Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Calcium Level Controlling Activities of Novel Derivatives of Amlodipine,Riodipine and Cerebrocrast

Author(s): R. Vilskersts, B. Vigante, Z. Neidere, A. Krauze, I. Domracheva, L. Bekere, I. Shestakova, G. Duburs, M. Dambrova.


A novel series of asymmetric 4-aryl-1,4-dihydropyridine (1,4-DHP) 3,5-diester derivatives and their symmetric analogues comprised of functional moieties of amlodipine, riodipine and cerebrocrast have been synthesized. The calcium channel blocking activity was evaluated in an isolated rat aortic ring model. The calcium overload preventing activity was tested in SH-SY5Y neuroblastoma cell line by a fluorescence-based calcium assay. Among synthesized and tested compounds, 4a showed the highest calcium overload preventing activity (IC50=39μM) and 7e demonstrated the highest calcium channel inhibiting activity (EC50=0.2 nM). Asymmetric ester 7a exerted both substantial calcium channel blocking and calcium overload preventing activity.

Keywords: Amlodipine, Asymmetric 1,4-dihydropyridines, Calcium channel antagonists, Cerebrocrast, Riodipine, 1,4-DHP, Calcium Level, Cardiovascular diseases, Varian Mercury, apoptosis, neuroprotective propertie, antihypertensive agents, NMR spectra, Aortic Ring Experiment

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Article Details

Year: 2012
Page: [322 - 328]
Pages: 7
DOI: 10.2174/157018012799129909
Price: $58