基于苯二氮䓬的线粒体F1F0 ATP水解酶选择性抑制剂。
Benzodiazepine-based selective inhibitors of mitochondrial F1F0 ATP hydrolase.
作者信息
Hamann Lawrence G, Ding Charles Z, Miller Arthur V, Madsen Cort S, Wang Paulina, Stein Philip D, Pudzianowski Andrew T, Green David W, Monshizadegan Hossain, Atwal Karnail S
机构信息
Department of Discovery Chemistry, Bristol-Myers Squibb, Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA.
出版信息
Bioorg Med Chem Lett. 2004 Feb 23;14(4):1031-4. doi: 10.1016/j.bmcl.2003.11.052.
A series of benzodiazepine-based inhibitors of mitochondrial F(1)F(0) ATP hydrolase were prepared and evaluated for their ability to selectively inhibit the enzyme in the forward direction. Compounds from this series showed excellent potency and selectivity for ATP hydrolase versus ATP synthase, suggesting a potentially beneficial profile useful for the treatment of ischemic heart disease.
制备了一系列基于苯二氮䓬的线粒体F(1)F(0) ATP水解酶抑制剂，并评估了它们在正向方向上选择性抑制该酶的能力。该系列化合物对ATP水解酶相对于ATP合酶表现出优异的效力和选择性，表明其具有治疗缺血性心脏病的潜在有益特性。
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