Listar por autoría "711a2b25-d389-4e87-8b74-b4259e3712de"
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Advances in the Development of SARS-CoV-2 Mpro Inhibitors
MDPI (2022-04-14)Since the outbreak of COVID-19, one of the strategies used to search for new drugs has been to find inhibitors of the main protease (Mpro) of the virus SARS-CoV-2. Initially, previously reported inhibitors of related ... -
Amidation through carbamates
Elsevier (2009)N-Alkyl carbamates of primary amines are easily converted into amides under treatment with Grignard reagents. Consequently, primary amines can be converted into amides in a one-pot reaction through carbamate protection and ... -
Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates
Elsevier (2018-09-01)A family of dipeptidyl enoates has been prepared and tested against the parasitic cysteine proteases rhodesain, cruzain and falcipain-2 related to sleeping sickness, Chagas disease and malaria, respectively. They have also ...
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Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–7
MDPI (2020)Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes is a series of editorials which is published on a biannual basis by the Editorial Board of the Medicinal Chemistry section of the journal ...
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Catalytic enantioselective epoxidation of nitroalkenes
Royal Society of Chemistry (2016)Nitroepoxides are potentially exploitable as synthons with vicinal electrophilic centers. Nevertheless, although advances have been made in the field, enantioselective epoxidation of nitroalkenes is still a challenging ...
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Cuestiones previas en Aula Virtual en los laboratorios de Química Orgánica
Colegio Oficial de Químicos de Galicia (2023-05-18)En las prácticas de laboratorio de las asignaturas de Química Orgánica es habitual introducir en el guion de prácticas una serie de preguntas previas que acompañan a la descripción de los experimentos y procedimientos ...
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Design and Synthesis of Cysteine Protease Inhibitors
MDPI (2017-09-08)We have been preparing new dipeptidyl inhibitors against parasitic cysteine proteases cruzain (related to Chagas disease) and rhodesain (related to Sleeping Sickness disease), and against human cathepsins. Inhibitors display ...
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Design, Synthesis and Evaluation of Fluorescent Analogues of Abscisic Acid
Wiley (2020-07-13)A fluorescent analogue of abscisic acid has been prepared by combining (S)‐abscisic acid (ABA) with nitrobenzoxadiazole (NBD) fluorophore using ethanol amine as a linker. Isomerization of the double bond at the side chain ...
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Development and validation of a liquid chromatography isotope dilution mass spectrometry method for the reliable quantificationof alkylphenols in environmental water samples by isotopepattern deconvolution
Copyright © 2015 Elsevier (2014-02-07)We present here a new measurement method for the rapid extraction and accurate quantification of technical nonylphenol (NP) and 4-t-octylphenol (OP) in complex matrix water samples by UHPLC-ESI-MS/MS. The extraction of ...
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Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action
Wiley (2015-07-14)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 ...
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Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain
American Chemical Society (2016)Dipeptidyl nitroalkenes are potent reversible inhibitors of cysteine proteases. Inhibitor 11 resulted to be the most potent one with Ki values of 0.49 and 0.44 nM against rhodesain and cruzain, respectively. According to ...
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Dynamic Kinetic Asymmetric Ring-Opening/Reductive Amination Sequence of Racemic Nitroepoxides with Chiral Amines: Enantioselective Synthesis of Chiral Vicinal Diamines
American Chemical Society (2013-05)We report a highly diastereoselective synthesis of vicinal diamines by the treatment of nitroepoxides with primary amines and then a reducing agent. When using a chiral primary amine, racemic nitroepoxides are transformed ...
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Elucidating the Dual Mode of Action of Dipeptidyl Enoates in the Inhibition of Rhodesain Cysteine Proteases
Wiley (2021-04-14)A computational study of the two possible inhibition mechanisms of rhodesain cysteine protease by the dipeptidyl enoate Cbz-Phe-Leu-CH=CH−CO2C2H5 has been carried out by means of molecular dynamics simulations with hybrid ...
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Fast methodology for the reliable determination of nonylphenol in water samples by minimal labeling isotope dilution mass spectrometry
Elsevier (2013-08)In this work we have developed and validated an accurate and fast methodology for the determination of 4-nonylphenol (technical mixture) in complex matrix water samples by UHPLC–ESI-MS/MS. The procedure is based on isotope ...
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Formal [3+2] Cycloaddition Reactions of Electron-Rich Aryl Epoxides with Alkenes under Lewis Acid Catalysis Affording Tetrasubstituted Tetrahydrofurans
MDPI (2020)We report on the regio- and stereoselective synthesis of tetrahydrofurans by reaction between epoxides and alkenes in the presence of a Lewis acid. This is an unprecedented formal [3+2] cycloaddition reaction between an ...
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Highly stereoselective epoxidation of O-protected 3-hydroxy-1-nitroalkenes
Elsevier (2009)[No abstract available]
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Impact of the Recognition Part of Dipeptidyl Nitroalkene Compounds on the Inhibition Mechanism of Cysteine Proteases Cruzain and Cathepsin L
American Chemical Society (2023-05-05)Cysteine proteases (CPs) are an important class of enzymes, many of which are responsible for several human diseases. For instance, cruzain of protozoan parasite Trypanosoma cruzi is responsible for the Chagas disease, ...
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Impact of the Warhead of Dipeptidyl Keto Michael Acceptors on the Inhibition Mechanism of Cysteine Protease Cathepsin L
American Chemical Society (2023-10-03)Cathepsin L (CatL) is a lysosomal cysteine protease whose activity has been related to several human pathologies. However, although preclinical trials using CatL inhibitors were promising, clinical trials have been ...
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Influence of the gas atmosphere on the deprotection of (Z)-γ -hydroxy- α , β-unsaturated esters
Bentham Science Publishers (2009)The deprotection of O-protected (Z)-α-methyl-γ-hydroxy-α,β-unsaturated ester 1 furnishes dimer 2 when the reaction is performed under a nitrogen atmosphere, while compound 3 forms when the reaction is performed under an ...
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Investigation of the Compatibility between Warheads and Peptidomimetic Sequences of Protease Inhibitors—A Comprehensive Reactivity and Selectivity Study
MDPI (2023-04-13): Covalent peptidomimetic protease inhibitors have gained a lot of attention in drug development in recent years. They are designed to covalently bind the catalytically active amino acids through electrophilic groups ...
