Collect. Czech. Chem. Commun. 1981, 46, 1397-1404

Some 2-substituted derivatives of 5-(2-amino-6-hydroxy-4-oxo-3,4-dihydro-5-pyrimidinyl)pentanoic acid

Rudolf Kotva, Jiří Křepelka, Antonín Černý, Vojtěch Pujman and Miroslav Semonský

Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3


On condensation of 6-substituted trialkyl esters of 2-carboxy-1,7-heptanedioic acids XIII-XXIII with guanidineand subsequent saponification 2-substituted 5-(2-amino-6-hydroxy-4-oxo-3,4-dihydro-5-pyrimidinyl)pentanoic acids II-XII were prepared. From the pharmacological point of view some of the substances prepared had a potentiating effect on the antileukemia effect of 5-fluorouracil in mice and the antineoplastic effect manifested by a diminution of the tumours in animals with experimental tumours.