Calmodulin inhibitory activity of the malbrancheamides and various analogs.

Calmodulin inhibitory activity of the malbrancheamides and various analogs.
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DOI:
10.1016/j.bmcl.2008.10.057
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发表时间:
2008-12-15
影响因子:
2.7
通讯作者:
Williams RM
Williams RM
中科院分区:
医学4区
文献类型:
--
作者:
Miller KA;Figueroa M;Valente MW;Greshock TJ;Mata R;Williams RM

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公开了各种结构类似物的制备及其生物活性。研究了吲哚氯化、C-12a相对立体化学和双环[2.2.2]重氮辛烷核心氧化态对这些类似物抑制钙调素依赖性磷酸二酯酶(PDE1)能力的影响,并鉴定了一些有效的化合物。
The preparation and biological activity of various structural analogs of the malbrancheamides are disclosed. The impact of indole chlorination, C-12a relative stereochemistry, and bicyclo[2.2.2]diazaoctane core oxidation state on the ability of these analogs to inhibit calmodulin dependent phosphodiesterase (PDE1) was studied, and a number of potent compounds were identified.
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