The syntheses of axillarin and its related compounds

Zusammenfassung Axillarin (5, 7, 3, 4-Tetrahydroxy-3,6-dimethoxyflavon). 5,3,4-Trihydroxy-3,6,7-trimethoxyflavon und 5,7,3,4-Tetrahydroxy-3,8-dimethoxyflavon wurden synthetisiert.     

Antigastric secretory activity of 4-chloro-α,α-dimethylphenethylaminopropan-2-one and related compounds

Zusammenfassung AY-14,948 [4-Chlor-,-Dimethylphenethylaminopropan-2-on] setzt die basale Ausscheidung von Magensäure in der Ratte herab. Die Prüfung der strukturverwandten Verbindungen ergab, dass AY-18,672 [,-Dimethylphenethylaminopropan-2-on] in dieser Hinischt wirksamer ist als AY-14,948, indem es auch die reserpinbedingte Erregung der Magensäureausscheidung blockiert.     

A novel oxidative cyclization of 4-arylthiosemicarbazides and related compounds

Résumé Il est démontré que les 4-arylthiosemicarbazides sont oxydés par le brome dissous en chloroforme aux 2-hydrazinobenzothiazoles avec de modestes rendements. Une telle réaction sur les thiosémicarbazones correspondants donne les 1-arylidénè 2-(2-benzothiazolyle)hydrazines avec de très bons rendements. Ceux-ci purent, par la suite, être oxydés par le chlorure de fer⁺³ en solution éthanolique aux 3-aryl-s-triazolo (3,4-b)benzothiazoles. La présence de quelques substituants dans les restes 4-aryl et/ou 1-arylidène dans la moitié thiosemicarbazone favoriserait la cyclisation aux 3:4-diaryl-5-mercapto-1:2:4-triazoles.     

Inhibition of brain enolases by acrylamide and its related compounds in vitro,and the structure-activity relationship

Summary Acrylamide and its related compounds inhibited brain enolases in vitro independently of their neurotoxicity. The inhibitory potency was a function of the binding constants of the compounds for phenylalanine. The binding constant for tryptophan was higher in neurotoxic compounds than in non-neurotoxic ones.     

Inhibition of brain enolases by acrylamide and its related compounds in vitro, and the structure-activity relationship

Acrylamide and its related compounds inhibited brain enolases in vitro independently of their neurotoxicity. The inhibitory potency was a function of the binding constants of the compounds for phenylalanine. The binding constant for tryptophan was higher in neurotoxic compounds than in non-neurotoxic ones.     

The syntheses of 3,8-Dimethoxy-5,7,4′-trihydroxyfIavone and related compounds

Zusammenfassung 3, 8-Dimethoxy-5, 7,4-trihydroxyflavon und 3,6-Dimethoxy-5, 7, 4-trihydroxyflavon wurden synthetisiert.     

On the association between lysogeny and carcinogenicity in nitroquinolines and related compounds

Zusammenfassung In einer Serie von 16 Nitroquinolinen und verwandten Substanzen wurde eine gute Übereinstimmung zwischen Phageninduktion inEscherichia coli C-600 und Karzinogenese nachgewiesen.

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Supported by grants No. C-6516 and FR-05526 from the National Cancer Institute and Contract NO. PH 86-66-169 from the Division of Air Pollution, U.S.P.H.S. We thank Dr.Y. Kawazoe of the National Cancer Center Research Institute, Tokyo, for his generous gift of the compounds tested.     

Effects of 1-alkyl-1,2,3,4-tetrahydrocarbazole-1-ethanamines and related compounds,potential antidepressants,on biogenic amine uptake mechanisms

Summary A new series of compounds structurally related to the potential antidepressant tandamine, i.e., the 1-alkyl-1,2,3,4-tetrahydrocarbazole-1-ethanamines, inhibit the noradrenaline uptake mechanism and are relatively ineffective in inhibiting the serotonin uptake mechanism in vivo. The potency of the most effective compound (9-ethyl-N,N, 1-trimethyl-1,2,3,4-tetrahydrocarbazole is similar to that of desimipramine and is of potential use in the treatment of endogenously depressed patients.The authors acknowledge the technical assistance of Mrs J. Farnsworth, Mrs B. Gut and Mr J. Lacasse.     

Diminution of 5-hydroxytryptamine in thrombocytesin vitro by chlorpromazine and related compounds

Riassunto Cloropromazina, imipramina, cloroprotixene e amitriptilinain vitro diminiscono la 5-idrossitriptamina (5HT) endogena nei trombociti di coniglio e, per quanto si è visto, anche in quelli umani. Nel plasma di coniglio pretrattato con isocarbossazide, inibitore della mono-amino-ossidasi, si osserva un corrispondente aumento di 5HT. Cocaina, -metil-dopa e triptamina hanno un effetto meno pronunciato sulla 5HT delle piastrine.

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Guest worker from the Istituto di Patologia sp. Medica dell'Università di Bologna (Italy).     

Effects of 1-alkyl-1,2,3,4-tetrahydrocarbazole-1-ethanamines and related compounds, potential antidepressants, on biogenic amine uptake mechanisms.

A new series of compounds structurally related to the potential antidepressant tandamine, i.e., the 1-alkyl-1,2,3,4-tetrahydrocarbazole-1-ethanamines, inhibit the noradrenaline uptake mechanism and are relatively ineffective in inhibiting the serotonin uptake mechanism in vivo. The potency of the most effective compound (9-ethyl-N,N,1-trimethyl-1,2,3,4-tetrahydrocarbazole) is similar to that of desimipramine and is of potential use in the treatment of endogenously depressed patients.     

The effect of the phytoalexins,lubimin, (−)-maackiain,pinosylvin, and the related compounds dehydroloroglossol and hordatine M on human lymphoblastoid cell lines

Summary We have tested the effect of the phytoalexins lubimin, (–)-maackiain and pinosylvin and the related compounds dehydroloroglossol and hordatine M on the growth of the human lymphoblastoid cell lines Molt and Raji. (–)-maackiain, pinosylvin and dehydroloroglossol showed significant growth inhibitory action on the cells. Suppression of [³H] thymidine and [³H] leucine uptake was tested and noted in pinosylvin and dehydroloroglossol. The phytoalexins and related compounds are widespread in plants and provide a potential source of antineoplastic substances.We would like to acknowledge the assistance of J. Hux in preparing the phytoalexins and related compounds. This work was supported by a grant from National Health and Welfare Canada. Correspondence to Dr. L. Skinnider, Department of Pathology, University of Saskatchewan, Saskatoon, Saskatchewan, Canada S7M OWO.