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ID: ALA1137751

Journal: Bioorg Med Chem Lett

Title: Molecular hybridization, synthesis, and biological evaluation of novel chroman I(Kr) and I(Ks) dual blockers.

Authors: Du L, Li M, Yang Q, Tang Y, You Q, Xia L.

Abstract: The combination of I(Kr) and I(Ks) blockade could lead to synergistic and safe class III anti-arrhythmic effect with the enhanced efficacy and reduced risk. On the rationale of structural hybridization of azimilide and HMR-1556, a novel series of I(Kr) and I(Ks) dual blockers were designed, synthesized and evaluated in vitro. One compound, 3r (CPUY11018), deserves further evaluation for its potent anti-arrhythmic activity and favorable cardiovascular profile.

CiteXplore: 19185489

DOI: 10.1016/j.bmcl.2009.01.022