A5051794350- Synthetic Organic Chemistry Methods
- Traditional and Medicinal Uses of Annonaceae
- Bioactive Compounds and Antitumor Agents
- COVID-19 Clinical Research Studies
- SARS-CoV-2 and COVID-19 Research
- Carbohydrate Chemistry and Synthesis
- Herbal Medicine Research Studies
- Transgenic Plants and Applications
- Synthesis and Biological Evaluation
- Cocoa and Sweet Potato Agronomy
- Marine Sponges and Natural Products
- Mosquito-borne diseases and control
- Hormonal Regulation and Hypertension
- Trypanosoma species research and implications
- X-ray Diffraction in Crystallography
- thermodynamics and calorimetric analyses
- Dermatology and Skin Diseases
- Ocular Surface and Contact Lens
- Synthesis of Organic Compounds
- Influenza Virus Research Studies
- Genetics, Bioinformatics, and Biomedical Research
- Enzyme Structure and Function
- Advancements in Transdermal Drug Delivery
- Multicomponent Synthesis of Heterocycles
- Protein Structure and Dynamics
Brazilian Biosciences National Laboratory
2019-2023
Brazilian Center for Research in Energy and Materials
2019-2023
Laboratório Nacional de Ciência e Tecnologia do Bioetanol
2021-2022
University of Nottingham
2008-2020
University of Birmingham
2020
National Centre for Research
2020
Universidade Estadual de Campinas (UNICAMP)
2013
An improved synthesis of the oxepinochromone ptaeroxylin is reported, together with syntheses related natural products ptaeroxylinol and eranthin. Ptaeroxylin were obtained from chromenone noreugenin by selective reaction 7-hydroxyl group, allylation 5-hydroxyl, followed Claisen rearrangement under microwave conditions concomitant deprotection 7-hydroxyl. Alkylation appropriate allyl bromide provides a precursor for ring-closing metathesis to deliver ring system. Eranthin was similar...
Abstract The nucleocapsid (N) protein plays critical roles in coronavirus genome transcription and packaging, representing a key target for the development of novel antivirals, which structural information on ligand binding is scarce. We used fluorescence polarization assay to identify small molecules that disrupt N RNA derived from SARS-CoV-2 packaging signal. Several phenolic compounds, including L-chicoric acid (CA), were identified as high-affinity N-protein ligands. CA was confirmed by...
The present work describes the preparation of a novel series compounds based on structure goniothalamin (1), natural styryl lactone with known cytotoxic and antiproliferative activities against variety cancer cell lines. A focused library 17 analogues displaying 5-methyl-2,5-dihydrofuran-2-one motif were prepared, their cytotoxicity evaluated. While bearing methoxy and/or hydroxy groups aromatic moiety usually at least three times less potent than lead compound ortho para-trifluoromethyl 10...
Until December 2021, the COVID-19 pandemic has caused more than 5.5 million deaths. Vaccines are being deployed worldwide to mitigate severe disease and death, but continued transmission emergence of SARS-CoV-2 variants indicate that specific treatments against still necessary. We screened 400 compounds from Medicines for Malaria Venture (MMV) Pathogen Box seeking molecules with antiviral activity by using a high-throughput screening (HTS) infection assay in Vero CCL81 cells. On resupply 15...
A synthesis of the unusual ansa-bridged farnesyl hydroquinone derivative likonide B in racemic form is described. The natural product, also known as smenochromene D, was obtained from geranylacetone by a route which key steps are regioselective microwave-mediated Claisen rearrangement an aryl propargyl ether to deliver chromene ring, and macrocyclization via intramolecular Mitsunobu reaction. Subsequent HPLC on chiral stationary phase gave pure (+)- (-)-enantiomers, that were studied CD...
Chagas disease is a parasitic infection affecting millions of people across Latin America, imposing dramatic socioeconomic burden. Despite the availability drugs, nifurtimox and benznidazole, lack efficacy incidence side-effects prompt identification novel, efficient, affordable drug candidates. To address this issue, one strategy could be probing susceptibility Trypanosoma parasites toward NADP-dependent enzyme inhibitors. Recently, steroids androstane group have been described as highly...
A synthesis of the unusual ansa farnesyl hydroquinone smenochromene D (likonide B) is described, in which key steps are a regioselective microwave-mediated Claisen rearrangement an aryl propargyl ether to deliver chromene ring, and macrocyclisation via intramolecular Mitsunobu reaction.
For disorders of the skin, eyes, ears, and respiratory tract, topical drugs, delivered directly to target organ, are a therapeutic option. Compared with systemic oral therapy, benefits treatments include faster onset action, circumventing liver first pass drug metabolism, reducing side effects. Nevertheless, some absorption still occurs for many agents resulting in One way prevent these would be develop drugs that instantly degraded upon entry into bloodstream by serum esterases. Because...
A descoberta de fármacos a partir produtos naturais vivencia uma nova era graças ao uso tecnologias ponta e abordagens integradas para superar as dificuldades inerentes à pesquisa com naturais. Estes são substâncias químicas altamente complexas inovadoras produzidas pela biota, em especial organismos sésseis como plantas micro-organismos, representam principal fonte inspiração novos fármacos. Resultante do reavivado interesse na medicamentos base naturais, novas identificação,...
The ongoing COVID-19 pandemic caused a significant loss of human lives and worldwide decline in quality life. Treatment patients is challenging, specific treatments to reduce aggravation mortality are still necessary. Here, we describe the discovery novel class epiandrosterone steroidal compounds with cationic amphiphilic properties that present antiviral activity against SARS-CoV-2 low micromolar range. Compounds were identified screening campaigns using cytopathic effect-based assay Vero...
A short 3-step synthesis of the antiviral agent 7DMA is described herein. The nature a major by-product formed during key N-glycosylation 6-chloro-7-deaza-7-iodopurine with perbenzoylated 2-methyl-ribose under Vorbrüggen conditions was also investigated. Spectroscopic analyses support that solvent itself converted into nucleophilic species competing nucleobase and further reacting activated riboside in an unanticipated fashion. These findings call for revision reaction when working weakly...
Abstract The nucleocapsid (N) protein plays critical roles in coronavirus genome transcription and packaging, representing a key target for the development of novel antivirals, which structural information on ligand binding is scarce. We used fluorescence polarization assay to identify small molecules that disrupt N RNA derived from SARS-CoV-2 packaging signal. Several phenolic compounds, including L-chicoric acid (CA), were identified as high-affinity N-protein ligands. CA was confirmed by...
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Chagas disease, an infectious condition caused by Trypanosoma cruzi, lacks treatment with drugs desired efficacy and safety profiles. To address this unmet medical need, a set of trypanocidal compounds were identified through large multicenter phenotypic-screening initiative assembled in the GSK Box. In present work, we report screening Box against T. cruzi malic enzymes (MEs) identification three potent inhibitors its cytosolic isoform (TcMEc). One these compounds, TCMDC-143108 (1), came...
In view of preparing furanone analogs – exemplified by compound 1- the cytotoxic naturally occurring styryl lactone goniothalamin (2), we envisioned a key cross-coupling metathesis reaction between vinyl 3 and range styrenes. Inspired work Piva et al, where would be formed in situ via ring-closing triene 4, herein report short synthesis variety furanones using tandem ringclosing/ (RCM/CCM) step.