Synthesis and Evaluation of Reducing Capacity and Calcium Channel Blocking Activity of Novel 3,5-Dipropargylcarbonyl-Substituted 1,4-Dihydropyridines

Химия гетероциклических соединений 2014
Martins Rucins, Marina Gosteva, Ilona Domracheva, Iveta Kanepe-Lapsa, Sergejs Beļakovs, Māra Plotniece, Kārlis Pajuste, Brigita Cekavicus, Madara Jekabsone, Arkadij Sobolev, Irina Shestakova, Aiva Plotniece

Novel pyridinium salts on the basis of 4-(3-pyridyl)-3,5-dipropargylcarbonyl-1,4-dihydropyridine were obtained by quaternisation 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. Callcium channel antagonist and agonist activities of the compounds were additionaly assayed by changes in intracellular calcium ion concentration in H9C2 and A7R5 cell lines. The obtained data confirmed that all synthesized 1,4-dihydropyridine derivatives have smouth muscle selective antagonist activities, and in the case of 4-phenyl derivative the activity was 4.7 times higher than that of amlodipine.

Atslēgas vārdi
1,4-DHP, alkylation, Calcium channel blocking activity, reducing capacity
Hipersaite
http://hgs.osi.lv/index.php/hgs/article/view/1921

Rucins, M., Gosteva, M., Domracheva, I., Kanepe-Lapsa, I., Beļakovs, S., Plotniece, M., Pajuste, K., Cekavicus, B., Jekabsone, M., Sobolev, A., Shestakova, I., Plotniece, A. Synthesis and Evaluation of Reducing Capacity and Calcium Channel Blocking Activity of Novel 3,5-Dipropargylcarbonyl-Substituted 1,4-Dihydropyridines. Химия гетероциклических соединений, 2014, N 10, 1557.-1568.lpp. ISSN 0132-6244.

Publikācijas valoda
English (en)