2-4-2-(2-AMINO-4-OXO-4,6,7,8-TETRAHYDRO-3H-PYRIMIDO-5,4-B- -1,4-THIAZINE-6-YL)ETHYLBENZOYL (OR THIENYLCARBONYL)-AMINO- -PENTANEDIOIC ACID OR ITS LOWER ALKYL ESTER, A METHOD OF INHIBITION AND PROLIFERATION OF CELLS AND A METHOD OF INHIBITION OF AN ENZYME ACTIVITY

摘要

FIELD: organic chemistry, biochemistry. SUBSTANCE: invention relates to new compounds of the general formula (I): where Ar means phenyl, thienyl or thienyl substituted with lower alkyl, or its lower alkyl ester that inhibit enzyme glycineamidoribonucleotide formyltransferase and to a method of inhibition and proliferation of bacterial cells or higher organism. Method involves administration to host a compound (I) or its ester at effective dose. Invention relates to a method of inhibition of activity of glycineamideribonucleotide formyltransferase in vitro by effect on this enzyme with an effective dose of compound of the formula (I) or its ester. Compounds of the formula (I) are synthesized by multistage method that involves interaction of compounds of the formula (III) with compound (IV) in the presence of a base and producing a compound (V) which interacts with acid in solvent and forms a compound (VI) . The latter is reduced and obtained compound (VII) is hydrolyzed to compound (VIII) or a compound (VII) where R₃ - hydrogen is subjected for interaction with glutamic acid diester hydrochloride and if necessary the synthesized compound is hydrolyzed. EFFECT: improved method of synthesis, enhanced inhibitory effectiveness. 6 cl, 3 tbl, 3 ex