Part II.
Arch Pharm (Weinheim). 2008 Oct; 341(10):661-4.AP

Abstract

3,4-Dihydroquinazoline derivatives have been known to be the novel and potent T-type calcium channel blockers. From a systematic variation of 3,4-dihydroquinazoline derivative 5c (KYS05043), plausible SAR results were established. It was revealed that a 5-(dimethylamino)pentylamino group at R(1), a biphenyl group at R(2), and a benzyl amido group at R(3)in the 3,4-dihydroquinazoline backbone are closely related with the channel selectivity (T/N-type) as well as the potency based on the discovery of 6k (KYS05090).

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Publisher Full Text (DOI)

Authors+Show Affiliations

Choe YJ
Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul, Korea.
Seo HN
No affiliation info available
Jung SY
No affiliation info available
Rhim H
No affiliation info available
Kim J
No affiliation info available
Choo DJ
No affiliation info available
Lee JY
No affiliation info available

MeSH

Calcium Channel BlockersCalcium Channels, T-TypeCell LineDrug DesignHumansMolecular StructureQuinazolinesStructure-Activity Relationship

Pub Type(s)

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

Language

eng

PubMed ID

18816587

Citation

Choe, Yun Jeong, et al. "Synthesis and SAR Study of T-type Calcium Channel Blockers. Part II." Archiv Der Pharmazie, vol. 341, no. 10, 2008, pp. 661-4.
Choe YJ, Seo HN, Jung SY, et al. Synthesis and SAR study of T-type calcium channel blockers. Part II. Arch Pharm (Weinheim). 2008;341(10):661-4.
Choe, Y. J., Seo, H. N., Jung, S. Y., Rhim, H., Kim, J., Choo, D. J., & Lee, J. Y. (2008). Synthesis and SAR study of T-type calcium channel blockers. Part II. Archiv Der Pharmazie, 341(10), 661-4. https://doi.org/10.1002/ardp.200800079
Choe YJ, et al. Synthesis and SAR Study of T-type Calcium Channel Blockers. Part II. Arch Pharm (Weinheim). 2008;341(10):661-4. PubMed PMID: 18816587.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and SAR study of T-type calcium channel blockers. Part II. AU - Choe,Yun Jeong, AU - Seo,Han Na, AU - Jung,Soo Yeon, AU - Rhim,Hyewhon, AU - Kim,Jungahn, AU - Choo,Dong Joon, AU - Lee,Jae Yeol, PY - 2008/9/26/pubmed PY - 2008/12/17/medline PY - 2008/9/26/entrez SP - 661 EP - 4 JF - Archiv der Pharmazie JO - Arch Pharm (Weinheim) VL - 341 IS - 10 N2 - 3,4-Dihydroquinazoline derivatives have been known to be the novel and potent T-type calcium channel blockers. From a systematic variation of 3,4-dihydroquinazoline derivative 5c (KYS05043), plausible SAR results were established. It was revealed that a 5-(dimethylamino)pentylamino group at R(1), a biphenyl group at R(2), and a benzyl amido group at R(3)in the 3,4-dihydroquinazoline backbone are closely related with the channel selectivity (T/N-type) as well as the potency based on the discovery of 6k (KYS05090). SN - 1521-4184 UR - https://www.unboundmedicine.com/medline/citation/18816587/Synthesis_and_SAR_study_of_T_type_calcium_channel_blockers__Part_II_ L2 - https://doi.org/10.1002/ardp.200800079 DB - PRIME DP - Unbound Medicine ER -