The Experts below are selected from a list of 44343 Experts worldwide ranked by ideXlab platform
Michel Baltas - One of the best experts on this subject based on the ideXlab platform.
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Study of the Two Steps and One-Pot Two-Step Mechanochemical Synthesis of Annulated 1,2,4-Triazoles
ACS Sustainable Chemistry & Engineering, 2020Co-Authors: Lori Gonnet, Michel Baron, Alain Chamayou, Brigitte Guidetti, Christiane André-barrès, Christophe Menendez, Rachel Calvet, Michel BaltasAbstract:The mechanochemical synthesis of 1,2,4-triazoles by using a planetary ball-mill is studied starting from hydralazine hydrochloride. Excellent conditions were found for achieving total conversion to intermediate Hydrazones in a few minutes in the presence of pyrogenic S13 silica as grinding auxiliary. The conversion to annulated 1,2,4-triazoles was optimal with iodobenzene diacetate (IBD) when using nonphenolic Hydrazones, while SeO2 was found to be efficient for phenolic compounds. The one-pot two-step synthesis was also successfully conducted for the first time leading to annulated 1,2,4-triazoles. Finally, green metrics showed the efficiency of the method in comparison to the conventional syntheses of hydrazone 10 and triazole 13.
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solvent free mechanochemical route for green synthesis of pharmaceutically attractive phenol Hydrazones
ChemInform, 2015Co-Authors: Paulo F M Oliveira, Michel Baron, Alain Chamayou, C Andrebarres, Brigitte Guidetti, Michel BaltasAbstract:Various substituted organic hydrazines and phenol aldehydes efficiently react in a vibratory ball-mill leading to Hydrazones with high level of purity and without the use of any environmentally unadvisable reagents, additives or catalysts.
Yongmiao Shen - One of the best experts on this subject based on the ideXlab platform.
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Visible-light mediated directed perfluoroalkylation of Hydrazones
Organic & biomolecular chemistry, 2017Co-Authors: Peng Zhi, Wei Wang, Jian-jun Shi, Yongmiao ShenAbstract:Perfluoroalkylation of N-alkylHydrazones has been achieved via visible light mediated photoredox reactions between the hydrazone and perfluoroalkyl iodide (RfI). This protocol provides a convenient and efficient access to a series of perfluoroalkylated aromatic aldehyde Hydrazones which tolerates a wide range of functional groups on the aromatic ring, and allows the use different types of primary and secondary perfluoroalkyl iodides with up to eight carbon atoms. Furthermore, aliphatic aldehyde Hydrazones and N-monosubstituted Hydrazones which are unreactive in previously reported hydrazone perfluoroalkylation reactions now take part in the reaction under our reaction conditions to give a satisfactory yield of products. Stern–Volmer quenching studies and spin-trapping experiments indicated that these reactions proceed by free radical addition of the Rf radical to the azomethine atom followed by one electron oxidation of the hydrazyl radical and deprotonation of the diazenium cation.
Jiří Klimeš - One of the best experts on this subject based on the ideXlab platform.
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Investigation of the stability of aromatic Hydrazones in plasma and related biological material.
Journal of pharmaceutical and biomedical analysis, 2008Co-Authors: Petra Kovaříková, Zlata Mrkvičková, Jiří KlimešAbstract:Abstract Novel aromatic Hydrazones derived from pyridoxal isonicotinoyl hydrazone (PIH) are interesting compounds from the viewpoint of their pharmacodynamic activity. However, they were recently shown to suffer from relatively short biological half-lives. The purpose of the present study was to investigate the stability of novel aroylHydrazones in plasma and related biological media in order to reveal its potential involvement in the pharmacokinetics of these drugs. Three different aroylHydrazones (pyridoxal isonicotinoyl hydrazone – PIH, salicylaldehyde isonicotinoyl hydrazone – SIH and pyridoxal 2-chlorobenzoyl hydrazone – o -108) were incubated in plasma from different species, plasma ultrafiltrate, bovine serum albumin, RPMI cell medium and phosphate buffer saline (PBS) at 37 °C. Stability of these compounds was determined using precise, selective and validated HPLC methods. Although the aroylHydrazones were relatively stable in PBS, they underwent rapid degradation in plasma. Plasma proteins as well as low molecular weight components were involved in this matter. Furthermore, the products of hydrazone bond splitting revealed in this study were also found in the chromatograms from pharmacokinetic experiments. In the light of short biological half-lives determined in vivo , these in vitro findings strongly suggest that hydrolysis of investigated aromatic Hydrazones in plasma could have a significant impact on their pharmacokinetics. Furthermore, these results also suggest that plasma stability of other novel drug candidates containing the hydrazone bond deserves to be considered.
T Soga - One of the best experts on this subject based on the ideXlab platform.
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discovery of novel thieno 2 3 d pyrimidin 4 yl hydrazone based inhibitors of cyclin d1 cdk4 synthesis biological evaluation and structure activity relationships
Bioorganic & Medicinal Chemistry Letters, 2009Co-Authors: Takao Horiuchi, Jun Chiba, Kouichi Uoto, T SogaAbstract:Abstract The synthesis and evaluation of new analogues of thieno[2,3-d]pyrimidin-4-yl Hydrazones are described. 2-Pyrdinecarboxaldehyde [6-(tert-butyl)thieno[2,3-d]pyrimidine-4-yl]hydrazone derivatives have been identified as cyclin-dependent kinase 4 (CDK4) inhibitors. The potency, selectivity profile, and structure–activity relationship of this series of compounds are discussed.
Michel Baron - One of the best experts on this subject based on the ideXlab platform.
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Study of the Two Steps and One-Pot Two-Step Mechanochemical Synthesis of Annulated 1,2,4-Triazoles
ACS Sustainable Chemistry & Engineering, 2020Co-Authors: Lori Gonnet, Michel Baron, Alain Chamayou, Brigitte Guidetti, Christiane André-barrès, Christophe Menendez, Rachel Calvet, Michel BaltasAbstract:The mechanochemical synthesis of 1,2,4-triazoles by using a planetary ball-mill is studied starting from hydralazine hydrochloride. Excellent conditions were found for achieving total conversion to intermediate Hydrazones in a few minutes in the presence of pyrogenic S13 silica as grinding auxiliary. The conversion to annulated 1,2,4-triazoles was optimal with iodobenzene diacetate (IBD) when using nonphenolic Hydrazones, while SeO2 was found to be efficient for phenolic compounds. The one-pot two-step synthesis was also successfully conducted for the first time leading to annulated 1,2,4-triazoles. Finally, green metrics showed the efficiency of the method in comparison to the conventional syntheses of hydrazone 10 and triazole 13.
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solvent free mechanochemical route for green synthesis of pharmaceutically attractive phenol Hydrazones
ChemInform, 2015Co-Authors: Paulo F M Oliveira, Michel Baron, Alain Chamayou, C Andrebarres, Brigitte Guidetti, Michel BaltasAbstract:Various substituted organic hydrazines and phenol aldehydes efficiently react in a vibratory ball-mill leading to Hydrazones with high level of purity and without the use of any environmentally unadvisable reagents, additives or catalysts.
