- Antihyperglycemic activity of novel substituted 3H-1,2,3,5-oxathiadiazole 2-oxides
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A series of substituted 3H-1,2,3,5-oxathiadiazole-2-oxides (6) was prepared and tested for antihyperglycemic activity in the db/db mouse, a model for type 2 (non-insulin dependent) diabetes mellitus. The oxathiadiazoles 6 were synthesized by a two-step sequence: treatment of a substituted acetonitrile (4) with hydroxylamine to give the corresponding amidoxime (5) and cyclization with thionyl chloride to yield 6. In terms of potency, the 2-naphthalenylmethyl group (as in compound 3) was found to be the optimal substituent in this series. Compound 3 was approximately 5 times more potent than ciglitazone (1).
- Ellingboe,Alessi,Dolak,Nguyen,Tomer,Guzzo,Bagli,McCaleb
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p. 1176 - 1183
(2007/10/02)
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- Novel substituted 3H-1,2,3,5-oxathiadiazole 2-oxides useful as anthihyperglycemic agents
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This invention relates to novel substituted 3H-1,2,3,5-oxathiadiazole 2-oxides, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical compositions thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.
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- Synthesis and antidepressant properties of novel 2-substituted 4,5-dihydro-1H-imidazole derivatives
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A unique combination of α2-adrenoreceptor antagonist and serotonin-selective reuptake inhibitory activities has been identified in a series of 2-substituted 4,5-dihydro-1H-imidazole derivatives. This combination of blocking activities has provided one of these derivatives, napamezole hydrochloride (2), with potential as an antidepressant. A discussion of the syntheses of these compounds includes a convenient method for the conversion of nitriles to imidazolines with ethylenediamine and trimethylaluminum.
- Wentland,Bailey,Alexander,Castaldi,Ferrari,Haubrich,Luttinger,Perrone
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p. 1482 - 1489
(2007/10/02)
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- Antidepressant imidazolines and related compounds
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2-(2-Naphthalenyl)alkyl-4,5-dihydro-1H-imidazoles and -tetrahydropyrimidines, the corresponding 3,4-dihydronaphthalenyl and 1,2,3,4-tetrahydronaphthalenyl compounds; and the corresponding indene and indane derivatives, useful as antidepressant or diuretic agents, are prepared by reacting the appropriate 2-(cyanoalkyl)naphthalene or -indane derivative (or the corresponding ester or imino-ether) with an alkylenediamine.
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