Lead discovery and optimization of T-type calcium channel blockers

…, JK Choi, E Lee, JK Lee, H Rhim, SH Seo, Y Kim…

Index: Park, Jung Hwan; Choi, Jin Kyu; Lee, Eunjung; Lee, Jae Kyun; Rhim, Hyewhon; Seo, Seon Hee; Kim, Yoonjee; Doddareddy, Munikumar Reddy; Pae, Ae Nim; Kang, Jahyo; Roh, Eun Joo Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 3 p. 1409 - 1419

Full Text: HTML

Citation Number: 25

Abstract

A series of compounds were designed as T-type calcium channel blocker containing 6 or 5 pharmacophore features from structure-based virtual screening. To optimize the suggested structure, over 130 derivatives were synthesized and their inhibitory activities on T-type calcium channel were assayed using in vitro screening system with α1G and α1H clones. For the compounds with higher activities in FDSS assay system, the efficacy was ...