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Oleg Melnyk - One of the best experts on this subject based on the ideXlab platform.

  • Synthesis of glyoxylyl peptides using an Fmoc-protected α,α′-diaminoacetic Acid Derivative
    Journal of Peptide Science, 2020
    Co-Authors: Oleg Melnyk
    Abstract:

    The synthesis of glyoxylyl peptides by coupling the masked Glyoxylic Acid Derivative (FmocNH)2CHCO2H, 1, to a peptidyl resin assembled using Fmoc/tert-butyl chemistry has been described recently. Deprotection and cleavage of the peptide from the solid support using TFA was followed by unmasking of the glyoxylyl group in solution in the presence of DBU. [] The glyoxylyl peptide was thus generated using non-oxidizing conditions by comparison with the method based on the periodic oxidation of a seryl-precursor. However, base treatment of the (FmocNH)2CHCO2-peptide led to the formation of a byproduct besides the desired glyoxylyl peptide. This paper describes an optimized procedure for unmasking the Fmoc-protected α,α′-diaminoacetic Acid moiety in solution which suppressed byproduct formation. Also presented is a series of experiments that permitted a structure and a mechanism of formation for the byproduct to be suggested. Copyright © 2005 European Peptide Society and John Wiley & Sons, Ltd.

  • a novel lipophilic Glyoxylic Acid Derivative for the lipidation of peptides using salt free hydrazone ligation
    Tetrahedron Letters, 2000
    Co-Authors: Dominique Bonnet, Line Bourel, Helene Grasmasse, Oleg Melnyk
    Abstract:

    Abstract A lipophilic vector, composed of a palmitoyl and glyoxylyl group linked by a 1,3-diaminopropane moiety, was found to react rapidly and almost quantitatively with N-terminal α-hydrazino acetyl peptides to give the corresponding hydrazones. The ligation was performed in salt-free conditions, using a 95/5 mixture of 2-methyl-propan-2-ol/water.

Dominique Bonnet - One of the best experts on this subject based on the ideXlab platform.

R V Lutsenko - One of the best experts on this subject based on the ideXlab platform.

  • experimental assessment of 2 oxyindolin 3 Glyoxylic Acid Derivative anticonvulsant effect
    Kazanskiy meditsinskiy zhurnal, 2015
    Co-Authors: R V Lutsenko
    Abstract:

    Aim. To explore the anticonvulsant effect of 2-oxyindolin-3-Glyoxylic Acid Derivative on the model of acute myoclonic seizures caused by pentylenetetrazol, picrotoxin and thiosemicarbazide. Methods. Median effective dose (ED50) of 2-hydro-N-naphthalene-1-yl-2-(2-oxy-1,2-dyhydro-indole-3-ylidene)-acetamide diethyl ether was determined by the maximal electroshock test in experiments on adult Wistar rats of both gender. The effect of median effective dose prophylactic administration of the study medication and comparators - diazepam and sodium valproate - on chemo-induced epileptogenesis was explored. Introduction of proconvulsant drugs (pentylenetetrazol, picrotoxin and thiosemicarbazide) was accompanied by the development of seizures, which was estimated by the intensity of seizures (points), latent period of seizures onset (seconds), the number of convulsive attacks, seizures, duration (seconds) and the number of survived animals in each group. Results. Median effective dose of 2-oxyindolin Derivative was 12 mg/kg as measured by maximal electroshock test. This dose of the test compound, similar to diazepam, effectively reduced the severity of seizures caused by pentylenetetrazol, seen as the increased duration of latent period before the seizures onset by 1.9 times, decreased severity of seizures by 1.7 times, decreased number of seizures by 2.1 times, and decreased seizure duration by 2.3 times together with lower mortality. The prophylactic administration of the substance has extended the latent period of seizures by 2.0 times, significantly reduced the number, intensity and duration of seizures, decreased the mortality after administration of picrotoxin. Also, 2-oxyindolin Derivative significantly increased the latent period of seizures onset and reduced the severity of seizures due to thiosemicarbazide. At that, the study substance was not inferior in anticonvulsant activity compared to the diazepam as the reference drug. Conclusion. The dose of 12 mg/kg of 2-hydro-N-naphthalene-1-yl-2-(2-oxy-1,2-dyhydro-indole-3-ylidene)-acetamide was effective in preventing seizures associated with gamma-aminobutyric Acid (GABA)-convulsants.

Line Bourel - One of the best experts on this subject based on the ideXlab platform.

Helene Grasmasse - One of the best experts on this subject based on the ideXlab platform.