Search results for: Ivone Carvalho

Items from 1 to 20 out of 29 results

article

Synthesis and evaluation of an ¹⁸F‐labeled trifluoroborate derivative of 2‐nitroimidazole for imaging tumor hypoxia with positron emission tomography

Paulo Sérgio Gonçalves Nunes, Zhengxing Zhang, Hsiou‐Ting Kuo, Chengcheng Zhang, more

Journal of Labelled Compounds and Radiopharmaceuticals > 61 > 4 > 370 - 379

2‐Nitroimidazole‐based hypoxia imaging tracers such as ¹⁸F‐FMISO are normally imaged at late time points (several hours post‐injection) due to their slow clearance from background tissues. Here, we investigated if a hydrophilic zwitterion‐based ammoniomethyl‐trifluoroborate derivative of 2‐nitroimidazole, ¹⁸F‐AmBF₃‐Bu‐2NI, could have the potential to image tumor hypoxia at earlier time points. AmBF...

article

Synthesis and 2D-QSAR studies of neolignan-based diaryl-tetrahydrofuran and -furan analogues with remarkable activity against Trypanosoma cruzi and assessment of the trypanothione reductase activity

Ana Paula Hartmann, Marcelo Rodrigues de Carvalho, Lilian Sibelle Campos Bernardes, Milena Hoehr de Moraes, more

European Journal of Medicinal Chemistry > 2017 > 140 > C > 187-199

Two series of diaryl-tetrahydrofuran and -furan were synthesised and screened for anti-trypanosomal activity against trypomastigote and amastigote forms of Trypanosoma cruzi, the causative agent of Chagas disease. Based on evidence that modification of a natural product may result in a more effective drug than the natural product itself, and using known neolignan inhibitors veraguensin 1 and grandisin...

article

Binding of triazole-linked galactosyl arylsulfonamides to galectin-3 affects Trypanosoma cruzi cell invasion

Marcelo Fiori Marchiori, Thalita B. Riul, Leandro Oliveira Bortot, Peterson Andrade, more

Bioorganic & Medicinal Chemistry > 2017 > 25 > 21 > 6049-6059

The synthesis of the O-3 triazole-linked galactosyl arylsulfonamides 1–7 as potential inhibitors of Trypanosoma cruzi cell invasion is described. These target compounds were synthesized by Cu(I)-catalysed azide-alkyne cycloaddition reaction (‘click chemistry’) between different azide arylsulfonamides and the alkyne-based sugar 3-O-propynyl-βGalOMe. Inhibition assays of T. cruzi cell invasion with...

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From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease

Talita P.C. Chierrito, Susimaire Pedersoli-Mantoani, Carlos Roca, Carlos Requena, more

European Journal of Medicinal Chemistry > 2017 > 139 > C > 773-791

The lack of an effective treatment for Alzheimer’ disease (AD), an increasing prevalence and severe neurodegenerative pathology boost medicinal chemists to look for new drugs. Currently, only acethylcholinesterase (AChE) inhibitors and glutamate antagonist have been approved to the palliative treatment of AD. Although they have a short-term symptomatic benefits, their clinical use have revealed important...

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CuAAC click chemistry with N-propargyl 1,5-dideoxy-1,5-imino-D-gulitol and N-propargyl 1,6-dideoxy-1,6-imino-D-mannitol provides access to triazole-linked piperidine and azepane pseudo-disaccharide iminosugars displaying glycosidase inhibitory properties

Luís Otávio B. Zamoner, Valquíria Aragão-Leoneti, Susimaire P. Mantoani, Michael D. Rugen, more

Carbohydrate Research > 2016 > 429 > C > 29-37

Protecting group-free synthesis of 1,2:5,6-di-anhydro-D-mannitol, followed by ring opening with propargylamine and subsequent ring closure produced a separable mix of piperidine N-propargyl 1,5-dideoxy-1,5-imino-D-gulitol and azepane N-propargyl 1,6-dideoxy-1,6-imino-D-mannitol. In O-acetylated form, these two building blocks were subjected to CuAAC click chemistry with a panel of three differently...

article

Neamine and 2‐deoxystreptamine neomycin derivatives exhibit antinociceptive activity in rat models of phasic, incision and neuropathic pain

Wiliam A. Prado, Ana C. Rossaneis, Ivone Carvalho, Luis Otávio B. Zamoner, more

Journal of Pharmacy and Pharmacology > 67 > 12 > 1696 - 1704

ObjectivesTo assess the antinociceptive activity of the neomycin derivatives neamine and 2‐deoxystreptamine following intraspinal administration in rats. MethodsWe used the tail‐flick test and measured the threshold to mechanical stimulation in models of incisional and neuropathic pain. Key findingsThe derivatives produced antinociception in the tail‐flick test and reduced mechanical allodynia in...

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1,2,3-Triazole-based analogue of benznidazole displays remarkable activity against Trypanosoma cruzi

Peterson de Andrade, Oswaldo A. Galo, Marcelo R. Carvalho, Carla D. Lopes, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 21 > 6815-6826

The current treatment of Chagas disease is based on the use of two drugs, nifurtimox and benznidazole, which present limited efficacy in the chronic stage of the disease and toxic side effects. Although some progress has been made in the development of new drugs to treat this disease, the discovery of novel compounds is urgently required. In this work we report the synthesis and biological evaluation...

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Click chemistry oligomerisation of azido-alkyne-functionalised galactose accesses triazole-linked linear oligomers and macrocycles that inhibit Trypanosoma cruzi macrophage invasion

Vanessa L. Campo, Irina M. Ivanova, Ivone Carvalho, Carla D. Lopes, more

Tetrahedron > 2015 > 71 > 39 > 7344-7353

Reaction of 2-(2-(2-azidoethoxy)ethoxy)ethyl 6-O-(prop-2-ynyl)-β-d-galactopyranoside (7) under CuAAC conditions gives rise to mixed cyclic and linear triazole-linked oligomers, with individual compounds up to d.p. 5 isolable, along with mixed larger oligomers. The linear compounds resolve en bloc from the cyclic materials by RP HPLC, but are separable by gel permeation chromatography. The triazole-linked...

article

Synthetic 1,2,3-triazole-linked glycoconjugates bind with high affinity to human galectin-3

Marcelo Fiori Marchiori, Dênio Emanuel Pires Souto, Leandro Oliveira Bortot, João Francisco Pereira, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 13 > 3414-3425

This work describes the synthesis of the 1,2,3-triazole amino acid-derived-3-O-galactosides 1–6 and the 1,2,3-triazole di-lactose-derived glycoconjugate 7 as potential galectin-3 inhibitors. The target compounds were synthesized by Cu(I)-catalyzed azide–alkyne cycloaddition reaction (‘click chemistry’) between the azido-derived amino acids N₃-ThrOBn, N₃-PheOBn, N₃-N-Boc-TrpOBn, N₃-N-Boc-LysOBn, N₃...

article

Design, synthesis and enzymatic evaluation of 3-O-substituted aryl β-d-galactopyranosides as inhibitors of Trypanosoma cruzi trans-sialidase

Bruno L. Silva, José D. S. Filho, Peterson Andrade, Ivone Carvalho, more

Bioorganic & Medicinal Chemistry Letters > 2014 > 24 > 18 > 4529-4532

The trans-sialidase of Trypanosoma cruzi (TcTS) is a surface enzyme that modifies the parasite glycocalyx covering it with sialic acid. This process is essential to adhesion and invasion mechanisms in life cycle of the protozoan in the human host, making TcTS a very attractive molecular target for drug design. Using the TcTS substrate 3′-sialyllactose as prototype, d-galactose-derived potential inhibitors...

article

Synthesis of neamine-based pseudodisaccharides as potential vestibulotoxic agents to treat vertigo in Ménière’s disease

Flávio Roberto Pinsetta, Daniel Fábio Kawano, Marcelo Rodrigues de Carvalho, José Antônio A. de Oliveira, more

Carbohydrate Research > 2013 > 373 > Complete > 97-102

Ménière’s disease (MD) is a progressive disease of the inner ear characterized by recurring attacks of disabling vertigo, hearing loss and tinnitus. Patients who do not respond to vestibular sedatives or steroids may require an intratympanic application of aminoglycoside antibiotics, which destroys the vestibular function of the affected ear in order to avoid the debilitating vertigo attacks. Although...

article

α-Selective glycosylation affords mucin-related GalNAc amino acids and diketopiperazines active on Trypanosoma cruzi

Maristela B. Martins-Teixeira, Vanessa L. Campo, Monica Biondo, Renata Sesti-Costa, more

Bioorganic & Medicinal Chemistry > 2013 > 21 > 7 > 1978-1987

This work addresses the synthesis and biological evaluation of glycosyl diketopiperazines (DKPs) cyclo[Asp-(αGalNAc)Ser] 3 and cyclo[Asp-(αGalNAc)Thr] 4 for the development of novel anti-trypanosomal agents and Trypanosoma cruzi trans-sialidase (TcTS) inhibitors. The target compounds were synthetized by coupling reactions between glycosyl amino acids αGalNAc-Ser 7 or αGalNAc-Thr 8 and the amino acid...

article

Simple and efficient synthesis of 2,5-anhydro-d-glucitol

Valquiria Aragão-Leoneti, Ivone Carvalho

Tetrahedron Letters > 2013 > 54 > 9 > 1087-1089

The synthesis of 2,5-anhydro-d-glucitol is described via intramolecular cyclization of diepoxide using ammonium formate in MeOH by a microwave-assisted reaction. The overall yield was 32% from d-mannitol derivative involving seven steps.

article

Design, synthesis and the effect of 1,2,3-triazole sialylmimetic neoglycoconjugates on Trypanosoma cruzi and its cell surface trans-sialidase

Vanessa L. Campo, Renata Sesti-Costa, Zumira A. Carneiro, João S. Silva, more

Bioorganic & Medicinal Chemistry > 2012 > 20 > 1 > 145-156

This work describes the synthesis of a series of sialylmimetic neoglycoconjugates represented by 1,4-disubstituted 1,2,3-triazole-sialic acid derivatives containing galactose modified at either C-1 or C-6 positions, glucose or gulose at C-3 position, and by the amino acid derivative 1,2,3-triazole fused threonine-3-O-galactose as potential TcTS inhibitors and anti-trypanosomal agents. This series...

article

Glycoclusters presenting lactose on calix[4]arene cores display trypanocidal activity

Eva Galante, Corrada Geraci, Sebastiano Sciuto, Vanessa L. Campo, more

Tetrahedron > 2011 > 67 > 33 > 5902-5912

A new series of water-soluble tetravalent glycoclusters incorporating β-lactosyl residues attached to a central calix[4]arene core was synthesised using azide–alkyne Cu(I)-catalysed cycloaddition (‘click chemistry’). Carbohydrate moieties were attached either to the upper or lower rim of rigid cone-shaped or partial cone macrocycles via 14–21 atom spacer arms. The glycoclusters with a C ₄ ...

article

Application of copper(I)-catalysed azide/alkyne cycloaddition (CuAAC) ‘click chemistry’ in carbohydrate drug and neoglycopolymer synthesis

Valquiria Aragão-Leoneti, Vanessa L. Campo, Adriane S. Gomes, Robert A. Field, more

Tetrahedron > 2010 > 66 > 49 > 9475-9492

An overview of the potential application of copper(I)-catalysed azide/alkyne cycloaddition (CuAAC) ‘click chemistry’ in the synthesis of bioactive carbohydrates and neoglycopolymers is described.

article

‘Click chemistry’ synthesis of a library of 1,2,3-triazole-substituted galactose derivatives and their evaluation against Trypanosoma cruzi and its cell surface trans-sialidase

Ivone Carvalho, Peterson Andrade, Vanessa L. Campo, Paulo M.M. Guedes, more

Bioorganic & Medicinal Chemistry > 2010 > 18 > 7 > 2412-2427

Trypanosoma cruzi trans-sialidase (TcTS) plays a key role in the recognition and invasion of host cells and in enabling the parasite to escape the human immune response. To explore this potential drug target, we have synthesized a small library of substrate analogues based on 1,4-disubstituted 1,2,3-triazole derivatives of galactose modified at either the C-1 or C-6 positions. This was achieved by...

article

Novel and facile solution-phase synthesis of 2,5-diketopiperazines and O-glycosylated analogs

Vanessa L. Campo, Maristela B. Martins, Carlos H.T.P. da Silva, Ivone Carvalho

Tetrahedron > 2009 > 65 > 27 > 5343-5349

This work describes the synthesis in solution of a series of related diketopiperazines with potential biological activities: cyclo(l-Pro-l-Ser), cyclo(l-Phe-l-Ser), cyclo(d-Phe-l-Ser) and the corresponding glycosylated analogs of the latter, cyclo[d-Phe-l-Ser(αGlcNAc)] and cyclo[d-Phe-l-Ser(βGlcNAc)]. The synthetic approach involved coupling reactions of –OH or O-glycosylated serine benzyl esters...

article

Carrageenans: Biological properties, chemical modifications and structural analysis – A review

Vanessa Leiria Campo, Daniel Fábio Kawano, Dílson Braz da Silva, Ivone Carvalho

Carbohydrate Polymers > 2009 > 77 > 2 > 167-180

Carrageenans are sulphated linear polysaccharides of d-galactose and 3,6-anhydro-d-galactose extracted from certain red seaweeds of the Rhodophyceae class. They have been extensively used in the food industry as thickening, gelling and protein-suspending agents, and more recently by the pharmaceutical industry as excipient in pills and tablets. Besides the well-known biological activities related...

article

Molecular Dynamics, Density Functional, ADMET Predictions, Virtual Screening, and Molecular Interaction Field Studies for Identification and Evaluation of Novel Potential CDK2 Inhibitors In Cancer Therapy ^†

Vinicius Barreto da Silva, Daniel Fábio Kawano, Adriane da Silveira Gomes, Ivone Carvalho, more

The Journal of Physical Chemistry A > 2008 > 112 > 38 > 8902 - 8910

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Search results for: Ivone Carvalho

Synthesis and evaluation of an ¹⁸F‐labeled trifluoroborate derivative of 2‐nitroimidazole for imaging tumor hypoxia with positron emission tomography

Synthesis and 2D-QSAR studies of neolignan-based diaryl-tetrahydrofuran and -furan analogues with remarkable activity against Trypanosoma cruzi and assessment of the trypanothione reductase activity

Binding of triazole-linked galactosyl arylsulfonamides to galectin-3 affects Trypanosoma cruzi cell invasion

From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease

CuAAC click chemistry with N-propargyl 1,5-dideoxy-1,5-imino-D-gulitol and N-propargyl 1,6-dideoxy-1,6-imino-D-mannitol provides access to triazole-linked piperidine and azepane pseudo-disaccharide iminosugars displaying glycosidase inhibitory properties

Neamine and 2‐deoxystreptamine neomycin derivatives exhibit antinociceptive activity in rat models of phasic, incision and neuropathic pain

1,2,3-Triazole-based analogue of benznidazole displays remarkable activity against Trypanosoma cruzi

Click chemistry oligomerisation of azido-alkyne-functionalised galactose accesses triazole-linked linear oligomers and macrocycles that inhibit Trypanosoma cruzi macrophage invasion

Synthetic 1,2,3-triazole-linked glycoconjugates bind with high affinity to human galectin-3

Design, synthesis and enzymatic evaluation of 3-O-substituted aryl β-d-galactopyranosides as inhibitors of Trypanosoma cruzi trans-sialidase

Synthesis of neamine-based pseudodisaccharides as potential vestibulotoxic agents to treat vertigo in Ménière’s disease

α-Selective glycosylation affords mucin-related GalNAc amino acids and diketopiperazines active on Trypanosoma cruzi

Simple and efficient synthesis of 2,5-anhydro-d-glucitol

Design, synthesis and the effect of 1,2,3-triazole sialylmimetic neoglycoconjugates on Trypanosoma cruzi and its cell surface trans-sialidase

Glycoclusters presenting lactose on calix[4]arene cores display trypanocidal activity

Application of copper(I)-catalysed azide/alkyne cycloaddition (CuAAC) ‘click chemistry’ in carbohydrate drug and neoglycopolymer synthesis

‘Click chemistry’ synthesis of a library of 1,2,3-triazole-substituted galactose derivatives and their evaluation against Trypanosoma cruzi and its cell surface trans-sialidase

Novel and facile solution-phase synthesis of 2,5-diketopiperazines and O-glycosylated analogs

Carrageenans: Biological properties, chemical modifications and structural analysis – A review

Molecular Dynamics, Density Functional, ADMET Predictions, Virtual Screening, and Molecular Interaction Field Studies for Identification and Evaluation of Novel Potential CDK2 Inhibitors In Cancer Therapy ^†

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