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Link to original content: https://pubmed.ncbi.nlm.nih.gov/24149495/
Synthesis and evaluation of 1,4-dihydropyridine derivatives with calcium channel blocking activity - PubMed Skip to main page content
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. 2014 Jul;466(7):1355-63.
doi: 10.1007/s00424-013-1376-z. Epub 2013 Oct 23.

Synthesis and evaluation of 1,4-dihydropyridine derivatives with calcium channel blocking activity

Chris Bladen  1 , Miyase Gözde Gündüz, Rahime Şimşek, Cihat Şafak, Gerald W Zamponi
Affiliations

Synthesis and evaluation of 1,4-dihydropyridine derivatives with calcium channel blocking activity

Chris Bladen et al. Pflugers Arch. 2014 Jul.

Abstract

1,4-Dihydropyridines (DHPs) are an important class of L-type calcium channel blockers that are used to treat conditions such as hypertension and angina. Their primary target in the cardiovascular system is the Cav1.2 L-type calcium channel isoform, however, a number of DHPs also block low-voltage-activated T-type calcium channels. Here, we describe the synthesis of a series of novel DHP derivatives that have a condensed 1,4-DHP ring system (hexahydroquinoline) and report on their abilities to block both L- and T-type calcium channels. Within this series of compounds, modification of a key ester moiety not only regulates the blocking affinity for both L- and T-type channels, but also allows for the development of DHPs with 30-fold selectivity for T-type channels over the L-type. Our data suggest that a condensed dihydropyridine-based scaffold may serve as a pharmacophore for a new class of T-type selective inhibitors.

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