1,4-Dihydropyridine Scaffold in Medicinal Chemistry, The Story so Far And Perspectives (Part 1): Action in Ion Channels and GPCRs

Title: 1,4-Dihydropyridine Scaffold in Medicinal Chemistry, The Story so Far And Perspectives (Part 1): Action in Ion Channels and GPCRs

Volume: 18 Issue: 32

Author(s): P. Ioan, E. Carosati, M. Micucci, G. Cruciani, F. Broccatelli, B. S. Zhorov, A. Chiarini and R. Budriesi

Affiliation:

Keywords: 1,4-Dihydropyridines, 4-DHPs, 1,4-Dihydropyridine scaffold, Ion Channels, G-protein coupled receptors, modulators, therapeutic applications, multi-target ligand, Voltage-Gated Calcium Channels, Ligand-Gated Ion Channels, Calcium antagonists, L-Type Calcium Channel blockers

Abstract: Since the pioneering studies of Fleckenstein and co-workers, L-Type Calcium Channel (LTCC) blockers have attracted large interest due to their effectiveness in treating several cardiovascular diseases. Medicinal chemists achieved high potency and tissue selectivity by decorating the 1-4-DHP nucleus, the most studied scaffold among LTCC blockers. Nowadays it is clear that the 1,4-DHP nucleus is a privileged scaffold since, when appropriately substituted, it can selectively modulate diverse receptors, channels and enzymes. Therefore, the 1,4-DHP scaffold could be used to treat various diseases by a single-ligand multi-target approach. In this review, we describe the structure-activity relationships of 1,4-DHPs at ion channels, G-protein coupled receptors, and outline the potential for future therapeutic applications.

Cite this article as:

Ioan P., Carosati E., Micucci M., Cruciani G., Broccatelli F., S. Zhorov B., Chiarini A. and Budriesi R., 1,4-Dihydropyridine Scaffold in Medicinal Chemistry, The Story so Far And Perspectives (Part 1): Action in Ion Channels and GPCRs, Current Medicinal Chemistry 2011; 18 (32) . https://dx.doi.org/10.2174/092986711797535173