Biomedical Research

All submissions of the EM system will be redirected to Online Manuscript Submission System. Authors are requested to submit articles directly to Online Manuscript Submission System of respective journal.
Reach Us +1 504 6082390

Research Article - Biomedical Research (2017) Volume 28, Issue 3

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

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.

Author(s): Gang Liu, Yan-yan Liu, Yong-cun Hu

Abstract Full Text PDF