63625-95-6Relevant articles and documents
Antihyperglycemic activity of novel substituted 3H-1,2,3,5-oxathiadiazole 2-oxides
Ellingboe,Alessi,Dolak,Nguyen,Tomer,Guzzo,Bagli,McCaleb
, p. 1176 - 1183 (2007/10/02)
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).
Synthesis and antidepressant properties of novel 2-substituted 4,5-dihydro-1H-imidazole derivatives
Wentland,Bailey,Alexander,Castaldi,Ferrari,Haubrich,Luttinger,Perrone
, p. 1482 - 1489 (2007/10/02)
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.
