A. G. Akopyan

Derivatives of condensed thienopyrimidines: Synthesis and anticonvulsant and tranquilizer activity of hydrochlorides of pyrano[4′,3′:4,5]thieno[3,2-e]imidazo[1,2-a]pyrimidines

New methods for the synthesis of 4-substituted 6,7-dihydro-7,7-dimethyl-5-oxo-9H-pyrano-[4′,3′: 4,5]-thieno[3,2-e]imidazo[1,2-a]pyrimidines and their hydrochlorides are developed. The anticonvulsant and tranquilizer properties of newly synthesized compounds have been studied.

Synthesis and Neurotropic Activity of 8-Amino Derivatives of Condensed Thieno[3,2-d]- and Furo[3,2-d]Pyrimidines

New derivatives of pyrano[4″,3″:4′,5′]pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidines based on 3-chloro derivatives of pyrano[3,4-c]pyridines and pyrano[4″,3″:4′,5′]pyrido[3′,2′:4,5]furo[3,2-d]pyrimidines based on previously prepared 8-chloro derivatives were synthesized. Studies of the biological activity of the synthesized compounds showed that several of them exhibited neurotropic properties.

Synthesis and Anticonvulsant Activity of 7(8)-Amino Derivatives of Condensed Thieno[3,2- d ]Pyrimidines

Methods for synthesizing novel amino derivatives of cyclopenta[4′,5′]pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidines and tetrahydropyrimido[4′,5′:4,5]thieno[2,3-c]isoquinoline from 3-chloro derivatives of alicyclo[c]pyridines were elaborated. Studies of the anticonvulsant activity of the synthesized compounds showed that they exhibited pronounced anticonvulsant activity and low toxicity.

Synthesis and Neurotropic Activity of Triazolo[3,4-a]-and Triazolo[5,1-a][2,7]Naphthyridines

Methods for synthesizing new substituted 7,8,9,10-tetrahydro[1,2,4]triazolo[3,4-a][2,7]naphthyridines from -hydrazino-7-isopropyl-3-chloro-5,6,7,8-tetrahydro[2,7]naphthyridine-4-carbonitrile were developed. It was shown that heating triazolo[3,4-a][2,7]-naphthyridines in an excess of amines produced isomeric triazolo[5,1-a][2,7]naphthyridine derivatives. These isomers were interconverted using a Dimroth rearrangement. The neurotropic activity of the synthesized compounds was studied.

Synthesis and conversions of polyhedral compounds: 28. Synthesis and psychotropic activity of some 1,3-diazaadamantane derivatives

The anticonvulsant and tranquilizer properties of some new derivatives of 1,3-diazaadamantane have been investigated. It is established that some of the synthesized compounds prevent corazole-induced convulsions in mice in a dose range of 18–75 mg-kg. The study of the influence of these compounds on the behavior of rats under open-field test conditions revealed a pronounced tranquilizer action.

Synthesis and neurotropic activity of 6,8-diamino derivatives of pyrano[3,4-c]pyridines

New diamino derivatives of pyrano[3,4-c]pyridines were synthesized by the pyridine ring recyclization. The presence of the intramolecular hydrogen bond in 6-[(4-methoxyphenyl)amino]-3,3-dimethyl8-methylamino-3,4-dihydro-1H-pyrano[3,4-c]pyridin-5-carbonitrile was identified by X-ray diffraction. A pharmacological study of the synthesized compounds was carried out in known tests, such as assay for antagonism induced by corazole subcutaneous injection and the open field test. The method of rotating rod was used to evaluate neurotoxicity. The diamino derivatives of pyrano[3,4-c]pyridines were found to possess neutrotropic properties. The synthesized compounds, as well as diazepam, prevent the occurrence of clonic seizures and clonic corazoleinduced convulsions in animals; however, they cause a behavior-depressing sedative effect.

Synthesis and neurotropic activity of 6-thio-substituted pyrano[3,4-c]pyridine and 1-aminopyrano[4,3-d]-thieno[2,3-b]pyridine derivatives and 9-substituted pyrido[2,3-b]thieno[3,2-d]pyrimidines

Methods for the synthesis of condensed thieno[3,2-d]pyrimidines based on 3,3-dimethyl-8-morpholino-6thioxo-3,4,6,7-tetrahydro-1H-pyrano[3,4-c]pyridine-5-yl cyanide have been developed. The neurotropic properties of the synthesized compounds have been investigated. Compounds possessing anticonvulsant activity and sedative properties are found. These compounds also exhibit an activating effect that makes them analogous to the well-known drug diazepam.

Synthesis and Neurotropic Activity of Amino Derivatives of Cyclopenta[4′,5′]pyrido[3′,2′:4,5]thieno[3,2-d ]pyrimidines and Pyrimido[4′,5′:4,5]thieno[2,3-c]isoquinolines

Amethod for synthesizing amino derivatives of cyclopenta[4′,5′]pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine and pyrimido[4′,5′:4,5]thieno[2,3-c]isoquinoline from thieno[3,2-d]pyrimidine derivatives was elaborated. The neurotropic activity of the synthesized compounds was studied.

Synthesis and Neurotropic Activity of New Pyrimido[4′,5′:4,5]Thieno[2,3-b]Quinoline Derivatives

New methods for preparing pyrimido[4′,5′:4,5]thieno[2,3-b]quinoline derivatives based on 3-cyanohexahydro-2-quinoline were developed. The neurotropic activity of these compounds was studied.

Synthesis and biological activity of condensed derivatives of thieno[3,2-d]thiazolo(thiazino, thiazepino)[3,2-a]pyrimidines

Methods for the synthesis of new heterosystems including condensed pyrano[4′,3′:4,5]pyrido[2,3-b]-thieno[3,2-d]thiazolo(thiazino, thiazepino)[3,2-a]pyrimidines, thiazolo(thiazino, thiazepino)[3″,2″:1′,2′]pyrimido[4′,5′:4,5]thieno[2,3-c]isoquinolines, and cyclopenta[4′,3′:4,5]pyrido[2,3-b]thieno[3,2-d]thiazolo(thiazino)[3,2-a]pyrimidines are developed. The synthesis is carried out on the basis of 1-amino-2-ethoxycarbonylpyrano[4,3-d]thieno[2,3-b]pyridines and -thieno[2,3-b]isoquinolines. Antitumor and anticonvulsant properties of the synthesized products have been evaluated. Compounds possessing low toxicity and moderate biological activity are found.