Search Results - "Guillermo Labadié"
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1
1,2,3-Triazoles in Biomolecular Crystallography: A Geometrical Data-Mining Approach
Published in Journal of medicinal chemistry (09-11-2023)“…The 1,2,3-triazole scaffold has become very attractive to identify new chemical entities in drug discovery projects. Despite the widespread use of click…”
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2
Editorial: Combatting tropical diseases: a multi-level approach
Published in Frontiers in cellular and infection microbiology (2024)Get full text
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3
Understanding the Fate of the Banert Cascade of Propargylic Azides: Sigmatropic versus Prototropic Pathway
Published in Journal of organic chemistry (21-07-2023)“…The Banert cascade is an efficient synthetic strategy for obtaining 4,5-disubstituted 1,2,3-triazoles. The reaction can proceed via a sigmatropic or…”
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4
Identification of a Bifunctional Maize C- and O-Glucosyltransferase
Published in The Journal of biological chemistry (01-11-2013)“…Flavonoids accumulate in plant vacuoles usually as O-glycosylated derivatives, but several species can also synthesize flavonoid C-glycosides. Recently, we…”
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5
Insight into the factors controlling the equilibrium of allylic azides
Published in RSC advances (27-01-2020)“…Several allylic azides with different double bond substitutions were studied to understand the factors, governing their equilibrium using density functional…”
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6
New one-pot synthesis of anti-tuberculosis compounds inspired on isoniazid
Published in European journal of medicinal chemistry (15-12-2020)“…A library of thirty N-substituted tosyl N’-acryl-hydrazones was prepared with p-toluenesulfonyl hydrazide, methyl propiolate and different aldehydes in a…”
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7
Identification of Novel Chemical Scaffolds Inhibiting Trypanothione Synthetase from Pathogenic Trypanosomatids
Published in PLoS neglected tropical diseases (12-04-2016)“…The search for novel chemical entities targeting essential and parasite-specific pathways is considered a priority for neglected diseases such as…”
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8
Systematic study of 1,2,3-triazolyl sterols for the development of new drugs against parasitic Neglected Tropical Diseases
Published in European journal of medicinal chemistry (05-06-2023)“…A series of thirty 1,2,3-triazolylsterols, inspired by azasterols with proven antiparasitic activity, were prepared by a stereocontrolled synthesis. Ten of…”
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9
Expanding the scope of novel 1,2,3-triazole derivatives as new antiparasitic drug candidates
Published in RSC medicinal chemistry (25-01-2023)“…We have previously shown that prenyl and aliphatic triazoles are interesting motifs to prepare new chemical entities for antiparasitic and antituberculosis…”
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10
Computational approaches for drug discovery against trypanosomatid-caused diseases
Published in Parasitology (01-05-2020)“…During three decades, only about 20 new drugs have been developed for malaria, tuberculosis and all neglected tropical diseases (NTDs). This critical situation…”
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11
Lipophilic modification of salirasib modulates the antiproliferative and antimigratory activity
Published in Bioorganic & medicinal chemistry (07-09-2023)“…[Display omitted] Salirasib, or farnesylthiosalicylic acid (FTS), is a salicylic acid derivative with demonstrated antineoplastic activity. While designed as a…”
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12
Biochemical characterization of the minimal domains of an iterative eukaryotic polyketide synthase
Published in The FEBS journal (01-12-2018)“…Iterative type I polyketide synthases (PKS) are megaenzymes essential to the biosynthesis of an enormously diverse array of bioactive natural products. Each…”
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13
Antifungal activity and cytotoxicity of extracts and triterpenoid saponins obtained from the aerial parts of Anagallis arvensis L
Published in Journal of ethnopharmacology (05-05-2017)“…Anagallis arvensis L. (Primulaceae) is used in argentinean northwestern traditional medicine to treat fungal infections. We are reporting the isolation and…”
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14
Expanding the scope of synthetic 1,2,4-trioxanes towards Trypanosoma cruzi and Leishmania donovani
Published in Bioorganic & medicinal chemistry letters (15-10-2020)“…[Display omitted] A series of synthetic 1,2,4-trioxanes related to artemisinin was tested against L. donovani and T. cruzi parasites. This screening identified…”
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15
Endocannabinoids in Caenorhabditis elegans are essential for the mobilization of cholesterol from internal reserves
Published in Scientific reports (23-04-2018)“…Proper cholesterol transport is crucial for the functionality of cells. In C . elegans , certain cholesterol derivatives called dafachronic acids (DAs) govern…”
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16
Antitubercular activity of 1,2,3-triazolyl fatty acid derivatives
Published in European journal of medicinal chemistry (05-01-2017)“…A collection of 1,2,3-triazoles unsaturated fatty acid mimics were efficiently synthesized by click chemistry. The 1,4-disubstituted analogs prepared covered…”
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17
Repurposing antiparasitic N,N′‐aliphatic diamine derivatives as promising antimycobacterial agents
Published in Archiv der Pharmazie (Weinheim) (01-11-2024)“…In previous studies, we demonstrated the potent activity of a library of 25 N,N′‐disubstituted diamines (NNDDA) toward Trypanosomatid and Apicomplexa…”
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Evaluation of proline analogs as trypanocidal agents through the inhibition of a Trypanosoma cruzi proline transporter
Published in Biochimica et biophysica acta. General subjects (01-11-2017)“…Trypanosoma cruzi, the etiological agent of Chagas disease, uses proline as its main carbon source, essential for parasite growth and stage differentiation in…”
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Synthesis and interaction of terminal unsaturated chemical probes with Mycobacterium tuberculosis CYP124A1
Published in Bioorganic & medicinal chemistry (15-08-2021)“…[Display omitted] A series of C15–C20 isoprenyl derivatives bearing terminal alkenyl and alkynyl groups were synthesized as possible substrates of the…”
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Exploring the chemical space of 1,2,3-triazolyl triclosan analogs for discovery of new antileishmanial chemotherapeutic agents
Published in RSC medicinal chemistry (01-01-2021)“…Triclosan and isoniazid are known antitubercular compounds that have proven to be also active against Leishmania parasites. On these grounds, a collection of…”
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