Discovery of novel neuronal voltage-dependent calcium channel blockers based on emopamil left hand as a bioactive template.
A series of novel neuronal voltage-dependent calcium channel (VDCC) blockers, with inhibitory activity at low micromolar and moderate solubility in water, was discovered by constructing and screening a focused library based on emopamil (1) left hand (ELH) as a bioactive template.
Suzuki
Yuichi
Y
Tsukuba Research Laboratories, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba-shi, Ibaraki 300-2635, Japan. y5-suzuki@hhc.eisai.co.jp
Yamamoto
Noboru
N
Iimura
Yoichi
Y
Kawano
Koki
K
Kimura
Teiji
T
Nagato
Satoshi
S
Ito
Koichi
K
Komatsu
Makoto
M
Norimine
Yoshihiko
Y
Kimura
Manami
M
Teramoto
Tetsuyuki
T
Kaneda
Yoshihisa
Y
Hamano
Takeshi
T
Niidome
Tetsuhiro
T
Yonaga
Masahiro
M
D000818:Animals; D002121:Calcium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology*; D020864:Calcium Channels, N-Type / Q000187:drug effects*; D020650:Combinatorial Chemistry Techniques; D015640:Ion Channel Gating / Q000187:drug effects; D010879:Piperazines / Q000737:chemistry; D051381:Rats; D012995:Solubility; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013574:Synaptosomes / Q000187:drug effects* / Q000378:metabolism; D014700:Verapamil / Q000031:analogs & derivatives* / Q000737:chemistry*
D002121:Calcium Channel Blockers; D020864:Calcium Channels, N-Type; D010879:Piperazines; D014700:Verapamil; C052752:emopamil