Novel Dihydropyridinyl acetamide and Piperidinyl acetamide derivatives

Title
Novel Dihydropyridinyl acetamide and Piperidinyl acetamide 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
이주현강순방김유승정낙철금교창
Keywords
neuropathic pain; acetamide; T-type calcium channel
Issue Date
2010-10
Publisher
대한화학회 제106회 총회 및 학술발표회 전자 논문집
Citation
VOL 106, MEDLP-50
Abstract
T-type Ca2+channel play important role in modulating neuronal excitability on the central and peripheral neuron system, and is the essential intermediary of hormon secrection. However, hyperactivity of T-type calcium channel generate neurological disorders such as epilepsy, hypertension and neuropathic pain. So, T-type Ca2+channel blockers has been researched on a great number of fields. Therefore, we tried to study on the new drug, which is active on T-type Ca2+ channel with good selectivity as a neuropa-thic pain therapy. A series of novel dihydropyridinyl acetamide and piperidinyl acetamide 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 1G and 1H channel in FDSS assay system. Some selected compounds α α were further studies the selectivity against hERG channel. Hence, we'll discuss the structure-activity relationship.
URI
http://pubs.kist.re.kr/handle/201004/41741
ISSN
1229-6708
Appears in Collections:
KIST Publication > Conference Paper
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