Synthesis and biological evaluation of aroylguanidines related to amiloride as inhibitors of the human platelet Na+/H+ exchanger

…, F Rogister, JV Dejardin, C Prosperi-Meys…

Index: Laeckmann, Didier; Rogister, Francoise; Dejardin, Jean-Victor; Prosperi-Meys, Christelle; Geczy, Joseph; Delarge, Jacques; Masereel, Bernard Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 6 p. 1793 - 1804

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Citation Number: 39

Abstract

Pyridine and benzene bioisosteres of amiloride were synthesized and evaluated for their inhibitory potency against the sodium–hydrogen exchanger (NHE) involved in intracellular pH regulation. The inhibition of NHE was determined by using the platelet swelling assay (PSA) in which the swelling of human platelets was induced by their incubation in an acid buffer (pH 6.7). Additionally, the inhibitory potency of the most active compounds was ...