Facile synthesis and biological evaluation of 3,3-diphenylpropanoyl piperazines as T-type calcium channel blockers

Yeon-hee Choi; Du Jong Baek; Seon Hee Seo; Jae Kyun Lee; Ae Nim Pae; Yong Seo Cho; Sun-Joon Min

doi:10.1016/j.bmcl.2010.11.033

Facile synthesis and biological evaluation of 3,3-diphenylpropanoyl piperazines as T-type calcium channel blockers

Bioorg Med Chem Lett. 2011 Jan 1;21(1):215-9. doi: 10.1016/j.bmcl.2010.11.033. Epub 2010 Nov 12.

Authors

Yeon-hee Choi¹, Du Jong Baek, Seon Hee Seo, Jae Kyun Lee, Ae Nim Pae, Yong Seo Cho, Sun-Joon Min

Affiliation

¹ Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongyang, Seoul 130-650, Republic of Korea.

PMID: 21126876
DOI: 10.1016/j.bmcl.2010.11.033

Abstract

We have developed a facile synthesis of 3,3-diphenylpropanamides using Meldrum's acid derivatives as amide coupling components. The in vitro biological evaluation of the title compounds led to the identification of compound 1h, which has good inhibitory activity against T-type calcium channel (IC(50) = 0.83 μM).

Publication types

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

MeSH terms

Benzhydryl Compounds / chemical synthesis*
Benzhydryl Compounds / chemistry
Benzhydryl Compounds / pharmacology
Calcium Channel Blockers / chemical synthesis*
Calcium Channel Blockers / chemistry
Calcium Channel Blockers / pharmacology
Calcium Channels, T-Type / chemistry*
Calcium Channels, T-Type / metabolism
ERG1 Potassium Channel
Ether-A-Go-Go Potassium Channels / antagonists & inhibitors
Ether-A-Go-Go Potassium Channels / metabolism
High-Throughput Screening Assays
Humans
Piperazines / chemical synthesis
Piperazines / chemistry*
Piperazines / pharmacology
Structure-Activity Relationship

Substances

Benzhydryl Compounds
Calcium Channel Blockers
Calcium Channels, T-Type
ERG1 Potassium Channel
Ether-A-Go-Go Potassium Channels
Piperazines