Michael addition of heteronucleophilic substances to N – Ar substituted maleimides: green approach

A new method for the preparation of the adducts of aromatic hetero nucleophiles (NH, SH, ОH) to the activated C=C bond of N-aryl-substituted maleimides using Michael reaction was developed. A possibility to obtain mono-adducts was demonstrated for 2-aminopyridine derivatives. It was proven that in the case of amino phenols, which possess three potential nucleophilic centers, only the addition to amino group occurs. Utility of the method for the formation of C–C bond in Michael reaction was also demonstrate

Synthesis of Potential Inhibitors of InhA with Pyrrolidine-2,5-dione Core Fragment and Evaluation of their Biological Activity

We report here the discovery, synthesis and screening results of the series of 3-bulky substituted pyrrolidine-2,5-dione derivatives as a novel class of potential inhibitors on InhA, a key enzyme involved in the fatty acid biosynthesis pathway (type II) of M. tuberculosis as well as inhibitors of Mycobacterium tuberculosis H37Rv

Peptide Synthesis in Ionic Liquids (PEPSIL): All You Need is in the Toolbox!

This personal account describes our studies regarding peptide synthesis in ionic liquids (PEPSIL). In addition, we summarize our experiments in which the use of ionic liquids gives simple and promising access to unnatural amino acids in an enantiomerically enriched form. Extension of PEPSIL method to complex structures such as cyclopeptides is also discussed. Some of these cyclopeptides are the direct precursors of bioactive and pharmaceutical compounds

Synthesis and evaluation of β-hydroxytriazoles and related compounds as antitubercular agents

A new series of β-hydroxytriazoles were synthesized and evaluated as Mycobacterium tuberculosis inhibitors. Our strategy implied the synthesis of alkyne precursors through a Barbier reaction between benzaldehydes and propargyl bromide followed by click chemistry to afford substituted β-hydroxyl benzyltriazoles. These compounds are also key intermediates either for oxidation reactions leading to α,β-diketotriazoles or for elimination reactions affording styryl triazoles. Evaluation of all new compounds for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv resulted in compounds with MIC up to 7 μM

Effect of the Nature of Surfactant on the Reactivity of C,N-diphenylnitrone towards Acrylonitrile in Different Microemulsions Systems

The present work provides an insight into the effect of the nature of surfactant (cationic, anionic), a component of water- and oil-borne microemulsions, on the reaction rate of 1,3-dipolar cycloaddition of C,N-diphenylnitrone with acrylonitrile. The electrostatically attractive character of the cationic surfactant, would bring the reactants closer to each other; hence, a rate enhancement would ensue, particularly within the water-rich zone. Besides the fact that acrylonitrile played a dual role, as a component of the microemulsion and a dipolarphile in the cycloaddition reaction, made the work-up advantageously sound. Additionally, the increase in reagents molar ratio was found to promote higher reactivity

Synthesis, In Silico, and In Vitro Evaluation of Anti-Leishmanial Activity of Oxadiazoles and Indolizine Containing Compounds Flagged against Anti-Targets

Due to the lack of approved vaccines against human leishmaniasis and the limitations of the current chemotherapy inducing side effects and drug resistance, development of new, effective chemotherapeutic agents is essential. This study describes the synthesis of a series of novel oxadiazoles and indolizine-containing compounds. The compounds were screened in silico using an EIIP/AQVN filter followed by ligand-based virtual screening and molecular docking to parasite arginase. Top hits were further screened versus human arginase and finally against an anti-target battery to tag their possible interactions with proteins essential for the metabolism and clearance of many substances. Eight candidate compounds were selected for further experimental testing. The results show measurable in vitro anti-leishmanial activity for three compounds. One compound with an IC50 value of 2.18 mu M on Leishmania donovani intramacrophage amastigotes is clearly better positioned than the others as an interesting molecular template for further development of new anti-leishmanial agents

Inhibiteurs sulfinamoyles et sulfamoyles de coniferyl alcool deshydrogenase : synthese, complexation et cinetique d'hydrolyse basique; approche du mecanisme d'inhibition

SIGLECNRS T 55754 / INIST-CNRS - Institut de l'Information Scientifique et TechniqueFRFranc

Dérivés phénoliques à activités antiathérogènes

TOULOUSE3-BU Sciences (315552104) / SudocSudocFranceF

Réactivité d'a,ß-époxyaldéhydes avec le (2-triméthylsilyloxy)-acrylate d'éthyle (synthèse en série ulosonique, fonctionnalisation et application biologique)

TOULOUSE3-BU Sciences (315552104) / SudocSudocFranceF