Abstract
3-Aryl-3-fluorooxindoles can be efficiently synthesized in two steps by the addition of an aryl Grignard to an isatin, followed by treatment with DAST. Oxindole 1 (BMS-204352; MaxiPost) can be isolated using chiral HPLC or prepared by employing chiral resolution. Cloned maxi-K channels are opened by 1, which demonstrates a brain/plasma ratio >9 in rats.
MeSH terms
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Animals
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Brain / drug effects*
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Brain / metabolism
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Calcium / metabolism
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Cells, Cultured / drug effects
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Diazonium Compounds*
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Humans
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Indoles / blood
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Indoles / chemical synthesis*
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Indoles / pharmacology*
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Large-Conductance Calcium-Activated Potassium Channels
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Male
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Microinjections
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Oocytes / drug effects*
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Oocytes / physiology*
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Patch-Clamp Techniques
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Potassium Channels, Calcium-Activated / drug effects*
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Potassium Channels, Calcium-Activated / genetics
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Potassium Channels, Calcium-Activated / metabolism
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RNA, Messenger / metabolism
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Rats
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Rats, Sprague-Dawley
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Xenopus
Substances
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BMS204352
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Diazonium Compounds
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Indoles
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Large-Conductance Calcium-Activated Potassium Channels
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Potassium Channels, Calcium-Activated
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RNA, Messenger
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selectfluor
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Calcium