Pyrimidine ring transformations to 6-nitroazolo[1,5-a]pyrimidines ? A one-step synthesis of azolylamino derivatives of nitropyridine

1987 ◽  
Vol 23 (6) ◽  
pp. 709-709 ◽  
Author(s):  
V. L. Rusinov ◽  
T. L. Pilicheva ◽  
A. A. Tumashov ◽  
O. N. Chupakhin
Keyword(s):  
Pyrimidine Ring ◽  
Ring Transformations ◽  
One Step ◽  
Derivatives Of

scholarly journals Affinity chromatography and inhibition of chorismate mutase-prephenate dehydrogenase by derivatives of phenylalanine and tyrosine

1977 ◽  
Vol 165 (1) ◽  
pp. 121-126 ◽  
Author(s):  
G D Smith ◽  
D V Roberts ◽  
A Daday
Keyword(s):  
Affinity Chromatography ◽  
Competitive Inhibitor ◽  
Chorismate Mutase ◽  
Prephenate Dehydrogenase ◽  
Step Procedure ◽  
One Step ◽  
High Degree ◽  
Sepharose 4B ◽  
Derivatives Of

Several derivatives of phenylalanine and tyrosine were prepared and tested for inhibition of chorismate mutase-prephenate dehydrogenase (EC 1.3.1.12) from Escherichia coli K12 (strain JP 232). The best inhibitors were N-toluene-p-sulphonyl-L-phenylalanine, N-benzenesulphonyl-L-phenylalanine and N-benzloxycarbonyl-L-phenylalanine. Consequently two compounds, N-toluene-sulphonyl-L-p-aminophenylalanine and N-p-aminobenzenesulphonyl-L-phenylalanine, were synthesized for coupling to CNBr-activated Sepharose-4B. The N-toluene-p-sulphonyl-L-p-aminophenylalanine-Sepharose-4B conjugate was shown to bind the enzyme very strongly at pH 7.5. The enzyme was not eluted by various eluents, including 1 M-NaCl, but could be quantitatively recovered by washing with buffer of pH9. Elution was more effective in the presence of 10 mM-1-adamantaneacetic acid, a competitive inhibitor of the enzyme. This affinity-chromatography procedure results in a high degree of purification of the enzyme and can be used to prepare the enzyme in a one-step procedure from the bacterial crude extract. Such a procedure may therefore prove useful in studying this enzyme in a state that closely resembles that in vivo.

Two in one: bifunctional derivatives of trolox acting as antimalarial and antioxidant agents

2020 ◽  
Vol 12 (20) ◽  
pp. 1845-1854
Author(s):  
Florence Souard ◽  
Edwige Nicolle ◽  
Delphine Cressend ◽  
Alexis Valentin ◽  
Ahcène Boumendjel
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
In Vivo Studies ◽  
Chemical Libraries ◽  
Falciparum Strain ◽  
Antioxidant Agents ◽  
One Step ◽  
Set Up ◽  
Derivatives Of

Background: The aim of the present work was to set-up compounds that are able to act simultaneously as antimalarial and antioxidants. Trolox, a known antioxidant was chosen as a core structure to ensure the antioxidant activity and contribute to antiplasmodial effect. Results: Ten compounds were prepared in one step and evaluated on chloroquino-sensitive (3D7) and chloroquino-resistant (FcB1) strains of Plasmodium falciparum. The most active compound (3d) shows antiplasmodial activity in the range of chloroquine against chloroquino-sensitive and chloroquino-resistant P. falciparum strain. The antioxidant activity of (3d) was conducted through four tests and was found to be more potent than trolox itself and L-ascorbic acid. Conclusion: Compound (3d) can be considered as an excellent lead molecule for further in vivo studies. This study paves the way for building large chemical libraries to be investigated in the field of malaria.

scholarly journals Pyrrolidine and oxazolidine ring transformations in proline and serine derivatives of α-hydroxyphosphonates induced by deoxyfluorinating reagents

RSC Advances ◽  
2018 ◽  
Vol 8 (43) ◽  
pp. 24444-24457 ◽  
Author(s):  
Patrycja Kaczmarek ◽  
Magdalena Rapp ◽  
Henryk Koroniak
Keyword(s):  
Ring Transformations ◽  
Derivatives Of

Diastereoselective reactions of hydroxyphosphonates from proline or serine with fluorinating agents yielding piperidine-, oxazolidine-, aziridine- or sulfonate phosphonates were reported.

scholarly journals A One-Step Microwave-Assisted Synthetic Method for an O/S-Chemoselective Route to Derivatives of the First Adenosine A3 PET Radiotracer

Molecules ◽  
2014 ◽  
Vol 19 (4) ◽  
pp. 4076-4082
Author(s):  
Karem Shanab ◽  
Catharina Neudorfer ◽  
Wolfgang Holzer ◽  
Markus Mitterhauser ◽  
Wolfgang Wadsak ◽  
...  
Keyword(s):  
Synthetic Method ◽  
Microwave Assisted ◽  
One Step ◽  
Derivatives Of

Synthesis of 3-(5-Alkyl-4-acetyl(ethoxycarbonyl))-2-propenoates from Derivatives of 3-Phenoxy-2-furylmethylene

1992 ◽  
Vol 57 (8) ◽  
pp. 1684-1692 ◽  
Author(s):  
Štefan Marchalín ◽  
Vladimír Mlynárik ◽  
Anna Staňová ◽  
Dušan Ilavský
Keyword(s):  
Acid Hydrolysis ◽  
Hydrogen Chloride ◽  
Pure Form ◽  
Geometric Isomers ◽  
Transition Mechanism ◽  
One Step ◽  
Hydrolysis Of ◽  
Derivatives Of ◽  
Trisubstituted Furans

3-(2-Furyl)propenoates IV-VIII were obtained by treatment of 5-phenoxy-2-furylmethylene derivatives I-III with alcoholic hydrogen chloride in one step. The probable transition mechanism of synthons I-III into the 2,4,5-trisubstituted furans is presented. The geometric isomers E-IV, Z-V and Z-VI, isolated in pure form, were transformed into the corresponding acids E-IX, Z-IX and E-X by base-catalyzed hydrolysis. Acid hydrolysis of the 1,3-diketone I afforded (4Z,6Z)-6-acetyl-7-hydroxy-2,4,6-octatrien-4-olide (XI). Structure of the products was verified by spectral (IR, UV, NMR and mass) methods.

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