Twenty four new l-aminoacyl-2,3-dihydro-4( III)-quinazolinone derivatives were prepared and evaluated for their pharmacological properties. The compounds with a cyclic amino group showed a choleretic activity. Some substances displayed also antifibrillatory and antiphlogistic activity.
Notes irradiation of 5-10 g of trans-zearalanol (3a or 3b)# was purified by column chromatography on 200 g of SilicAR, CC-7, with 3% methanol-chloroform to give cis-zearalenol (4a or 4b) as a white amorphous solid,** mp (4a) 124-128°, mp (4b) 126-131°. Anal.(C18H240 5)C, H. Uterotropic Assays. Stock solutions prepared in methanol were diluted and poured on small animal ration (Allied Mills), which was allowed to dry overnight at room temperature. Each test diet was further mixed in a high-speed blender for 1 min before being offered to eight adult castrate female mice for 5 days at 3 g per mouse per day. On day six the animals were sacrificed, and uteri were removed and weighed.Acknowledgment. The author is grateful to Mr. Harold Burns for technical assistance, Mr. Carl Power for performing the uterotropic assays, and Mr. Bill Boyll for carrying
The search for new (3-adrenergic blocking drugs with enhanced therapeutic properties is still very active1 and there has recently been an increasing interest in heterocyclic (e.g., benzodioxane,2'3 indole,4'5 benzofuran,6 dibenzofuran,7 quinoline, etc.8) derivatives. We now report the preparation of some new (3-adrenergic blocking derivatives of the chromone and flavone group, with which we wish to illustrate further the versatility of the benzo-y-pyrone molecule as a carrier moiety in medicinal research. We have also prepared 2 analogous xanthone derivatives (19, 20) on the basis of the results obtained among the CNS stimulants of the same group.9'10 The basic chain was located, according to the
3.4‐Dihydro‐2H‐1.2‐benzothiazinon‐(3)‐1.1‐dioxid (la) und 3.4‐Dihydro‐1H‐2.3‐benzothi‐azinon‐(4)‐2.2‐dioxid (2a) sowie einige N‐Substitutionsprodukte werden ausgehend von den Sulfonamiden 4 bzw. 15 dargestellt. Die Nitrierung der Verbindungen wird untersucht.
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