Biomedical subjects
Publications and source records attributed to Z Machoń.
2,4-Disubstituted 5-amino-6-pyrimidinecarboxylic acid derivatives 5-20 were synthesized and evaluated for their pharmacological activity. Compounds 11-14, 17-19 showed antiaggressive effect, compounds 5, 8, 9, 11, 12 and 19 displayed antiserotonin activity while compound 14 exerted antireserpine action.
Furo[3,4-d]pyrimidine was obtained in the reaction of 2-phenyl-4-phenylamino-6-methyl-5-pyrimidinecarboxylic acid with SOCl2. This compound, heated with aliphatic amines, yielded mono- and diamino-derivatives. Some of the obtained compounds exhibited a potent antineoplastic activity.
The synthesis of 4-hydroxy-4-amino substituted 5-phenylisoxazolo [5,4-d]-6,7-dihydropyrimidines was described. The compounds with alkylamine and semicarbazide substituents in position 4 showed the activity against sarcoma Sa-180, while those with heterocyclic substituents at the same position have analgesic properties.
Several new 5-substituted 1-phenylpyrazole [3,4-d] pyrimidine derivatives were synthesized and tested for antitumor activity. Compound 17, which has 3,4-dichlorophenyl moiety at N5 of the pyrazole pyrimidine ring, shows a strong activity against L-1210 leukemia (152%). On the other hand, compounds 15, 17 and 21 were the most active against sarcoma Sa-180. It was observed that many derivatives of pyrazole [3,4-d] pyrimidine possess different biological, especially antitumor properties [1-6, 9, 10].
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2,4-Disubstituted 5-amino-6-pyrimidinecarboxylic acid derivatives 5-13 were synthesized and evaluated for their pharmacological activity. Compounds 5, 7, 9, 10 and 12 showed antiaggressive effect, compounds 6 and 10 showed synergism with hexobarbital while compound 6 exerted analgesic activity.