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Short Paper | Regular issue | Vol 96, No. 6, 2018, pp.1101-1107
Published online, 21st May, 2018
DOI: 10.3987/COM-18-13904
■ Pyrimidine Derivatives of N-Acetylguanidine: Novel Inhibitors of Sodium-Hydrogen Exchanger 1

Alexander Ozerov,* Mikhail Novikov, Alexander Spasov, Igor Iezhitsa, Natalia Gurova, and Valeria Gurova

*Department of Pharmaceutical & Toxicological Chemistry, Volgograd State Medical University, Pavshikh Bortsov Sq. 1, Volgograd 400131, Russia

Abstract

Sodium-hydrogen exchanger (Na+/H+) type 1 (NHE-1) inhibitors have been shown to protect the heart during ischaemia and early reperfusion. As such, NHE-1 inhibitors are of special interest for clinical development for the attenuation of both acute and chronic post-myocardial infarction responses. New pyrimidine derivatives of N-acetylguanidine containing fragments of uracil, thymine, and their 3-benzyl derivatives were synthesised. These compounds showed in vitro inhibitory effects on NHE-1 that were significantly higher than those of zoniporide in platelet swelling assays.