Pyrimidine derivatives of n-acetylguanidine: Novel inhibitors of sodium-hydrogen exchanger 1

• Published in: Heterocycles
• Main Author: Ozerov A.; Novikov M.; Spasov A.; Iezhitsa I.; Gurova N.; Gurova V.
• Format: Article
• Language: English
• Published: Japan Institute of Heterocyclic Chemistry 2018
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85051959874&doi=10.3987%2fCOM-18-13904&partnerID=40&md5=39d4a0b4c03d631d58a84861bd84e99f

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. © 2018 The Japan Institute of Heterocyclic Chemistry.