P. Yu. Ivanov

Antiviral activity of 1-amino-1,2,3,4-tetrahydrocarbazoles

We have shown in the preceding paper [2] that l-aminotetrahydrocarbazo!es (I-XI) suppress the growth of tuberculosiss myobacteria in in vitro experiments. During more extensive biological studies of compounds I-XI we have found that compounds VIII-XI have an inhibiting action on the reproduction of the herpes virus. Therefore we have also synthesized the l-aminotetrahydrocarbazoles (XI!-XX) and studied their antiviral activity.

Antitubercular, antifungal, and antibacterial activity in vitro of 1-phenethylamino-1,2,3,4-tetrahydrocarbazoles

The biological activity of l-aminotetrahydrocarbazoles was discovered by in vitro experiments in [i, 6]. Of the compounds studied, the most active was 6-methyl-l-phenethylamino1,2,3,4-tetrahydrocarbazole (I). In order to find the relationship between the biological activity and the structure of the compounds, we studied the analogs of compound I: its homologs (II, III), the hydrogenated derivatives (IV, V), and also compounds with various substituents in the 6-position (VI-XI).

Study of pyrazidol metabolism

Sheinker I Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 30, No. 5, pp. 15 - 17, May, 1996. Original article submitted September 19. 1995. Pyrazidol, 8-methyl-2,3,3a,4,5,6-hexahydro-IH-pyraz- ino[3,2,I-jk]carbazole hydrochloride, is an original Russian drug belonging to the group of antidepressants [1]. In this work, we studied the metabolism of pyrazidol in vivo by experiments on rats. The structure of metabolites was established by the methods of electron impact mass spec- trometry (ELMS), secondary ion mass spectrometry (SIMS), and I H NMR spectroscopy. EXPERIMENTAL PART

Synthesis and pharmacological examination of hydrogenated 8-phenyl-1H-pyrazino-[3,2,1-jk]carbazoles

The pyrazinocarbazoie (IV) was synthesized as follows. Reaction of the diazobiphenyi (VI) with the formyicyciohexanone salt (VII) afforded the cyciohexanedione biphenyiyihydrazone (VIIi), which was then converted into the ketocarbazole (IX) by the Fischer method. The overall yield of the ketone (IX) (calculated on 4-aminobiphenyl) was 70%. Using a method similar to that used for pyrazidoi [i], the ketocarbazoie (IX) was converted via the iminocarbazoies (X) and (XI) into the required compound (IV). The overall yield of the pyrazinocarbazoie (IV) was 44%, calculated on the ketone (IX).

Synthesis and investigation of 8-(quinuclidin-3-yl)containing analog of pyrazidole

In continuation of the systematic investigation of the pyrazidole analogs we synthesized and studied a new derivative hexahydro-iH-pyrazino[3,2,l-j,k]carbazole having a quinuclidin-3-yl residue (II) in the 8-position. It was assumed that the introduction of the quinuclidinyl substituent, which is bulkier than the methyl group, would make it possible to magnify its antidepressant action, increase the solubility in water, decrease the stimulating effect and introduce a sedative component of activity characteristic for the quinuclidine compounds [ 7 ].