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Z Machoń

Publications and source records attributed to Z Machoń.

At least 37 records · Page 2Linked to original sources
PubMed1981

Synthesis and biological properties of some 5-aminoorotic acid derivatives.

2,4-Dihydroxy-5-benzoylaminopyrimidine-6-carboxylic acid 1 in the reaction with SOCI2 gave 1-benzoyl-2-oxo-4,6-dihyroxyazetino [3.2-d] pyrimidine 2 which reacted with aliphatic and aromatic amines in ethanol to give appropriate amides 4a-4h of 1 and ethyl 2,4-dihydroxy-5-benzolaminopyrimidine-6-carboxylate 5. Compounds 4d-4g and 8 were centrally active and showed a promising anti-inflammatory and analgesic activity.

Animals↗
PubMed1981

Chemical and biological properties of 2-pyridyl-benzyl-carbinol.

Three isomers of pyridylbenzylcarbinol were synthetized and their chemical properties and biological activity were studied. Clear dependence between chemical structure and antitumor activity was observed. As expected most active appeared 2-pyridylbenzylcarbinol (alpha-carbinol). It showed significant antitumor activity against subcutaneous tumors of Ehrlich carcinoma. Nemeth-Kellner lymphoma and sarcoma 180. On a chronic treatment schedule tumor inhibition from 60 to 80% was induced. No activity was seen in L1210 and P388 models. In B16 melanoma the significant inhibition of tumor growth was obtained at 200 mg/kg/injection. Tumor inhibitory effect was also observed in Yoshida sarcoma. Depending on a dose and schedule the increase in lifespan from 45 to 147% was achieved. LD50 and MTD were determined and were 750 +/- 87.65 mg/kg and 557.8 mg/kg, respectively. Only slight suppressive effect of alpha-carbinol on immunological system was showed. It concerned mainly immunological reactions with cellular system involved, in which distinct suppressive effects were noted. Specific and nonspecific humoral reactivity was little or not at all affected by alpha-carbinol.

Animals↗
PubMed1981

Synthesis and biological properties of 5-benzoylamino-3-methyl-4-isoxazolocarboxylic acid derivatives.

A series of amides of 5-amino-3-methyl-4-isoxazolocarboxylic acid derivatives was synthesized and tested for antiinflammatory and antibacterial activity. P-etoxyphenylamid and p-chlorophenylamid of 5-benzoylamino-3-methyl-4-isoxazolocarboxylic acid displayed strong antiinflammatory and antibacterial effect. The most potent effect of these amides is accounted for the presence of benzoyl group in position 5 of isoxazole group.

Anti-Inflammatory Agents↗
PubMed1980

Pharmacological studies on p-chlorophenylamide of 3-methyl-5-benzoylaminoizothiazole-4-carboxylic acid (compound ITCL) the preparation of eventual anti-inflammatory effect.

Pharmacological activity of p-chlorophenylamide of 3-methyl-5-benzoylaminoizothiazole-4-carboxylic acid (compound ITCl) was studied with special regard to its anti-inflammatory effect. Compound ITCl is moderately toxic with no distinct circulatory and central effect. On the other hand, it shows strong anti-inflammatory activity in many tests of immunologically specific, nonspecific and infectious inflammations. The greatest efficacy of the compound was noted in the therapy of experimental, immunologically non-specific (xylene, carrageenin and cotton-test) inflammations. Weaker and less regular therapeutic effect was noted in the cases of immunologic inflammations -- mainly in contact reaction to dinitrochlorobenzene. Compound ITCl was ineffective in relation to transplantation barrier. Therapeutic efficacy of the compound was not observed in herpetic inflammation of the skin. On the other hand, a promising therapeutic effect was noticed in relation to cow-pox virus keratitis. Compound ITCl is well tolerated. It shows no toxic effect on white and red blood cells system in a 4-week exposition. Compound ITCl stabilizes cell membranes. Practical aspect of the obtained results was discussed.

Animals↗
PubMed1976

Derivatives of 2-hydroxy-4-mercapto-6-methylpyrimidine-5-carboxylic acid. II. Pirazolo-[3,4-d]-pyrimidine and hydrazinopyrimidine.

Heating of 2-hydroxy-4-mercapto-6-methylpyrimidine-5-carboxylic acid 1 with hydrazine or its derivatives in ethanolic solution gave 4-hydrazino derivatives 10--12. However, at 150--160 degrees in the absence of a solvent after decarboxylation the 4-hydrazino derivatives 13 and 14 were formed. Under similar conditions form 2 (the ethyl ester of 1), 4-methylpyrazole-[3,4-d]-5(H)-pyrimidine-3,6-dione and the corresponding 1--substituted derivatives 3,7,8 of this ring system were obtained. These compounds were easily chlorinated (POCl3/PCl5) in 6 and 3 and 6 position. Compounds 3 and 7 have strong cytostatic activity in vitro and in vivo, compound 13 acts as virostatic and antiinflammatory.

Animals↗
PubMedDate not supplied

Immunotropic activity of vratizolin (ITCL, Denotivir).

The aim of this study was to evaluate immunotropic properties of vratizolin, a known antiviral drug, in several in vitro and in vivo assays in mouse and human models. We demonstrated that vratizolin exerted strong immunosuppressive actions both in the humoral and cellular immune response to SRBC in mice. The compound affected not only the inductive phase of delayed type hypersensitivity (DTH) but also the effector phase of that response. Vratizolin was effective when given intraperitoneally and orally. The inhibitory action of vratizolin was comparable to that of cyclosporin A (CsA), the reference drug. Vratizolin exhibited also suppressory properties with regard to PHA-induced proliferation of human peripheral blood lymphocytes and that effect exceeded the inhibitory action of CsA. We also showed that vratizolin inhibited to some degree LPS-induced cytokine production in human peripheral blood cultures. The activities of TNF-alpha, IL-1 and IL-6 were inhibited on average by 37, 26 and 35%, respectively. This was in contrast to the effects of CsA which strongly inhibited only IL-1 production. Lastly, we demonstrated that vratizolin markedly inhibited growth of several tumor cell lines. In particular, the compound significantly inhibited growth of mouse leukemia L-1210 and human acute lymphoblastoid leukemia CCRF-CEM cell lines. The presented data suggest that the immunosuppressory action of vratizolin, although similar to that of CsA, is mediated by a different mechanism. The properties of vratizolin, described in this report, indicate that the drug should be further investigated for possible immunosuppressory and antitumor application.

Animals↗