Тhio-containing pteridines: Synthesis, modification, and biological activity.

The present article is devoted to searching for biologically active agents among novel thio-containing pteridines. Synthetic protocols based on the condensation of 5,6-diamino-2-thioxo-2,3-dihydropyrimidin-4(1H)-ones with dicarbonyl compounds were elaborated and used for the synthesis of target products. The directions for further modification of the obtained thio-containing pteridines were substantiated and realized.

A Simple and Convenient Method for the Synthesis of 1-Methyl-7-arylfuro[3,2-g]pteridine-2,4(1H,3H)-diones and Their Substituted Derivatives.

A simple and effective method for the synthesis of unknown 1-methyl-7-arylfuro[3,2-g]pteridine-2,4(1H,3H)-diones by dehydration of the corresponding 1-methyl-6-phenacyl-pteridine-2,4,7(1H,3H,8H)-triones is reported in the article. It was shown that their alkylation by butyl chloroacetate in basic medium proceeded by the N3-atom of the heterocycle. The structure and purity of the synthesized compounds were confirmed by IR, 1H, 13C NMR spectroscopy, gas chromatography-mass spectrometry, mass spectrometry, as well as X-ray diffraction analysis.

Directed Search of Biologically Active Compounds among Hydrogenated Isoindolylalkyl(alkylaryl-,aryl-)carboxylic Acids with Quinazoline Fragment that Modify the Carbohydrate Metabolism: Design, Synthesis and Modification.

An effective synthesis of (3H-quinazoline-4-ylidene)hydrazides of N-carboxyalkyl-(arylalkyl-,aryl-)isoindoline-1,3-diones, using activated N-protected aminoacids and 4-hydrazinoquinazoline was proposed in the framework methodology of directed search of hypoglycemic agents (fragment-oriented design, molecular docking). These hydrazides prepared via cyclocondensation under acid catalysis were converted to the corresponding 2-([1,2,4]triazolo[1,5-c]quinazoline-2-yl-) alkyl-(alkylaryl-,aryl-)-hydroisoindole-1,3(2H)-diones. The structure of synthesized compounds was established using IR, 1H and 13C NMR spectroscopy and LC-MS and the features of spectral pattern were discussed.

Search for Compounds with Hypoglycemic Activity in the Series of 1-[2-(1H-Tetrazol-5-yl)-R(1)-phenyl]-3-R(2)-phenyl(ethyl)ureas and R(1)-Tetrazolo[1,5-c]quinazolin-5(6H)-ones.

Methods of 1-[2-(1H-tetrazol-5-yl)-R(1)-phenyl]-3-R(2)-phenyl(ethyl)ureas and R(1)-tetrazolo[1,5-c]quinazolin-5(6H)-ones synthesis were designed. IR, LC-MS, (1)H NMR, and elemental analysis data evaluated the structure and purity of the obtained compounds. Different products, depending on the reaction conditions, were distinguished and discussed.