Open Access Open Access  Restricted Access Subscription Access

SYNTHESIS AND EVALUATION OF REDUCING CAPACITY AND CALCIUM CHANNEL BLOCKING ACTIVITY OF NOVEL 3,5-DIPROPARGYLCARBONYL-SUBSTITUTED 1,4-DIHYDROPYRIDINES

M. Rucins, M. Gosteva, I. Domracheva, I. Kanepe-Lapsa, S. Belyakov, M. Plotniece, K. Pajuste, B. Cekavicus, M. Jekabsone, A. Sobolev, I. Shestakova, A. Plotniece
Cover Image

Abstract


Novel pyridinium salts on the basis of 4-(3-pyridyl)-3,5-dipropargylcarbonyl-1,4-dihydropyridine were obtained by quaternization of pyridine moiety with different alkyl halides. The reducing capacity of the synthesized compounds was evaluated using phosphomolybdenum complex method. The obtained results confirmed that all tested compounds possessed reducing capacity. Ca2+ channel antagonist and agonist activities of the compounds were additionaly assayed by changes in intracellular Ca2+ ion concentration in H9C2 and A7R5 cell lines. The obtained data confirmed that all synthesized 1,4-dihydropyridine derivatives have smooth muscle selective antagonist activities, and in the case of 4-phenyl derivative the activity was 4.7 times higher than that of amlodipine.

How to Cite
Rucins, M.; Gosteva, M.; Domracheva, I.; Kanepe-Lapsa, I.; Belyakov, S.; Plotniece, M.; Pajuste, K.; Cekavicus, B.; Jekabsone, M.; Sobolev, A.; Shestakova, I.; Plotniece, А. Chem. Heterocycl. Compd. 2015, 50, 1432. [Khim. Geterotsikl. Soedin. 2014, 1557.]

For this article in the English edition see DOI 10.1007/s10593-014-1607-z


Keywords


N-alkylpyridinium; 1,4-dihydropyridines; calcium antagonists; Hantzsch synthesis; quaternization; reducing capacity

Full Text: PDF Supplementary File(s): None


 

 

Latvian Institute of Organic Synthesis - Aizkraukles iela, 21, Riga, LV-1006, Latvia - hgs@osi.lv