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Biomedical subjects

Z Machoń

Publications and source records attributed to Z Machoń.

At least 19 recordsLinked to original sources
PubMed1999

Synthesis and immunological activity of new 5-amino-3-methyl 4-amido and 4-ureilene isoxazole derivatives.

5-Amino-3-methylisoxazole-4-carboxylic acid amides and ureilenes have been synthesized from 5-amino-3-methylisoxazole-4-carbonyl azide. The compounds were investigated for potential immunotropic activity in several immunological tests. The most interesting suppressory activities in the humoral and cellular immune response were compared to activities of analogous compounds previously described as immunostimulatory.

Adjuvants, Immunologic↗
PubMed1997

Synthesis and structure elucidation of 5-aminomethinimino-3-methyl-4-isoxazolecarboxylic acid phenylamides and their immunological activity.

A series of 5-aminomethinimino-3-methyl-4-isoxazolecarboxylic acid phenylamides 4 has been prepared by condensation of 5-amino-3-methyl-4-isoxazolecarboxylic acid phenylamides 1 with trichloroacetic aldehyde. Alcoholysis of trichloro derivatives 2 gave 5-alkoxymethine derivatives 3 which, on reaction with an appropriate amine, formed the corresponding compounds 4. The compounds obtained were evaluated for their immunological activity. The properties of three compounds, described in this report, permitted inhibition of the immune response in all possible ways: diminishing both types of immune response (4d), humoral immune response (4a), or cellular immune response (4c). Preparation 4d is comparable in its effectiveness to CsA, so it may be potentially used as an agent for prolongation of the function of transplanted organs. Two other compounds may potentially be used in cases where only one type the immune response is required for combating pathogen invasion.

Adjuvants, Immunologic↗
PubMed1995

Antitumor and immunosuppressive activity of Merbarone's analogues and arylidenehydrazinopyrimidines.

The synthesis of Merbarone's analogues, the 4-thio- or 4-oxo derivatives of 5-carbamoyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine is described, starting from 5-carboxy-6-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidine+ ++. That was also used as staring material for synthesis of NCS624947 analogues, the 4-arylidenehydrazino-5-carbamoylpyrimidines. The reduction of arylidenehydrazinopyrimidines with hydrogen on Pd/C was also performed. The obtained compounds were successfully tested for anticancer and immunomodulating activity.

Animals↗
PubMed1993

Synthesis and biological properties of 5-hydroxy-methylpyrimidines.

Reduction of 4-arylamine-6-methyl-2-phenyl-5-pyrimidine carboxylic acid and its ethyl esters as well as 5,7-dihydrofuro (3,4-d)-pyrimidines resulted in obtaining some 4-arylamine-6-methyl-2-phenyl-5-hydroxymethylpyrimidines exhibiting strong immunomodulatory and cytostatic properties.

Adjuvants, Immunologic↗
PubMed1992

Synthesis of isothiazole derivatives with potential biological activity.

The synthesis of acyl and ureido derivatives of substituted amides of 3-methyl-5-aminoisothiazole-4-carboxylic acid is presented. The structures of the compounds obtained were established on the basis of IR, 1H NMR and elemental analysis. The influence on the circulatory system of the derivatives was investigated. All structures of the compounds obtained were fully confirmed by IR and 1H NMR as well as by elemental analysis (Table).

Animals↗
PubMed1990

[Imidazopyrimidodiazepines--new heterocyclic system; synthesis and properties].

The synthesis of the new tricyclic system ring 6-methyl-2,3,10,11-tetrahydroimidazo (1',2',3'-CD) pyrimido (5,4-b) (1,4) diazepinediones-5,8 is described. The 4-aryl- and 5-amino-imidazopyrimidodiazepines have also been obtained. The synthesis started from derivatives of 2-hydroxy-6-methyl-5-pyrimidine carboxylic acids. Some of the chemical and biological properties of new compounds are described.

Animals↗
PubMed1990

Pyrimidobenzodiazepines. Synthesis of pirenzepine analog.

The synthesis of Pyrimido[4,5-b][1,5]benzodiazepine derivatives from 4-(o-aminophenylene)amino-5-ethoxy-carbonyl-1,2-dihydro-6-methyl-2 - oxopyrimidine has been described. Pyrimidobenzodiazepine 5 alkylated with N-methyl-N'-chloroacetyl-piperazine gives a product related to pirenzepine. Compound 5 shows weak antianxiety and antidepressive action.

Animals↗
PubMed1988

Synthesis of p-menthane derivatives with potential biological activity.

The synthesis of amino ketones and amino alcohols in p-menthane series is presented. These compounds were obtained in Mannich reaction, starting from the unsaturated ketone p-mentha-6,8-dien-2-one and its saturated analogue p-menthan-2-one. The structures of the compounds obtained were established by means of chemical transformations and elemental and spectral (IR, 1H NMR) analysis. The compounds obtained were subjected to the pharmacological investigations.

Amino Alcohols↗
PubMed1987

Isothiazolopyrimidines--new group of anticancer agents. I.

Synthesis and biological properties of 27 derivatives of 5-amino-3-methylisothiazolo[5,4-d]pyrimidine-4-dione and of 3-methyl-5-semicarbazido-4-isothiazolocarboxylic acid ethyl esters are discussed. 5-Amino-3-methylisothiazolo[5,4-d]pyrimidine-4-dione was converted by reaction with aldehydes into Schiff bases, which under reduction of NaBH4, were transformed into appropriate N-methylene analogs. 3-Methyl-5-semicarbazido-4-isothiazolocarboxylic acid ethyl esters in reaction with aldehydes were converted into benzylidene derivatives. Some of the compounds obtained, especially those of Schiff base structure, displayed strong activity against L-1210 leukemia, Sa-180 sarcoma. Ehrlich carcinoma and Nemeth Kellner lymphoma.

Animals↗
PubMed1987

Isothiazolopyrimidines--new group of anticancer agents. II.

In reactions of 5-aminoisothiazolopyrimidines 1 with glycosilisothiocyanates and phenyl isocyano- or isocyanates, N-glycosilo-N-phenylo- and N-isothiazolopyrimidinothiocarbamides type II were obtained. The same compound--5-aminoisothiazolopyrimidine 1 in reaction with glucose, arabinose and ribose bromoderivatives was converted into N-glycosiloaminoisothiazolopyrimidies type 3. Some of the newly synthetized compounds appeared effective against L-1210 leukemia and Sa-180 sarcoma.

Animals↗
PubMed1985

Synthesis of perhydropyrazino [1,2-c] pyrimidine derivatives.

The reaction of 1-benzoyl-2-oxo-4,6-dihydroxyazetino-[3,2-d] pyrimidine (III) with diethanolamine affords the amide (IV). Heating of the last with SOCl2 yields 2-beta-chloroethyl-8-hydroxy-9-benzoylamino-perhydropyrazino [1,2-c] pyrimidine-1,6-dione (VI). Reaction of compound (VI) with different amines gives the respective 2-beta-aminosubstituted derivatives (VII-XIII). Some of the obtained compounds showed central activity.

Animals↗
PubMed1983

Chemical, pharmacological and oncostatic properties of 5-(4'-hydroxybenzylidenoimino)-4, 6-diketo-4, 5, 6, 7-tetrahydropyrimidine-[4, 5-d]-3-methyl-isothiazole (compound IP-10).

Advanced preclinical studies on IP-10 preparation (4,6-diketo-4, 5, 6, 7-tetrahydropyrimidine-[4, 5-d]-3-methyl-isothiazole) were carried out. The drug was shown to be devoid of the irritating local effect, mildly toxic and hardly absorbing when administered per os. The toxic effect showed tendency toward cumulation. In the long-term exposure it did not affect either the elements of peripheral blood or parenchymatous organs. It exerted slight hypotensive effect on the circulatory system but only after intravenous administration. In relation to the smooth muscle organs and central nervous system, IP-10 was only slightly active. Weak effect of the compound was observed with bacteria and fungi. In the case of transplantable tumors, its activity was differentiated. It exerted a significant effect in relation to leukemia, melanoma B-16, Ehrlich carcinoma and Nemeth-Kellner lymphoma. As other isothiasole derivatives, IP-10 exhibits an interesting pharmacological, easy to render activity; particular attention should be paid to its oncostatis activity.

Animals↗