Regiospecific Reduction of 4,6-Dinitrobenzimidazoles : Synthesis, Characterization, and Biological Evaluation

International audienceThe regiospecific reduction of 4,6-dinitrobenzimidazole derivatives leading to the corresponding 4-amino-6-nitrobenzimidazoles was studied. The identification of the formed product structures was accomplished by spectroscopic and X-ray diffraction data. The anticancer and antiparasitic activities of the synthesized compounds were examined, and promising activities against Toxoplasma gondii and Leishmania major parasites were discovered for certain 4,6-dinitrobenzimidazoles in addition to moderate anticancer activities of the 4-amino-6-nitrobenzimidazole derivatives against T. gondii cells. However, the tumor cell experiments revealed a promising sensitivity of p53-negative colon cancer cells to these compounds. © 2023 The Authors. Chemistry and Biodiversity published by Wiley-VHCA AG, Zurich, Switzerland

Reactions de l'acrylate de methyle et de l'acrylonitrile avec les aldehydes : applications a la synthese d'une #delta#-lactone, de paracyclophanes, d'un cryptand et de podands

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

Nβ-Fmoc-Nβ-Methyl-aza-β3-aminoAcids

International audienceThe potential of peptides as drug candidates is limited by theirpoor pharmacokinetic properties. Many peptides have a short half-life,in vivo half-life, and insufficient oral availability. Inspired bythe N-methylation of peptides as a promising way to rationally improvekey pharmacokinetic characteristics, we report our efforts towardan easy synthesis of new monomers Nβ-Fmoc- Nβ-Me-aza-β3-aminoacids. These synthetic building blocks will be useful for solid-phasesynthesis of new peptidomimetics

Synthesis of aza-β3-homoserine, incorporation of this new aza-β3-amino acid into 26RFa(20-26) and microwave-assisted deprotection of its side chain

International audienc

Synthesis of new (pyrazol-1-yl)(7-nitro-1h-indol-2-yl)ketone derivatives

International audienceThe condensation of 7-nitroindole-2-carbohydrazide derivatives with acetylacetone lead to (pyrazol-1-yl)(7-nitroindol-2-yl)ketones

Rational design of a low molecular weight, stable, potent, and long-lasting GPR103 aza-β3-pseudopeptide agonist

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