A. S. Noravyan

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 antitumor activity of pyrano[4′,3′:4,5]pyrido[2,3-b]thieno[3,2-d]-1,2,3-triazine and l,2,3-triazino[4′,5′:4,5¦thieno-[2,3-c]isoquinoline derivatives

Methods for the synthesis of new heterosystems of condensed thieno[3,2-d]-1,2,3-triazines on the basis of pyrido[2,3-b]thiophenes have been developed. The antitumor activity of the synthesized compounds was studied and several compounds possessing low toxicity and moderate antitumor activity were found.

Synthesis and anticonvulsant activity of pyrano[4′,3′:4,5]pyrido[2,3-b]thieno[3,2-d] pyrimidine derivatives and pyrimido[5′,4′:2,3]-thieno[2,3-c]isoquinoline derivatives

Methods for the synthesis of condensed thieno[3,2-d]pyrimidines based on pyrano[4,3-d]thieno[2,3-b]pyridines and thieno[2,3-b]isoquinolines have been developed and a series of new derivatives have been synthesized. The anticonvulsant activity of the synthesized compounds has been studied. Several compounds possessing specific anticonvulsant activity with respect to corazole-induced convulsions are revealed.

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 anticonvulsive activity of a series of new pyrano(thiopyrano,pyrido)-[4′,3′:4,5]thieno[2,3-d]pyrimidines

Previously we have established some relationships between the chemical structure of thieno[2,3-d]pyrimidines and their pharmacological activity [ 1 -4] . In this work, we have used condensed 2-amino-3-ethoxyearbonylthieno[2,3-c]pyrans, -thiopyrans, and -pyridines ( I IV) [5, 6] and 2-alkyl, 3-, or 4-aminothieno[2,3-d]pyrimidines [4, 5, 7] for the synthesis of new 2-amino-3-ethoxycarbonylthiophene derivatives (V, VI), 2,3-substituted (VIIIX, XIII XVII) and 2,4substituted thieno[2,3-d]pyrimidines (XX, XXI, XXIIIXXIX), and 3,4-(XXXI, XXXII) and 2,3-condensed (XXXIII XL) compounds of the latter pyrimidines. The synthesized compounds were characterized with respect to their anticonvulsive activity. The acylated derivatives V and VI were obtained by interaction of compound II with the corresponding acid chloroanhydrides.

Synthesis and anticonvulsant activity of condensed thieno[2,3-e]pyrrolo[1,2-a]pyrimidin-8,12-diones

New condensed thieno[2,3-e]pyrrolo[1,2-a]pyrimidin-8,12-ones were synthesized from 2-thioxo-1,2-dihydropyridine-3-carbonitriles. The synthesized compounds were shown to exhibit pronounced anticonvulsant activity for corazole convulsions.

Synthesis and antibacterial activity of N-amino-derivatives of condensed pyridines

A method based on condensed 4-cyanopyridinethiones using O-tosylhydroxylamine as the aminating agent was developed for preparing tosylates of N-amino-derivatives of pyrano[3,4-c]pyridines; 5,6,7,8-tetrahydroisoquinolines; and cyclopenta[c]pyridines. The antibacterial activity of the synthesized compounds was assessed.

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 biological activity of pyrano[4,3-d]furo[2,3-b]pyridine derivatives

Furopyridines have a wide spectrum of biological activity [1 3] and some of them are used in medicine [4], thus stimulating a search for biologically active compounds among the derivatives of a new heterocyclic system, pyrano[4,3d]furo[2,3-b]pyridine. Synthesis was performed on the basis of 3-phenacyloxy-4-cyanopyrano[3,4-c]pyridines ( I a u) obtained earlier [5]. The presence of an active methylene group in these compounds makes it possible to carry out intramolecular cyclization in the presence of sodium ethylate, which yields 9-aminopyrano[4,3-d]furo[2,3-b]pyridines ( I I a u).