Discovery of a class of potent gap-junction modifiers as novel antiarrhythmic agents.
作者信息
Piatnitski Chekler Eugene L, Butera John A, Di Li, Swillo Robert E, Morgan Gwen A, Rossman Eric I, Huselton Christine, Larsen Bjarne D, Hennan James K
机构信息
Wyeth Research, Chemical Sciences, Collegeville, PA 19426, USA.
出版信息
Bioorg Med Chem Lett. 2009 Aug 15;19(16):4551-4. doi: 10.1016/j.bmcl.2009.07.014. Epub 2009 Jul 9.
PMID:19616941
Abstract
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.
摘要
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