Listar por autoría "cf8db822-b266-4675-a7e5-43c6ba097f43"
Mostrando ítems 1-20 de 20
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Advances in the Development of SARS-CoV-2 Mpro Inhibitors
Agost Beltrán, Laura; de la hoz rodriguez, Sergio; Bou Iserte, Lledó; Rodríguez, Santiago; Fernández de la Pradilla Ibáñez, Adrián; González, Florenci 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
Latorre, Antonio; Rodríguez, Santiago; Izquierdo Ferrer, Javier; González, Florenci 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
Royo, Santiago; Schirmeister, Tanja; Kaiser, Marcel; Jung, Sascha; Rodríguez, Santiago; Bautista, José Manuel; González, Florenci 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 ... -
Catalytic enantioselective epoxidation of nitroalkenes
Vidal-Albalat, Andreu; Świderek, Katarzyna; Izquierdo Ferrer, Javier; Rodríguez, Santiago; Moliner, Vicent; González, Florenci 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 ... -
Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action
Royo Calvo, Santiago; Rodríguez, Santiago; Schirmeister, Tanja; Kesselring, Jochen; Kaiser, Marcel; González, Florenci 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 ... -
Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain
Latorre, Antonio; Schirmeister, Tanja; Kesselring, Jochen; Jung, Sascha; Johé, Patrick; Hellmich, Ute A.; Heilos, Anna; Engels, Bernd; Krauth-Siegel, R. Luise; Dirdjaja, Natalie; Bou Iserte, Lledó; Rodríguez, Santiago; González, Florenci 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 ... -
Dynamic Kinetic Asymmetric Ring-Opening/Reductive Amination Sequence of Racemic Nitroepoxides with Chiral Amines: Enantioselective Synthesis of Chiral Vicinal Diamines
Agut Gregori, Juan; Vidal-Albalat, Andreu; Rodríguez, Santiago; González, Florenci 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 ... -
Formal [3+2] Cycloaddition Reactions of Electron-Rich Aryl Epoxides with Alkenes under Lewis Acid Catalysis Affording Tetrasubstituted Tetrahydrofurans
Macías-Villamizar, Víctor; Cuca-Suárez, Luís; Rodríguez, Santiago; González, Florenci 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 ... -
Highly stereoselective epoxidation of O-protected 3-hydroxy-1-nitroalkenes
Jain, Amit; Rodríguez, Santiago; López Martín, Irakusne; González, Florenci Elsevier (2009)[No abstract available] -
Influence of the gas atmosphere on the deprotection of (Z)-γ -hydroxy- α , β-unsaturated esters
López Martín, Irakusne; Rodríguez, Santiago; Izquierdo Ferrer, Javier; González, Florenci; Vicent Barrera, Cristian 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 ... -
Investigation of the Compatibility between Warheads and Peptidomimetic Sequences of Protease Inhibitors—A Comprehensive Reactivity and Selectivity Study
Müller, Patrick; Meta, Mergim; Meidner, Jan Laurenz; Schwickert, Marvin; Meyr, Jessica; Schwickert, Dr. Kevin; Kersten, Christian; Zimmer, Collin; Hammerschmidt, Stefan Josef; Frey, Ariane; Lahu, Albin; de la hoz rodriguez, Sergio; Agost Beltrán, Laura; Rodríguez, Santiago; Diemer, Kira; Neumann, Wilhelm; González, Florenci; Engels, Bernd; Schirmeister, Tanja 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 ... -
Lignoids Isolated from Nectandra turbacensis (Kunth) Nees (Lauraceae)
Macías-Villamizar, Víctor; Cuca-Suárez, Luís; González, Florenci; Rodríguez, Santiago Academy of Chemistry of Globe Publications (2016)A new 7,8-secolignan, as well as seven known compounds; were isolated from Nectandra turbacensis (Kunth) Nees (Lauraceae) (leaves and root bark). These compounds were identified as, one secolignan, turbacenlignan A (1); ... -
Nitroepoxides as versatile precursors to 1,4-diamino heterocycles
Vidal-Albalat, Andreu; Rodríguez, Santiago; González, Florenci American Chemical Society (2014)Nitroepoxides are easily transformed into 1,4- diamino heterocycles such as quinoxalines and pyrazines by treatment with 1,2-benzenediamines and ammonia, respectively. Additionally, related saturated heterocycles, such ... -
Radical Mechanism in the Elimination of 2-Arylsulfinyl Esters
Latorre, Antonio; López Martín, Irakusne; Ramírez, Victoria; Rodríguez, Santiago; Izquierdo Ferrer, Javier; González, Florenci; Vicent Barrera, Cristian American Chemical Society (2012-05)The mechanism of the dehydrosulfenylation of 2-arylsulfinyl esters was investigated. The reaction was found to follow a homolytic cleavage mechanism as verified by electrospray ionization tandem mass spectrometry and ... -
Regioselective ring opening and isomerization reactions of 3,4-epoxyesters catalyzed by boron trifluoride
Rodríguez, Santiago; González, Florenci; Izquierdo Ferrer, Javier American Chemical Society (2011)Efficient ring opening of 3,4-epoxyesters with alcohols to produce 4-alkoxy-3-hydroxyesters and their isomerization into 4-ketoesters using boron trifluoride as the catalyst are presented. Both transformations are simple ... -
Stereoisomerization of α-hydroxy-β-sulfenyl-α,β-dimethyl naphthoquinones controlled by nonbonded sulfur–oxygen interactions
Latorre, Antonio; Rodríguez, Santiago; Jain, Amit; González, Florenci; Mata Martínez, Jose A Elsevier (2013-03)The anti α-hydroxy-β-sulfenyl-α,β-dimethyl naphthoquinones isomerize in basic media into syn/anti mixtures of isomers, giving the syn isomer as the major product. Conversely, anti α-hydroxy-β-alkoxy-α,β-dimethyl naphthoquinones ... -
Stereoisomerization of β-Hydroxy-α-sulfenyl-γ-butyrolactones Controlled by Two Concomitant 1,4-Type Nonbonded Sulfur−Oxygen Interactions As Analyzed by X-ray Crystallography
González, Florenci; Jain, Amit; Rodríguez, Santiago; Sáez, José A.; Vicent Barrera, Cristian; Peris, Gabriel American Chemical Society (2010)We have synthesized nine β-hydroxy-α-sulfenyl-γ-butyrolactones having different substituents. The syn-anti or syn-syn lactones (or any mixture of both) invariably isomerized into syn-anti/syn-syn lactones in a ratio of ... -
Study of the Stereoselectivity of the Nucleophilic Epoxidation of 3-Hydroxy-2- methylene Esters
Latorre, Antonio; Sáez Cases, José Antonio; Rodríguez, Santiago; González, Florenci Elsevier (2013-01)The diastereoselectivity of the nucleophilic epoxidation of 3-hydroxy-2-methylene esters has been studied. The 3-hydroxy-2-methylene esters were obtained through a Morita–Baylis–Hillman reaction. The resulting epoxyesters ... -
Synthetic studies on the preparation of alanyl epoxysulfones as cathepsin cysteine protease electrophilic traps
Latorre, Antonio; Rodríguez, Santiago; González, Florenci; Florea, Bogdan I.; Overkleeft, Herman S. American Chemical Society (2015-07)A Darzens reaction between tert-butoxycarbonyl alaninal and chloromethyl phenyl sulfone afforded chlorohydrins, which were converted into epoxysulfones by reaction with sodium tert-butoxide. Epoxysulfone 10 and chloroketone ... -
Three-Step Telescoped Synthesis of Monosubstituted Vicinal Diamines from Aldehydes
Bou Iserte, Lledó; Latorre, Antonio; Rodríguez, Santiago; González, Florenci (2019)Aldehydes are easily transformed into vicinal diamines and piperazines through a one-pot procedure including a Darzens reaction and treatment with an amine or diamine and then with a reducing agent. Additionally, quinoxalines ...