… ) phenyl]-1, 3, 4-oxadiazol-2 (3 H)-one, BMS-191011: Opener of Large-Conductance Ca2+-Activated Potassium (Maxi-K) Channels, Identification, Solubility, and SAR

…, J Natale, S Moon, A Ortiz, S Yeleswaram…

文献索引：Romine, Jeffrey L.; Martin, Scott W.; Meanwell, Nicholas A.; Gribkoff, Valentin K.; Boissard, Christopher G.; Dworetzky, Steven I.; Natale, Joanne; Moon, Sandra; Ortiz, Astrid; Yeleswaram, Swamy; Pajor, Lorraine; Gao, Qi; Starrett Jr., John E. Journal of Medicinal Chemistry, 2007 , vol. 50, # 3 p. 528 - 542

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被引用次数: 31

摘要

Compound 8a (BMS-191011), an opener of the cloned large-conductance, Ca2+-activated potassium (maxi-K) channel, demonstrated efficacy in in vivo stroke models, which led to its nomination as a candidate for clinical evaluation. Its maxi-K channel opening properties were consistent with its structural topology, being derived by combining elements from other known maxi-K openers. However, 8a suffered from poor aqueous solubility, which ...