| abstract |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new derivatives of 5-acylamino-1,2,4-thiadiazoles of the formula (I) where Ar means an aromatic nitrogen-containing heterocycle taken among quinolinyl, isoquinolinyl, indolyl being the latter can be substituted with a group W at nitrogen atom where W is taken from a group involving: (a) -(CH 2 ) n COR where "n" means 1 or 2 and R means OR 1 where R 1 is taken from hydrogen atom and (C 1 -C 4 )-alkyl; (b) tetrahydropyranyl and (c) chain -(CH 2 ) 3 where the last carbon atom is fixed in phenyl ring of indole that results to formation of 6-membered heterocycle; Z means: (a) group where A and B mean -C and X 1 ,X 2 ,X 3 ,X 4 are similar or distinct and mean hydrogen atom, chlorine or bromine atom, (C 1 -C 3 )-alkyl group, (C 1 -C 3 )-alkoxyl group or trifluoromethyl group; (b) naphthyl group and their pharmaceutically acceptable salts also. Compounds show affinity to biological receptors of cholecystokinin. Invention describes also a method of synthesis of derivatives of 5-acylamino-1,2,4-thiadiazoles of the formula (I) by any of p. p. 1-6 that involves an interaction of derivative of 5-aminothiadiazole of the formula (II) where Z has a value indicated in p. 1 with a reactive derivative of an acid of the formula Ar′-COOH where Ar′ has values indicated in p. 1 for Ar or means a derivative of Ar where reactive centers under acylation conditions are protected. Then if necessary protective groups are removed from the above indicated reactive centers of aromatic ring. EFFECT: improved method of synthesis, affinity of synthesized compounds to cholecystokinin receptors. 8 cl, 2 tbl, 9 ex |