- Preparation of synthetic auxin-amino acid conjugates
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Auxin amide conjugates are regulators of the most important auxin, indole-3-acetic acid (IAA), which is considered responsible for many important processes within the plants. Herein, amide conjugates of IAA were synthesized employing a simple and efficient coupling method with WSCI·HCl, a water-soluble condensing reagent, in the presence of 1-hydroxybenzotriazole. IAA conjugates with 10 amino acids along with their corresponding methyl esters were prepared in excellent yields, up to 95%, aiming to facilitate their identification in plant species. Eight IAA-amino acid methyl ester conjugates are characterized here for the first time.
- Revelou, Panagiota-Kyriaki,Constantinou-Kokotou, Violetta
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supporting information
p. 1708 - 1712
(2019/05/15)
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- Tryptophan and thiosemicarbazide derivatives: Design, synthesis, and biological evaluation as potential β-D-galactosidase and β-D-glucosidase inhibitors
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Glycosidases, including β-D-galactosidase and β-D-glucosidase, are involved in a range of metabolic disorders, such as cancer, viral or bacterial infections, and diabetes. Previously, we scanned the pharmacophoric space of these enzymes and had a self-consistent and predictive quantitative structure-activity relationship that was used to identify several β-D-galactosidase and β-D-glucosidase inhibitors via in silico search of structural databases. Guided by the preceding modeling efforts, synthesis of a series of tryptophan and thiosemicarbazide derivatives as β-D-galactosidase and β-D-glucosidase inhibitors that match the generated pharmacophores followed by in vitro bioassay was carried out. Synthesized compounds 3c (37 % inhibition at 100 μM) and 4d (49 % inhibition at 100 μM) exhibited the best inhibitory bioactivities against β-D-galactosidase and β-D-glucosidase, respectively. They can serve as a promising lead compounds for the development of potential glycosidase inhibitors.
- Abu Khalaf, Reema,Abdula, Ahmed Mutanabbi,Mubarak, Mohammad S.,Taha, Mutasem O.
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p. 2529 - 2550
(2015/06/22)
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- Syntheses of IAA- and IPA-amino acid conjugates
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(Chemical Equation Presented) Amino acid derivatives of IAA and IPA are prepared conveniently and efficiently by coupling of readily available 2a-b with diverse free amino acids 3a-g and (3c+3c′) to give compounds 4a-j, (4c+4c′) and (4h+4h′) in 38-70% yie
- Katritzky, Alan R.,Khelashvili, Levan,Munawar, Ali
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supporting information; experimental part
p. 9171 - 9173
(2009/04/11)
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- Therapeutic and diagnostic ligand systems comprising transport molecule binding properties and medicaments containing the same
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The invention relates to transport molecule binding ligand compounds which comprise a therapeutically and/or diagnostically active substance and a carrier molecule-affine substance with a high association constant to the carrier molecule. The invention also relates to medicaments containing these ligand compounds and to diagnostic kits.
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