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

Authors

  • M. Rucins Latvian Institute of Organic Synthesis; Faculty of Medicine, University of Latvia
  • M. Gosteva Latvian Institute of Organic Synthesis
  • I. Domracheva Latvian Institute of Organic Synthesis
  • I. Kanepe-Lapsa Latvian Institute of Organic Synthesis
  • S. Belyakov Latvian Institute of Organic Synthesis
  • M. Plotniece Latvian Institute of Organic Synthesis
  • K. Pajuste Latvian Institute of Organic Synthesis
  • B. Cekavicus Latvian Institute of Organic Synthesis
  • M. Jekabsone Faculty of Medicine, University of Latvia
  • A. Sobolev Latvian Institute of Organic Synthesis
  • I. Shestakova Latvian Institute of Organic Synthesis
  • A. Plotniece Latvian Institute of Organic Synthesis

DOI:

https://doi.org/10.1007/1921

Keywords:

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

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

Author Biographies

M. Rucins, Latvian Institute of Organic Synthesis; Faculty of Medicine, University of Latvia

Martins Rucins

M. Gosteva, Latvian Institute of Organic Synthesis

Marina Gosteva

I. Domracheva, Latvian Institute of Organic Synthesis

Ilona Domracheva

I. Kanepe-Lapsa, Latvian Institute of Organic Synthesis

Iveta Kanepe-Lapsa

S. Belyakov, Latvian Institute of Organic Synthesis

Sergey Belyakov

M. Plotniece, Latvian Institute of Organic Synthesis

Mara Plotniece

K. Pajuste, Latvian Institute of Organic Synthesis

Karlis Pajuste

B. Cekavicus, Latvian Institute of Organic Synthesis

Brigita Cekavicus

M. Jekabsone, Faculty of Medicine, University of Latvia

Madara Jekabsone

A. Sobolev, Latvian Institute of Organic Synthesis

Arkadij Sobolev

I. Shestakova, Latvian Institute of Organic Synthesis

Irina Shestakova

A. Plotniece, Latvian Institute of Organic Synthesis

Aiva Plotniece

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Published

2014-10-28

Issue

No. 10 (2014)

Section

Original Papers