用于选择性T型钙通道阻滞剂的3,4-二氢喹唑啉类化合物的合成及生物活性
Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers.
作者信息
Rhim Hyewhon, Lee Yong Sup, Park Seong Jun, Chung Bong Young, Lee Jae Yeol
机构信息
Life Sciences Division, Korea Institute of Science & Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2005 Jan 17;15(2):283-6. doi: 10.1016/j.bmcl.2004.10.078.
We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca(2+) channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca(2+) channels and N-type Ca(2+) channels. Among them, 5b (KYS05044, IC(50)=0.56+/-0.10 microM) was identified as potent T-type Ca(2+) channel blocker with in vitro selectivity profile at meaningful level (T/N-type, SI=>100).
我们合成了用于高效选择性T型Ca(2+)通道阻滞剂的3,4-二氢喹唑啉衍生物，并评估了它们对两种T型Ca(2+)通道亚型和N型Ca(2+)通道的抑制活性。其中，5b（KYS05044，IC(50)=0.56±0.10 microM）被鉴定为具有有意义水平体外选择性谱（T/N型，SI>100）的高效T型Ca(2+)通道阻滞剂。
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