Synthesis and Cardiotropic Activity of Linear Methoxyphenyltriazaalkanes
- Authors: Mokrov G.V.1, Likhosherstov A.M.1, Barchukov V.V.1, Stolyaruk V.N.1, Tsorin I.B.1, Vititnova M.B.1, Kryzhanovskii S.A.1, Gudasheva T.A.1, Seredenin S.B.1
 - 
							Affiliations: 
							
- V. V. Zakusov State Institute of Pharmacology
 
 - Issue: Vol 53, No 6 (2019)
 - Pages: 500-506
 - Section: Article
 - URL: https://journals.rcsi.science/0091-150X/article/view/245832
 - DOI: https://doi.org/10.1007/s11094-019-02027-7
 - ID: 245832
 
Cite item
Abstract
A new group of potential pFOX inhibitors among linear methoxyphenyltriazaalkanes were designed and synthesized. Cardiotropic activity in rodent experiments was found for most of the synthesized compounds. The most active compound N1-(2,3,4-trimethoxybenzyl)-N2-{2-[(2,3,4-trimethoxybenzyl)amino]ethyl}-1,2-ethanediamine trihydrochloride (LM-1) combined anti-ischemic, antiarrhythmic, and antifibrillatory activities (1 mg/kg, i.v.) and low toxicity (LD50 = 119 mg/kg, mice, i.p.) and was selected for development as a potential cardiotropic drug.
About the authors
G. V. Mokrov
V. V. Zakusov State Institute of Pharmacology
							Author for correspondence.
							Email: g.mokrov@gmail.com
				                					                																			                												                	Russian Federation, 							8 Baltiiskaya St., Moscow, 125315						
A. M. Likhosherstov
V. V. Zakusov State Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Russian Federation, 							8 Baltiiskaya St., Moscow, 125315						
V. V. Barchukov
V. V. Zakusov State Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Russian Federation, 							8 Baltiiskaya St., Moscow, 125315						
V. N. Stolyaruk
V. V. Zakusov State Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Russian Federation, 							8 Baltiiskaya St., Moscow, 125315						
I. B. Tsorin
V. V. Zakusov State Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Russian Federation, 							8 Baltiiskaya St., Moscow, 125315						
M. B. Vititnova
V. V. Zakusov State Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Russian Federation, 							8 Baltiiskaya St., Moscow, 125315						
S. A. Kryzhanovskii
V. V. Zakusov State Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Russian Federation, 							8 Baltiiskaya St., Moscow, 125315						
T. A. Gudasheva
V. V. Zakusov State Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Russian Federation, 							8 Baltiiskaya St., Moscow, 125315						
S. B. Seredenin
V. V. Zakusov State Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Russian Federation, 							8 Baltiiskaya St., Moscow, 125315						
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