Search results

1

Simple synthesis of 3-acyl-5-alkyl(aryl)isoxazoles from terminal alkynes and nitrates of alkaline metals or ammonium

100%

Rogachev V., Filimonov V., Kulmanakova J., Yusubov M., Bender W.

Open Chemistry

|

2005

|

vol. 3

|

issue 3

370-376

EN

A simple and general synthesis of 3-acyl-5-alkyl(aryl)isoxazoles by reaction of terminal alkynes with nitrates in acetic acid in the presence of SO3 or alkaline salts is described.

2

Synthesis, immunosuppressive properties, mechanism of action and X-ray analysis of a new class of isoxazole derivatives

88%

Bąchor U., Ryng S., Mączyński M., Artym J., Kocięba M., Zaczyńska E., Kochanowska I., Tykarska E., Zimecki M.

|

2019

|

vol. 76

|

issue 2

251-263

EN

In the search for potential therapeutics, isoxazole derivatives are still objects of interest. Previously described immunoregulatory properties of 5-amino-3-methyl-4-isoxazolecarboxylic acid (AC) benzylamides prompted us to synthesize a new class of compounds of immunotropic activity. A series of new compounds containing the isoxazole moiety were synthesized using Passerini three-component reaction. The effects on phytohemagglutinin A (PHA)-induced proliferation of human peripheral blood mononuclear cells (PBMC), production of tumor necrosis factor alpha (TNF α) in human whole blood cultures stimulated with lipopolysaccharide (LPS) and two-way mixed lymphocyte reaction (MLR) of PBMC, were investigated. Also, the effect of 1-(cyclohexylcarbamoyl)cyclohexyl 5-amino-3-methylisoxazole-4-carboxylate (PUB1) on the expression of signaling molecules associated with cell apoptosis in Jurkat cells was also determined. The results showed that the compounds inhibited to various degree mitogen-induced PBMC proliferation in a dose-dependent manner and TNF α production at 10 μg/ml. PUB1 compound, selected on the basis of its strongest antiproliferative activity, was also shown to inhibit MLR. The molecular data suggest that immunosuppressive action of PUB1 depended on induction of Fas and elevation of caspase 8 expression. In summary, we revealed immunosuppressive properties of a new class of isoxazoles and established the mechanism of action of a representative PUB1 compound.

3

Synthesis, spectral studies and antimicrobial activity of newly chalcones and isoxazoles in diphenyl amine derivatives

88%

Bhoraniya N. C., Purohit D. M.

World News of Natural Sciences

|

2024

|

vol. 54

17-25

EN

A new series of compounds, namely 2-{[4'-(3''-aryl)-2''-propene-1''-one-phenyl]amino}benzoic acids (3a-3j) and 2-{[4'-(5''-aryl)isoxazol-3''-yl]phenyl amino} benzoic acids (4a-4j), were synthesized. The structures of these compounds were confirmed by 1H NMR, IR, Mass spectral analysis. The compounds (3a-3j) and (4a-4j) have been evaluated their antimicrobial activity.

4

Synthesis and Biological Evaluation of Some New Pyridines, Isoxazoles and Isoxazolopyridazines Bearing 1,2,3-Triazole Moiety

75%

hassan a., Rashdan H. R., nabil s., elnagar d.

|

2019

|

vol. 76

|

issue 3

469-482

EN

Some new isoxazole derivatives 3a-d were synthesized via the reaction of 3-(dimethylamino)-1-(5-methyl-1-(3-nitrophenyl)-1H-1,2,3-triazol-4-yl)prop-2-en-1-one (1) with different hydroximoyl chlorides derivatives 2a-d. From these new isoxazoles 3a-d a new series of isoxazolopyridazines 4a-d was derived using hydrazine hydrate. In addition, enaminone 1 was reacted with ethyl acetoacetate to afford the corresponding ester derivative 6, the latter was submitted to react with different chemical reagents to obtain a variety of bioactive substituted pyridine derivatives. The azido derivative 14, was used as the key molecule for the synthesis of new urea and aryl carbamate derivatives upon its reaction with different amines and phenol through Curtius rearrangement. The chemical structures of all new compounds were investigated from their spectral and microanalytical data. The synthesized compounds were tested for their pharmacological potency as, anti-hepatic cancer and anti-microbial agents. Most of the tested compounds showed good anti-hepatic cancer results comparing with the standard drug doxorubicin especially when their toxic effects on the normal cell lines were studied. Referring to the anti-microbial test most of the compounds showed strong effects.

Refine search results

2 Acta Poloniae Pharmaceutica - Drug Research

1 Open Chemistry

1 World News of Natural Sciences

1 2024

2 2019

1 2005

1 Artym J.

1 Bender W.

1 Bhoraniya N. C.

1 Bąchor U.

1 Filimonov V.

1 Kochanowska I.

1 Kocięba M.

1 Kulmanakova J.

1 Mączyński M.

1 Purohit D. M.

1 Rashdan H. R.

1 Rogachev V.

1 Ryng S.

1 Tykarska E.

1 Yusubov M.

1 Zaczyńska E.

1 Zimecki M.

1 elnagar d.

1 hassan a.

1 nabil s.

Simple synthesis of 3-acyl-5-alkyl(aryl)isoxazoles from terminal alkynes and nitrates of alkaline metals or ammonium

Synthesis, immunosuppressive properties, mechanism of action and X-ray analysis of a new class of isoxazole derivatives

Synthesis, spectral studies and antimicrobial activity of newly chalcones and isoxazoles in diphenyl amine derivatives

Synthesis and Biological Evaluation of Some New Pyridines, Isoxazoles and Isoxazolopyridazines Bearing 1,2,3-Triazole Moiety