Design, synthesis, and biological evaluation of 1,3-dioxoisoindoline-5-carboxamide derivatives as T-type calcium channel blockers

  • Bioorg Med Chem Lett. 2007 Jan 15;17(2):476-81. doi: 10.1016/j.bmcl.2006.10.042.
Hwa Sil Kim  1 ,  Yoonjee Kim ,  Munikumar Reddy Doddareddy ,  Seon Hee Seo ,  Hyewhon Rhim ,  Jinsung Tae ,  Ae Nim Pae ,  Hyunah Choo ,  Yong Seo Cho
Affiliations
  • 1. Life Sciences Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
PMID: 17092715 DOI: 10.1016/j.bmcl.2006.10.042
Abstract

A small molecule library of 1,3-dioxoisoindoline-5-carboxamides 4 was designed based on the pharmacophore model, synthesized and biologically evaluated as potential T-type calcium channel blockers. The most active compounds 4d and 4n show T-type calcium channel blocking activity with IC50 values of 0.93 and 0.96 microM, respectively.