Abstrait

Design, synthesis and calcium channel blocking activity of novel tetrahydropyrimidine derivatives for potential benefit in angina pectoris

Gang Liu, Yan-yan Liu, Yong-cun Hu

Aim: The present study deals with the discovery of some novel tetrahydropyrimidine derivatives for its possible effect on calcium channel blocking activity.

Methods: A novel series tetrahydropyrimidine derivatives were synthesized by simple and cost effective synthetic route. The structure of the synthesized derivatives was ascertained by the ¹H-NMR, ¹²C-NMR, mass, FT-IR and elemental analyses.

Results: Results revealed that, designed compounds effectively antagonises the Ca²⁺ in A7r5 cell than SH-SY5Y cells suggesting its specific modulation of L-type calcium channel as A7r5 cells are highly expressed for L-type calcium channel. Moreover, the results has been further substantiated by molecular docking study, where, the most active analogue 6a has been docked with AID-β complex of L-type calcium channel and showed Ki of 23.73 μM. The estimated free energy of binding was found to be -6.31 kcal/mol.

Conclusion: In the present study, we have discovered a novel tetrahydropyrimidine derivative by simple and cost effective synthetic route which able to effectively antagonise the Ca²⁺ in SH-SY5Y and A7r5 cells in comparison to standard drug.