Title
Synthesis of some new C2 substituted dihydropyrimidines and their electrophysiological evaluation as L-/T-type calcium channel blockers
Document Type
Article
Publication Date
7-1-2019
Abstract
Drugs targeting different calcium channel subtypes have strong therapeutic potential for future drug development for cardiovascular disorders, neuropsychiatric diseases and cancer. This study aims to design and synthesize a new series of C2 substituted dihydropyrimidines to mimic the structure features of third generation long acting dihydropyridine calcium channel blockers and dihydropyrimidines analogues. The target compounds have been evaluated as blockers for Ca1.2 and Ca3.2 utilizing the whole-cell patch clamp technique. Among the tested compounds, compound 7a showed moderate calcium channel blockade activity against Ca3.2. Moreover, the predicted physicochemical properties and pharmacokinetic profiles of the target compounds recommend that they can be considered as drug-like candidates. The results highlight some significant information for the future design of lead compounds as calcium channel blockers.
Publication Source (Journal or Book title)
Bioorganic chemistry
First Page
102915
Recommended Citation
Teleb, M., Rizk, O. H., Zhang, F., Fronczek, F. R., Zamponi, G. W., & Fahmy, H. (2019). Synthesis of some new C2 substituted dihydropyrimidines and their electrophysiological evaluation as L-/T-type calcium channel blockers. Bioorganic chemistry, 88, 102915. https://doi.org/10.1016/j.bioorg.2019.04.009