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Background. In the production of hybrid medicines, the principle of hybrid blocks of molecules is used. Of interest are the processes of combining fragments with biological activity - thienopyrimidine and benzotriazole, synthesis and study of their structure. Purpose Reaction of nucleophilic substitution of 5,6-disubstituted 4-chlorothieno[2,3-d]pyrimidine with 1H-1,2,3-benzotriazole in the presence of tertiary amines and synthesis of new types of hybrid molecules. Methodology. Derivatives of the target product were studied by IR, 1H, 13C NMR spectroscopy and mass spectrometry. Originality. Synthesis of substituted-4-chlorothieno[2,3-d]pyrimidine derivatives under various conditions was carried out, a new type of thienopyrimidine-benzotriazole hybrid molecules was synthesized, and their physicochemical properties were determined. Findings. Hybrid molecules with alternating fragments of different activity, and substances in the molecules of which there was a C (sp2) - N bond were obtained. The structure was studied. [ABSTRACT FROM AUTHOR]

Background. In recent years, new medicinal substances have been identified, including derivatives of condensed thieno[2,3-d]pyrimidine. It is important to obtain their new derivatives using organic synthesis, to determine their biological activity for the creation of medicines. Purpose: synthesis of 4-chloro-5,6,7-trihydrocyclopenta[4,5]thieno[2,3-d]pyrimidine and based on it the reaction of nucleophilic exchange with secondary amines, to determine the factors affecting the reaction and the optimal reaction conditions. Methodology. Methods of organic synthesis were used to create new derivatives of 4-chloro-5,6,7trihydrocyclopenta[4,5]thieno[2,3-d]pyrimidine. The structure of the synthesized substances was confirmed by IR and 1H NMR spectroscopy. Originality. Based on 4-chloro-5,6,7-trihydrocyclopenta[4,5]thieno[2,3-d]pyrimidine, 4-piperidino5,6,7-trihydrocyclopenta[4,5]thieno[2,3-d]pyrimidine, 3-(5,6,7-trihydrocyclopenta-[4,5]thieno[2,3-d]pyrimidin4-yl)1,2,3,4,5,6-hexahydro8H-1,5-methanopyrido-[1,2-a][1,5]diazocin-8-one, 4-morpholino-5,6,7trihydrocyclopenta[4,5]thieno[2,3-d]pyrimidines. Findings. 4-Chloro-5,6,7-trihydrocyclopenta [4,5]thieno[2,3-d]pyrimidine and new compounds based on it were synthesized in high yield. Their IR, 1H, and 13C NMR spectra were analyzed and their compliance with the proposed structure was proved. [ABSTRACT FROM AUTHOR]

The sympatholytic properties of pyrimidines and pyrido[1,2-a]pyrimidine derivatives, involving two, that exhibit strong antimonoamine oxidase (MAO) properties, are investigated. It was shown that the 3-isobutylthio derivative is most active as an MAO inhibitor and exhibits some sympatholytic properties. The obtained data point to the possibility of creating antidepressant medications on the basis of MAO inhibitors, which, due to simultaneous manifestation of sympatholytic activity, will be significantly less safe due to reduction of the risk of arterial hypertension caused by these drugs. [ABSTRACT FROM AUTHOR]

Inhibition activity against protein kinase CK2 of thieno[2,3-d]pyrimidinone derivatives was discovered. In vitro testing of 86 compounds allowed finding of 15 compounds with IC50 less than 20 μM. The most active compound is 4-{[5-(4-ethylphenyl)-4-oxothieno[2,3-d]pyrimidine-3-(4H)-yl]methyl} benzoic acid (IC50=2.5 μM). The structure- actvity relationship of thieno[2,3-d]pyrimidinones was investigated and the binding modes of their interaction with protein kinase CK2 were proposed. [ABSTRACT FROM AUTHOR]

By the interaction of 2-bromomethyl derivatives of imidazo[1,2-a]pyridine, imidazo[1,2-a]pyrimidine and imidazo[1,2-a]thiazole with natural 7-hydroxyisoflavone formononetin and with its synthetic analogues the corresponding 7-(imidazo[1,2-a]hetaryl-2-methoxy)-3-aryl-4H-4-chromenones were synthesized. [ABSTRACT FROM AUTHOR]