2. Academic Validation
  3. Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers

Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers

  • J Med Chem. 2010 Sep 23;53(18):6773-7. doi: 10.1021/jm1006758.
Michele Melchiorre 1,  Martina Del Lungo,  Luca Guandalini,  Elisabetta Martini,  Silvia Dei,  Dina Manetti,  Serena Scapecchi,  Elisabetta Teodori,  Laura Sartiani,  Alessandro Mugelli,  Elisabetta Cerbai,  Maria Novella Romanelli
Affiliations

Affiliation

  • 1 Laboratory of Design, Synthesis, and Study of Biologically Active Heterocycles (HeteroBioLab), Department of Pharmaceutical Sciences, Via Ugo Schiff 6, 50019 Sesto Fiorentino (FI), Italy.
PMID: 20795648 DOI: 10.1021/jm1006758
Abstract

New I(f) blockers have been designed and tested on HEK293 cells stably expressing the HCN1, HCN2, and HCN4 channels to find compounds able to discriminate among the channel isoforms. Among the synthesized compounds, the cis-butene derivative (R)-5 shows some preference for HCN2 while the pseudodimeric product (R)-6 shows selectivity for HCN1. These compounds can be important pharmacological tools to study the channels in native tissues and may be useful to design safe drugs.

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