2. Academic Validation
  3. Molecular hybridization, synthesis, and biological evaluation of novel chroman I(Kr) and I(Ks) dual blockers

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

  • Bioorg Med Chem Lett. 2009 Mar 1;19(5):1477-80. doi: 10.1016/j.bmcl.2009.01.022.
Lupei Du 1,  Minyong Li,  Qian Yang,  Yiqun Tang,  Qidong You,  Lin Xia
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Jiangsu 210009, China.
PMID: 19185489 DOI: 10.1016/j.bmcl.2009.01.022
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.

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