- Hypolipidemic 1,4-benzothiazepine derivative
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The invention is concerned with a novel hypolipidemic compound, which is of (3R,5R)-3-Butyl-3-ethyl-2,3,4,5-tetrahydro-7-methoxy-5-phenyl-1,4-benzothiazepin-8-ol 1,1-dioxide; or a salt, solvate, or physiologically functional derivative thereof, with processes for its preparation, pharmaceutical compositions containing it and with its use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as athersclerosis.
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- Determination of the sequential order of acidity in a polyhydroxylated benzophenone series. Consequence on the oxidation reaction in relation to hepatotoxicity
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The pKa values of successive acid-base equilibria involved in the pyrogallol ring ionisation of exifone, 2,3,4-trihydroxybenzophenone 1, and related methoxy derivatives were determined by UV-VIS absorption spectrometry and potentiometric titration.Due to strong intramolecular hydrogen bonding, the sequential order of acidity of the three hydroxy groups of 1 was found to be 4-OH > 3-OH > 2-OH.The polyhydroxylated benzophenones were oxidized to 3,4-quinone only in a narrow range of acidity in which the monoanionic 4-olate species predominated in solution.The attachment of an amino-alcohol residue resulted in the trapping of the transient 3,4-quinone and provided a convenient route to novel 1,4-benzoxazine derivatives.Cytotoxicity experiments in rat hepatocytes indicated that some of these compounds were significantly less toxic than the parent exifone.
- Largeron, Martine,Langevin-Bermond, Dominique,Fleury, Maurice-Bernard
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p. 893 - 900
(2007/10/03)
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- Studies on uricosuric diuretics. III. Substituted 1,3-dioxolo[4,5-f]-1,2-benzisoxazole-6-carboxylic acids and 1,3-dioxolo[4,5-g]-1,2-benzisoxazole-7-carboxylic acids
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A series of substituted 1,3-dioxolo[4,5-f]-1,2-benzisoxazole-6-carboxylic acids 13 and 1,3-dioxolo[4,5-g]-1,2benzisoxazole-7-carboxylic acids 14 were synthesized and evaluated for diuretic and uricosuric activities in rats. Most of the benzisoxazole deriv
- Sato,Dan,Onuma,Tanaka,Aoki,Koga
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p. 109 - 116
(2007/10/02)
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