Search results for " Synthetic"

showing 2 items of 182 documents

Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action

2015

Dipeptidyl enoates were prepared through a high-yielding two-step synthetic route. They have a dipeptidic structure with a 4-oxoenoate moiety as a warhead with multiple reactive sites. Dipeptidyl enoates were screened against rhodesain and human cathepsins B and L, and were found to be potent and selective inhibitors of rhodesain. Among them (S,E)-ethyl 5-((S)-2-{[(benzyloxy)carbonyl]amino}-3-phenylpropanamido)-7-methyl-4-oxooct-2-enoate (6) was the most potent, with an IC50 value of 16.4 nm and kinact/Ki=1.6×106 m−1 s−1 against rhodesain. These dipeptidyl enoates display a reversible mode of inhibition at very low concentrations and an irreversible mode at higher concentrations. Inhibition…

trypanosomiasisStereochemistrysleeping sicknessCathepsin LDrug Evaluation PreclinicalChemistry Techniques SyntheticInhibition kineticsCysteine Proteinase InhibitorsBiochemistryCathepsin BInhibitory Concentration 50Structure-Activity RelationshipinhibitorsDrug DiscoveryHumansMoietyMolecular Targeted TherapyGeneral Pharmacology Toxicology and PharmaceuticsIC50Volume concentrationrhodesainPharmacologyChemistryOrganic ChemistryDual modeDipeptidesTrypanocidal AgentsCombinatorial chemistryMolecular Docking SimulationCysteine EndopeptidasesKineticsdipeptidyl enoatesTrypanosomiasis AfricanDocking (molecular)Molecular MedicineCysteine thiolateChemMedChem
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Effects of NAA and Ecklonia maxima Extracts on Lettuce and Tomato Transplant Production

2022

Ecklonia maxima and the commercial biostimulants produced from it contain various plant growth regulators that are responsible for the growth stimulation recorded in many crops. Auxins are one of the major plant growth regulators contained in E. maxima extracts. The aim of this research was to evaluate the growth-promoting effect of a seaweed extract from E. maxima on lettuce and tomato transplant production under nursery conditions, and to compare the effect of this extract with an equal concentration of synthetic auxin. Two doses of natural or synthetic exogenous auxins (50 or 100 μg L−1) were supplied to the substrate through the irrigation water with an ebb and flow system, 4, …

vegetable nurserybiostimulantsSolanum lycopersicumLactuca sativaseaweed extractsynthetic auxinSettore AGR/04 - Orticoltura E Floricolturaseedlingnatural auxinAgronomy and Crop Sciencevegetable nursery; seedling; <i>Solanum lycopersicum</i>; <i>Lactuca sativa</i>; seaweed extract; synthetic auxins; natural auxins; biostimulants
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