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Title: Search for angiotensin II receptor antagonists among 4-aryl-n-(aryl)-3-(prop-2-en-1-yl)-2,3- dihydro-1,3-thiazol-2-imine derivatives
Authors: Drapak, I. V.
Драпак, І. В.
Zimenkovsky, B. S.
Зіменковський, Б. С.
Perekhoda, L. O.
Перехода, Л. О.
Suleyman, M. M.
Сулейман, М. М.
Yeromina, H. O.
Єрьоміна, Г. О.
Skaletska, N.
Seredynska, N.
Demchenko, A. M.
Keywords: synthesis;4-aryl-N-(aryl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine derivatives;molecular docking;angiotensin receptor ІІ antagonists
Issue Date: 2019
Bibliographic description (Ukraine): Search for angiotensin II receptor antagonists among 4-aryl-N-(aryl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine derivatives / I. Drapak, B. Zimenkovsky, L. Perekhoda, М. Suleyman, H. Yeromina, N. Seredynska, N. Seredynska  A. Demchenko // Pharmacia. - 2019. - Vol. 66 (4). - Р. 181-186.  
Abstract: The aim of study was to find potential antihypertensive and cardiotropic drugs among new 4-aryl-N-(aryl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imines.
Description: In order to expand the arsenal of biologically active substances of cardiotropic action a systematic series of new 4-arylN-(aryl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine derivatives were synthesized. The structure and purity of the compounds synthesized were confirmed by 1 H, 13C NMR-spectroscopy and elemental analysis. Based on the results of docking studies using Autodock 4.2.6 software, selected compounds with the best affinity for protein biomes (PDB codes: 3R8A) are promising for experimental studies of hypotensive and cardiotropic activity. The most effective antihypertensive effect, which is similar in duration and strength of the effect of valsartan, was the effect of compound 3(5). A comparative analysis of the results of molecular docking and in vivo results suggests that there is a positive correlation between scoring protein inhibition and experimental data.
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