Discovery of a class of potent gap-junction modifiers as novel antiarrhythmic agents.

نویسندگان

  • Eugene L Piatnitski Chekler
  • John A Butera
  • Li Di
  • Robert E Swillo
  • Gwen A Morgan
  • Eric I Rossman
  • Christine Huselton
  • Bjarne D Larsen
  • James K Hennan
چکیده

In an effort to discover potent, orally bioavailable compounds for the treatment of atrial fibrillation (AF) and ventricular tachycardia (VT), we developed a class of gap-junction modifiers typified by GAP-134 (1, R(1)=OH, R(2)=NH(2)), a compound currently under clinical evaluation. Selected compounds with the desired in-vitro profile demonstrated positive in vivo results in the mouse CaCl(2) arrhythmia model upon oral administration.

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عنوان ژورنال:
  • Bioorganic & medicinal chemistry letters

دوره 19 16  شماره 

صفحات  -

تاریخ انتشار 2009