Novel Benzenesulfonamide derivatives

Title
Novel Benzenesulfonamide derivatives; their synthesis and biological activities as T-type calcium channel blocker

Title
their synthesis and biological activities as T-type calcium channel blocker
Authors
이주현강순방정낙철김유승금교창
Issue Date
2010-04
Publisher
대한화학회 제105회 총회 및 학술발표회
Citation
, IV38P154포
Abstract
T-type calcium channels are important regulators of neuronal excitation, and are essential mediators of hormone secretion. However, T-type calcium channel hyperactivity has been linked to neurological disorders such as epilepsy and neuropathic pain. Mibefradil is the first marketed selective T-type calcium channel blocker. So, We have particullary studied the structure of Mibefradil for the development of novel T-type calcium channel blockers. A series of novel benzenesulfonamide derivatives were designed and synthesized based on the 3D pharmacophore model constructed with known T-type Ca2+ channel blockers. The compounds were studied for the evaluation of in-vitro inhibitory activities with a1G and a1H channel in FDSS assay system, and the selectivity against hERG channel. Some selected compounds were further studies PK and in-vivo activity using animal model. So, we'll discuss the structure-activity relationship.
URI
http://pubs.kist.re.kr/handle/201004/37366
Appears in Collections:
KIST Publication > Conference Paper
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