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

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 (IC50=...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2011-01, Vol.21 (1), p.215-219
Main Authors: Choi, Yeon-hee, Baek, Du Jong, Seo, Seon Hee, Lee, Jae Kyun, Pae, Ae Nim, Cho, Yong Seo, Min, Sun-Joon
Format: Article
Language:English
Subjects:
3,3-Diphenylpropanoyl piperazine
Benzhydryl Compounds - chemical synthesis
Benzhydryl Compounds - chemistry
Benzhydryl Compounds - pharmacology
Biological and medical sciences
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
HTS assays
Humans
Medical sciences
Meldrum’s acid
Miscellaneous
Neuropharmacology
Pharmacology. Drug treatments
Piperazines - chemical synthesis
Piperazines - chemistry
Piperazines - pharmacology
Structure-Activity Relationship
T-Type calcium channel blockers
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Summary: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 (IC50=0.83μM).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.11.033