Novel openers of Ca2+-dependent large-conductance potassium channels: Symmetrical pharmacophore and electrophysiological evaluation of bisphenols

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 8, 2003, Pages 1437-1439

  Li, Yi ^a   Johnson, Graham ^a   Romine, Jeffrey L ^a   Meanwell, Nicholas A ^a   Martin, Scott W ^a   Dworetzky, Steven I ^a   Boissard, Christopher G ^a   Gribkoff, Valentin K ^a   Starrett Jr , John E ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 (5 CHLORO 2 HYDROXYPHENYL) 5 TRIFLUOROMETHYL 2 BENZIMIDAZOLONE; CALCIUM ACTIVATED POTASSIUM CHANNEL; IBERIOTOXIN; NS 1608; PHENOL DERIVATIVE; POTASSIUM CHANNEL BLOCKING AGENT; POTASSIUM CHANNEL STIMULATING AGENT; UNCLASSIFIED DRUG; BENZIMIDAZOLE DERIVATIVE; CHLOROPHENOL; LARGE CONDUCTANCE CALCIUM ACTIVATED POTASSIUM CHANNEL;

ANIMAL CELL; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG SCREENING; DRUG STRUCTURE; ELECTROPHYSIOLOGY; MEMBRANE CURRENT; NONHUMAN; OOCYTE; PHARMACOPHORE; PROTEIN EXPRESSION; XENOPUS LAEVIS; ANIMAL; CHEMISTRY; DOSE RESPONSE; DRUG EFFECT; DRUG POTENTIATION; PATCH CLAMP; PHYSIOLOGY;

STAPHYLOCOCCUS PHAGE 3A;

ANIMALS; BENZIMIDAZOLES; CHLOROPHENOLS; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTROPHYSIOLOGY; LARGE-CONDUCTANCE CALCIUM-ACTIVATED POTASSIUM CHANNELS; OOCYTES; PATCH-CLAMP TECHNIQUES; PHENOLS; POTASSIUM CHANNELS, CALCIUM-ACTIVATED; XENOPUS LAEVIS;

EID: 0037451826     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00156-2     Document Type: Article

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23. The following selected compounds are available commercially: 2a Tetrachlorophene (Pfaltz-Bauer); 2b Hexachlorophene (Aldrich); 2c 2,2′-Methylenebis-(4-chlorophenol) (Aldrich); 2g Bithionol (Fluka); 4a 4,4′,6,6′-Tetrabromo-2,2′-biphenol (Salor).
24. Procedure for 3b: 5-Chloro-2-methoxyphenyl isocyanate was treated with 5-chloro-2methoxyaniline in dichloromethane to generate the urea which was treated with a 1M solution boron tribromide at 0°C to deprotect the phenols (mp 183-185.5°C).
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