Synthesis of Water-Soluble Prodrugs of BMS-191011: A Maxi-K Channel Opener Targeted for Post-Stroke Neuroprotection

P Hewawasam,M Ding,N Chen,D King,J Knipe,L Pajor,A Ortiz,VK Gribkoff,J Starrett

Bioorganic & medicinal chemistry letters（2003）

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摘要

A variety of water-soluble prodrugs of BMS-191011 was synthesized and evaluated for solution state stability and rate of conversion to BMS-191011 in rat and human plasma. The deoxycarnitine ester prodrug (11c) was selected for clinical evaluation based on its superior chemical stability, crystallinity and cleavage to BMS-191011 in human plasma.

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