ABsrFucT.-"he crinine-type alkaloids (+)-buphanisine [l] and (-)-siculine E21 have been obtained from Sternbwgia sicula, while (-)-epimaritinarnine 131 and (-kmaritinarnine [4]were found in Sternbergia lutea.

Myeloperoxidase (MPO), a heme protein expressed by polymorphonuclear leukocytes, generates potent oxidants which are proposed to contribute to tissue damage during inflammation and certain pathogenesis such as neurodegenerative disorders. In this study, twenty omega-[2-oxo-3H-benzoxazol-3-yl]-N-phenylacetamide and propionamide derivatives having substituents of different lipophilic and electronic nature on the N-phenyl ring were synthesized to evaluate the inhibitory effects on in vitro leukocyte MPO chlorinating activity. The most active compounds in the series were the derivatives bearing 2-methyl and 4-nitro substituent on the N-phenyl ring.

In this study, inspired by the structures of the taltrimide, 2-phthalimidoethanesulphonamide, and the anilide pharmacophore known to be synthetically produced anticonvulsant compounds, fifteen N-phenyl-2-phtalimidoethanesulfonamide derivatives bearing substituents with diverse electronic and hydrophobic features on N-phenyl ring were synthesized. The structural confirmation of the title compounds was achieved by interpretation of spectral and analytical data. The anticonvulsant activity of the title compounds was determined against maximal electroshock seizure in mice at a dose level of 100 mg/kg. The preliminary screening results indicated that the exchange of the N-isopropyl moiety for an N-phenyl ring in the taltrimide molecule abolished the anticonvulsant activity. However, introducing certain substituents, such as nitro, methyl, and chloro, into the N-phenyl ring lead to more active compounds in comparison to the unsubstituted derivatives.

Hypecoum imberbe, Hypecoum procumbens. and Hypecoum pendulum of Turkish origin produce the new benzophenanthridine alkaloid (±)-nitrotyrasanguinatine {!].Until recently, the genus Hypecoum, which includes some 15 species distributed from the Mediterranean to Central Asia and Northern China, had been counted as belonging to the family Papaveraceae (1,2). It has now been recognized, however, that Hypecoum species belong more appropriately to the botanical family Hypecoaceae (1,2). This family includes only one genus and is intermediate between the Papaveraceae and the Fumariaceae (1).Protopine is known to be the main alkaloid in Hypecoum species (3). In addition, protoberberines (4), secoberbines (4), aporphines (4), spirobenzylisoquinolines ( 5), isoquinolones (6), and benzophenanthridines ( 4) are known to be present, besides the structurally uncommon ( + )-turkiyenine (7).Presently, as a result of a study of Hypecoum imberbe Sibth. Sm., collected in western Turkey, we have obtained the new and unusual alkaloid (±)-nitrotyrasanguinarine [1],C2gH22N207, which is the first isoquinoline alkaloid to incorporate an aliphatic nitro group. The occurrence of aromatic nitro groups among the isoquinoline-derived aristolochic acids is, of course, well documented (8).

No abstract