Elisabete F. Freitas, Catarina Mendonça, Jorge A. Santos, Carla Murteira, João Pedro Ferreira,
In this paper, annoyance ratings from traffic noise recorded on cobblestones, dense asphalt, and open asphalt rubber pavements are assessed with regard to car speeds and traffic densities. It was found that cobblestones pavements are the most annoying; also while open asphalt rubber pavement imposes less annoyance than dense asphalt it is not significantly different. Higher car speeds always lead to greater annoyance, as does higher traffic densities. LAeq and LAmax correlate well with annoyance, ...
Tópico(s): Vehicle Noise and Vibration Control
2012 - Elsevier BV | Transportation Research Part D Transport and Environment
Produção Nacional
Revisado por pares
Pedro de Sena Murteira Pinheiro, Lucas Silva Franco, Tadeu L. Montagnoli, Carlos Alberto Manssour Fraga,
Introduction The current drug discovery paradigm of 'one drug, multiple targets' has gained attention from both the academic medicinal chemistry community and the pharmaceutical industry. This is in response to the urgent need for effective agents to treat multifactorial chronic diseases. The molecular hybridization strategy is a useful tool that has been widely explored, particularly in the last two decades, for the design of multi-target drugs.
Tópico(s): Cholinesterase and Neurodegenerative Diseases
2024 - Taylor & Francis | Expert Opinion on Drug Discovery
Produção Nacional
Revisado por pares
Pedro de Sena Murteira Pinheiro, Lucas Silva Franco, Carlos Alberto Manssour Fraga,
One of the key scientific aspects of small-molecule drug discovery and development is the analysis of the relationship between its chemical structure and biological activity. Understanding the effects that lead to significant changes in biological activity is of paramount importance for the rational design and optimization of bioactive molecules. The "methylation effect", or the "magic methyl" effect, is a factor that stands out due to the number of examples that demonstrate profound changes in either ...
Tópico(s): Histone Deacetylase Inhibitors Research
2023 - Multidisciplinary Digital Publishing Institute | Pharmaceuticals
Produção Nacional
Revisado por pares
Daniel A. Rodrigues, Pedro de Sena Murteira Pinheiro, Fernanda S. Sagrillo, María Laura Bolognesi, Carlos Alberto Manssour Fraga,
Abstract Despite the applicability of histone deacetylase inhibitors (HDACis) for cancer treatment, several works in the literature have shown that these inhibitors can be used in several other diseases, such as neurodegenerative diseases (NDs). This review begins by discussing the signaling pathways of HDACs, focused on the context of NDs, presenting a discussion about the pharmacophoric features of HDACis and crystal structure analysis and discussing interesting case studies from the literature ...
Tópico(s): Catalytic C–H Functionalization Methods
2020 - Wiley | Medicinal Research Reviews
Produção Nacional
Revisado por pares
Daniel A. Rodrigues, Fabiana Sélos Guerra, Fernanda S. Sagrillo, Pedro de Sena Murteira Pinheiro, Marina Amaral Alves, Sreekanth Thota, Lorrane de Souza Chaves, Carlos Maurício R. Sant’Anna, Patrícia Dias Fernandes, Carlos Alberto Manssour Fraga,
Abstract Targeting histone deacetylases (HDACs) and phosphatidylinositol 3‐kinases (PI3Ks) is a very promising approach for cancer treatment. This manuscript describes the design, synthesis, in vitro pharmacological profile, and molecular modeling of a novel class of N ‐acylhydrazone (NAH) derivatives that act as HDAC6/8 and PI3Kα dual inhibitors. The surprising selectivity for PI3Kα may be related to differences in the conformation in the active site. Cellular studies showed that these compounds act ...
Tópico(s): Peptidase Inhibition and Analysis
2020 - Wiley | ChemMedChem
Produção Nacional
Revisado por pares
Daniel A. Rodrigues, Pedro de Sena Murteira Pinheiro, Carlos Alberto Manssour Fraga,
The discovery of histone deacetylase (HDAC) inhibitors is a hot topic in the medicinal chemistry community regarding cancer research. This is related primarily to two factors: success in the clinic, e. g., the four FDA-approved HDAC inhibitors, and strong versatility to combine their pharmacophoric features to design new hybrid compounds with multitarget profiles. Thus, the selection of adequate pharmacophores to combine, i. e., combining targets that can result in a synergistic effect, is desirable, ...
Tópico(s): Click Chemistry and Applications
2020 - Wiley | ChemMedChem
Produção Nacional
Revisado por pares
Claudia Albertini, Alessandra Salerno, Pedro de Sena Murteira Pinheiro, María Laura Bolognesi,
The continued drug discovery failures in complex neurodegenerative diseases, including Alzheimer's disease (AD), has raised questions about the classical paradigm "one-drug, one-target, one-disease." In parallel, the ever-increasing awareness of the multiplicity of the underlying pathways has led to the affirmation of polypharmacological approaches. Polypharmacology, which broadly embodies the use of pharmaceutical agents acting on multiple targets, seems to be the best way to restore the complex ...
Tópico(s): Click Chemistry and Applications
2020 - Wiley | Medicinal Research Reviews
Produção Nacional
Revisado por pares
Pedro de Sena Murteira Pinheiro, Daniel A. Rodrigues, Rodolfo C. Maia, Sreekanth Thota, Carlos Alberto Manssour Fraga,
During the early preclinical phase, from hit identification and optimization to a lead compound, several medicinal chemistry strategies can be used to improve potency and/or selectivity. The conformational restriction is one of these approaches. It consists of introducing some specific structural constraints in a lead candidate to reduce the overall number of possible conformations in order to favor the adoption of a bioactive conformation and, as a consequence, molecular recognition by the target ...
Tópico(s): Histone Deacetylase Inhibitors Research
2019 - Bentham Science Publishers | Current Topics in Medicinal Chemistry
Produção Nacional
Revisado por pares
Sreekanth Thota, Daniel A. Rodrigues, Pedro de Sena Murteira Pinheiro, Lı́dia Moreira Lima, Carlos Alberto Manssour Fraga, Eliezer J. Barreiro,
Over the last two decades, N-acylhydrazone (NAH) has been proven to be a very versatile and promising motif in drug design and medicinal chemistry. Herein, we discuss the current and future challenges in the emergence of bioactive NAH-based scaffolds and to developing strategies to overcome the failures in drug discovery. The NAH-related approved drugs nitrofurazone, nitrofurantoin, carbazochrome, testosterone 17-enanthate 3-benzilic acid hydrazine, nifuroxazide, dantrolene, and azumolene are already ...
Tópico(s): Pharmacogenetics and Drug Metabolism
2018 - Elsevier BV | Bioorganic & Medicinal Chemistry Letters
Produção Nacional
Revisado por pares
Pedro de Sena Murteira Pinheiro, Daniel A. Rodrigues, Marina Amaral Alves, Luzineide W. Tinoco, Gláucio B. Ferreira, Carlos Maurício R. Sant’Anna, Carlos Alberto Manssour Fraga,
Sigma-hole (σ-hole) bonds are interactions that are gaining special attention in medicinal chemistry.
Tópico(s): Synthesis of heterocyclic compounds
2017 - Royal Society of Chemistry | New Journal of Chemistry
Produção Nacional
Revisado por pares
Rosaria Carmela Perone, Claudia Albertini, Elisa Uliassi, Flaminia Di Pietri, Pedro de Sena Murteira Pinheiro, Sabrina Petralla, Nicola Rizzardi, Romana Fato, Lenka Pulkrabkova, Ondřej Soukup, Anna Tramarin, Manuela Bartolini, María Laura Bolognesi,
Thanks to the widespread use and safety profile of donepezil (1) in the treatment of Alzheimer's disease (AD), one of the most widely adopted multi-target-directed ligand (MTDL) design strategies is to modify its molecular structure by linking a second fragment carrying an additional AD-relevant biological property. Herein, supported by a proposed combination therapy of 1 and the quinone drug idebenone, we rationally designed novel 1-based MTDLs targeting Aβ and oxidative pathways. By exploiting a ...
Tópico(s): Medicinal Plants and Neuroprotection
2020 - Wiley | ChemMedChem
Produção Nacional
Revisado por pares
Roberta Tesch, Christian F. W. Becker, Matthias Müller, Michael E. Beck, Lena Quambusch, Matthäus Getlik, Jonas Lategahn, Niklas Uhlenbrock, Fanny N. Costa, Marcelo D. Polêto, Pedro de Sena Murteira Pinheiro, Daniel A. Rodrigues, Carlos Maurício R. Sant’Anna, Fábio Furlan Ferreira, Hugo Verli, Carlos Alberto Manssour Fraga, Daniel Rauh,
Abstract PIK‐75 is a phosphoinositide‐3‐kinase (PI3K) α‐isoform‐selective inhibitor with high potency. Although published structure–activity relationship data show the importance of the NO 2 and the Br substituents in PIK‐75, none of the published studies could correctly determine the underlying reason for their importance. In this publication, we report the first X‐ray crystal structure of PIK‐75 in complex with the kinase GSK‐3β. The structure shows an unusual U‐shaped conformation of PIK‐75 within ...
Tópico(s): Organophosphorus compounds synthesis
2018 - Wiley | Angewandte Chemie International Edition
Produção Nacional
Revisado por pares
Daniel A. Rodrigues, Pedro de Sena Murteira Pinheiro, Thayssa Tavares da Silva Cunha Ferreira, Sreekanth Thota, Carlos Alberto Manssour Fraga,
G‐protein‐coupled receptor 40 ( GPR 40) was recently identified as an interesting target for treatment of type 2 diabetes. The high level of expression in pancreatic beta cells and the dependence of glucose on stimulating the secretion of insulin led to great excitement in this field. The identification of this target was followed by the development of a series of agonists with great potential for the treatment of diabetes. All known agonists have the presence of a pharmacophoric carboxylic acid group ...
Tópico(s): Diabetes Treatment and Management
2017 - Wiley | Chemical Biology & Drug Design
Produção Nacional
Revisado por pares
Harold Hilarion Fokoue, Pedro de Sena Murteira Pinheiro, Carlos Alberto Manssour Fraga, Carlos Maurício R. Sant’Anna,
MEDICINAL CHEMISTRY?.In Medicinal Chemistry, the knowledge, the study and the understanding of the intermolecular interactions inherent to the molecular recognition of a ligand by its target bioreceptor are essential.This is because understanding these interactions, which define the molecular complementarity between the two, is the key to analyze critically structure-activity relationship studies, allowing the optimization of the modulation of a target bioreceptor by a ligand.Thus, it is necessary ...
Tópico(s): Science and Education Research
2020 - Brazilian Chemical Society | Química Nova
Produção Nacional
Revisado por pares
Isadora T.S. Bastos, Pedro de Sena Murteira Pinheiro, Fanny N. Costa, Miguel Divino da Rocha, Carlos Maurício R. Sant’Anna, Delson Braz, Éverton Tenório de Souza, Marco A. Martins, Eliezer J. Barreiro, Fábio Furlan Ferreira, R.C. Barroso, Carlos Alberto Manssour Fraga,
Pulmonary arterial hypertension (PAH) is a chronic cardiovascular disease that displays inflammatory components, which contributes to the difficulty of adequate treatment with the available therapeutic arsenal. In this context, the N-acylhydrazone derivative LASSBio-1359 was previously described as a multitarget drug candidate able to revert the events associated with the progression of PAH in animal models. However, in spite of having a dual profile as PDE4 inhibitor and adenosine A2A receptor agonist, ...
Tópico(s): Nonlinear Optical Materials Research
2018 - Multidisciplinary Digital Publishing Institute | Pharmaceuticals
Produção Nacional
Marília M. Guimarães, Carla T.G. Guerra, Solange Travassos de Figueiredo Alves, Maria C.S.A. Cunha, Luiz A. Marins, Luiz Felipe Mena Barreto, Evelyn Teich, Flávia Nardes, José F.R. Ornellas, Gerson Carakushansky, Gustavo Pinheiro, Helena P. Oliveira, Isabel C.R. Beserra, Juraci Ghiaroni, Marcelo V. Peixoto, Maria Lúcia Fleiuss Farias, Mônica M.A. Lanfredi, Munira Aiex Proença, Paula P. Ramalho, Pedro de Sena Murteira Pinheiro, Roberto Zagury, Roberto Azevedo Antunes,
Neste trabalho descrevemos as malformações e co-morbidades observadas em pacientes com síndrome de Turner (ST). Foi realizado um estudo retrospectivo, avaliando os prontuários de 60 pacientes cujo diagnóstico de ST foi confirmado através do cariótipo, desde a fase pré-natal até a idade de 49 anos. As pacientes encontram-se com idades entre 1 e 50 anos e foram evoluídas num período de 4 meses a 29 anos. Trinta e uma apresentavam o cariótipo 45XO, 24 eram mosaico e 5 apresentavam o padrão 46Xi, (i,Xq). ...
Tópico(s): Genomic variations and chromosomal abnormalities
2001 - Editora da Universidade de São Paulo | Arquivos Brasileiros de Endocrinologia & Metabologia
Produção Nacional
Revisado por pares
Pedro de Sena Murteira Pinheiro,
Treatment of the Slipped Capital Femoral Epiphysis remains a cause of concern due to the fact that the true knowledge of the etiopathogeny is unknown, as well as one of its major complications: chondrolysis. The conservative treatment remains controversial; it has been overlooked in the studies and subjected to intense criticism. The purpose of this study is to investigate the results of treatment on the hip of patients displaying slipped capital femoral epiphysis, using the plaster cast immobilization ...
Tópico(s): Bone and Joint Diseases
2011 - BioMed Central | Journal of Orthopaedic Surgery and Research
Produção Nacional
Revisado por pares
Luan Pereira Diniz, Juliana Morgado, Ana Paula Bérgamo Araújo, Leticia Maria da Silva Antônio, Hannah P. Mota-Araujo, Pedro de Sena Murteira Pinheiro, Fernanda S. Sagrillo, Gabriele Vargas, Sérgio T. Ferreira, Cláudia P. Figueiredo, Carlos Alberto Manssour Fraga, Flávia Carvalho Alcântara Gomes,
Background and Purpose Inhibitors of histone deacetylases (iHDACs) are promising drugs for neurodegenerative diseases. We have evaluated the therapeutic potential of the new iHDAC LASSBio‐1911 in Aβ oligomer (AβO) toxicity models and astrocytes, key players in neuroinflammation and Alzheimer's disease (AD). Experimental Approach Astrocyte phenotype and synapse density were evaluated by flow cytometry, Western blotting, immunofluorescence and qPCR, in vitro and in mice. Cognitive function was evaluated ...
Tópico(s): Histone Deacetylase Inhibitors Research
2024 - Wiley | British Journal of Pharmacology
Produção Nacional
Revisado por pares
Pedro de Sena Murteira Pinheiro, Daniel A. Rodrigues, Carlos Maurício R. Sant’Anna, Carlos Alberto Manssour Fraga,
Abstract Semiempirical methods can be applied to calculations of much larger systems than classical ab initio or DFT methods, reaching accuracy sometimes comparable with more advanced levels of theory. These methods are important tools that can be used in research projects focused in structure‐based drug design (SBDD). Thus, a notion of the precision of each method in describing key‐interactions with target receptors is necessary. With this goal in mind, we applied several semiempirical methods (AM1, ...
Tópico(s): Nuclear Receptors and Signaling
2018 - Wiley | International Journal of Quantum Chemistry
João Pedro Aguiar, F. Borges, Rodrigo Murteira, Catarina Ramos, Emanuel Gouveia, Maria José Passos, Ana Miranda, Filipa Alves da Costa,
Tópico(s): Cancer Immunotherapy and Biomarkers
2018 - Springer Science+Business Media | International Journal of Clinical Pharmacy
Produção Nacional
Revisado por pares
Daniel A. Rodrigues, Pedro de Sena Murteira Pinheiro, Fernanda S. Sagrillo, Maria Clara Ramalho Freitas, Marina Amaral Alves, Sreekanth Thota, Luzineide W. Tinoco, Alviclér Magalhães, Carlos Maurício R. Sant’Anna, Carlos Alberto Manssour Fraga,
A serendipitous identification and characterization of a new non-classical hydrogen bond donor moiety found in N -acylhydrazones containing 3-acyl-substituted furan subunit is presented.
Tópico(s): Chemical Reaction Mechanisms
2020 - Royal Society of Chemistry | New Journal of Chemistry
Catarina Tomás, Emanuel Oliveira, Daniellen Cristina Ferreira Sousa, Matheus Uba Chupel, Guilherme Eustáquio Furtado, Clara Rocha, Ana Teixeira, Pedro Lopes Ferreira, C. Alves, Stefan Gisin, Elisabete Catarino, Nelma Carvalho, Tiago Coucelo, Luís Américo Silva Bonfim, Carina Silva, Débora Franco, Jesús Alcoba González, Maria Helena de Agrela Gonçalves Jardim, Rita Silva, Cristina Lavareda Baixinho, Ma Helena Presado, Ma Fátima Marques, Mário E. Cardoso, Marina Cunha, Joana Mendes, Ana Xavier, Ana Galhardo, Margarida Couto, João Frade, Carla Nunes, João R. Mesquita, María Säo José Nascimento, Guilherme Gonçalves, Conceição Castro, Alice Mártires, M. João Monteiro, Conceição Rainho, Francisco P. Caballero, Fátima M. Monago, José T. Guerrero, Rocio M. Monago, Africa P. Trigo, Milagros L. Gutierrez, Gemma M. Milanés, Mercedes G. Reina, Ana G. Villanueva, Ana S. Piñero, Isabel R. Aliseda, Francisco Buitrago Ramírez, Andrea Ribeiro, Ana Quelhas, Maria Conceição Manso, Francisco P. Caballero, José T. Guerrero, Fátima M. Monago, Rafael Brito Santos, Nuria R. Jimenez, Cristina G. Nuñez, Inmaculada Rodríguez Gómez, Ma Jose L. Fernandez, Laura A. Marquez, Ana L. Moreno, Ma Jesus Tena Huertas, Francisco Buitrago Ramírez, Daniel Seabra, Ma Céu Salvador, Luciene Muniz Braga, Pedro Parreira, Anabela Salgueiro‐Oliveira, Cristina Arreguy-Sena, Bibiana F. Oliveira, Ma Adriana Henriques, Joana Santos, Sara Lebre, Alda Marques, Clarinda Festas, Sandra Rodrigues, Andrea Ribeiro, José Lumini‐Oliveira, Ana Gabriela Figueiredo, Francisco J. Hernandez-Martinez, Liliana Campi, Ma Pino Quintana-Montesdeoca, Juan F. Jimenez-Diaz, Bienvenida C. Rodriguez-De-Vera, Alexandra Parente, Ma Augusta Mata, Ana Ma Pereira, Adília Fernandes, Manuel Brás, Ma Rosário Pinto, Pedro Parreira, Marta Lima Basto, Ana C. Rei, Lisete Mónico, Gilberta Sousa, Clementina Morna, Otília Freitas, Gregório Freitas, Ana Carolina Gomes Jardim, Rita P. Vasconcelos, Lina G. Horta, Roger dos Santos Rosa, Luís Fernando Kranz, Rita C. Nugem, Mariana Santiago Siqueira, Ronaldo Bordin, Rosiane Kniess, Josimari Telino de Lacerda, Joana Guedes, Idalina Machado, Sidalina Almeida, Adriano Zilhão, Hélder Alves, Óscar Ribeiro, Ana Paula Martins Amaral, Ana Maria Ribeiro dos Santos, Joana Monteiro, Ma Clara Rocha, Rui Cruz, Ana Paula Martins Amaral, Marina Lourenço, Ma Clara Rocha, Rui Cruz, Sandra Regina Masetto Antunes, Verónica Mendonça, Isabel Andrade, Nádia Osório, Ana Valado, Armando Caseiro, Antonio Padua y Gabriel, Anabela Correia Martins, Fernando Mendes, Lídia Cabral, Manuela Ferreira, Amadeu Gonçalves, Tatiana Durão D`Ávila Luz, Leonardo Gomes de Oliveira Luz, Raúl A. Martins, Alice Murteira Morgado, Maria da Luz Vale-Dias, Rui Porta-Nova, Tânia Cristina Malezan Fleig, Éboni Marília Reuter, Miriam Beatris Froemming, Sabrina Luciane Camara Guerreiro, Lisiane Lisbôa Carvalho, Daniel Guedelha, Pedro S. Coelho, A.T. Pereira, António Calha, Raúl Cordeiro, Ana Gonçalves, Ana Certo, Ana Cristina Araújo de Andrade Galvão, Ma Augusta Mata, Aline Welter, Elayne Crestani Pereira, Sandra Aparecida Ribeiro, Márcia Regina Kretzer, Juan-Fernando Jiménez-Díaz, Carla Jiménez-Rodríguez, Francisco-José Hernández-Martínez, Bienvenida-Del-Carmen Rodríguez-De-Vera, Alexandre Marques-Rodrigues, Patrícia Brazil Pereira Coelho, Tiago Bernardes, Alexandre de Araújo Pereira, Patrícia Sousa, João Ghizzo Filho, Nazaré Otília Nazário, Márcia Regina Kretzer, Odete Amaral, António Garrido, Nélio Veiga, Carla Nunes, Ana Rita Pedro, Carlos Pereira, António Almeia, Hélder Miguel Fernandes, Carlos Vasconcelos, Nélson Sousa, Víctor Machado Reis, M. João Monteiro, Romeu Mendes, Isabel Pinto, Tânia C. S. P. Pires, João Gama, Vera Preto, Norberto Silva, Carlos Pires Magalhães, Matilde Martins, Mafalda Duarte, Constança Paúl, Ignácio Martín, Arminda Pinheiro, Sandra Doria Xavier, J. Azevedo, E. Bento, C. Marques, M. Marques, A. Macedo, A.T. Pereira, José Pedro Almeida, António Almeida, Josiane Alves, Nélson Sousa, Francisco Saavedra, Romeu Mendes, Ana S. Maia, Michelle Teixeira Oliveira, Anderson Reis de Sousa, Paulo P. Ferreira, Luci S. Lopes, Eujcely C. Santiago, Sílvia Monteiro, Ângelo Jesus, Armanda Colaço, Antônio Ivo de Carvalho, Rita P. Silva, Agostinho Cruz, Ana Ferreira, Catarina Marques, João Paulo Figueiredo, Susana Paix�ão, Ana Ferreira, Carla Lopes, Fernando Moreira, João Paulo Figueiredo, Ana Ferreira, Diana Ribeiro, Fernando Moreira, João Paulo Figueiredo, Susana Paix�ão, Telma Fernandes, Diogo Amado, Jéssica Denise Vieira Leal, Marcelo Costa Velho Mendes de Azevedo, Sónia Ramalho, Catarina Mangas, Jaime Ribeiro, Rita Maria de Abreu Gonçalves, Amélia Fernandes Nunes, Ana Rita Tuna, Carlos Martins, Henriqueta D. Forte, Cláudia Costa, José António Tenedório, Paula Santana, José Augusto Andrade, Joana Pinto, C. Campofiorito, S. C. Nunes, Ana Sofia Carmo, A. Kaliniczenco, Bárbara Erllen da Silva Alves, Francisco Mendes, Carlos Jesus, Felipe Paiva Fonseca, Flávia de Sousa Gehrke, Carlos Albuquerque, Rita Batista, Madalena Cunha, António Dias, Olivério Ribeiro, Rosa Maria Grangeiro Martins, Teresa Madeira, Catarina Peixoto-Plácido, Nuno Rebelo dos Santos, Osvaldo Santos, Astrid Bergland, Asta Bye, Carla Lopes, Violeta Alarcão, Beatriz Goulão, Nuno Mendonça, Paulo Nicola, J. Gorjão Clara, João Gomes, Ana Querido, Catarina Tomás, Daniel Carvalho, Marina Cordeiro, Marlene Rosa, Alda Marques, Daniela Brandão, Óscar Ribeiro, Lia Araújo, Constança Paúl, Beatriz Minghelli, Sylvina Richaud, Ana Laura Mendes, Joana Marta‐Simões, Inês A. Trindade, Cláudia Ferreira, Teresa Carvalho,
S1 Health literacy and health education in adolescence Catarina Cardoso Tomás S2 The effect of a walking program on the quality of life and well-being of people with schizophrenia Emanuel Oliveira, D. Sousa, M. Uba-Chupel, G. Furtado, C. Rocha, A. Teixeira, P. Ferreira S3 Diagnosis and innovative treatments - the way to a better medical practice Celeste Alves S4 Simulation-based learning and how it is a high contribution Stefan Gisin S5 Formative research about acceptability, utilization and promotion ...
BioMed Central
Produção Nacional
Revisado por pares
Jéssica de Siqueira Guedes, Teiliane Rodrigues Carneiro, Pedro de Sena Murteira Pinheiro, Carlos Alberto Manssour Fraga, Carlos Maurício R. Sant’Anna, Eliezer J. Barreiro, Lı́dia Moreira Lima,
Sulfonylhydrazones are privileged structures with multifaceted pharmacological activity. Exploring the hypoglycemic properties of these organic compounds, we previously revealed a new series of N-sulfonylhydrazones (NSH) as antidiabetic drug candidates. Here, we evaluated the microsomal metabolism, chemical stability, and permeability profile of these NSH prototypes, focusing on the pharmacokinetic differences in N-methylated and non-N-methylated analogs. Our results demonstrated that the N-methylated ...
Tópico(s): Tryptophan and brain disorders
2022 - American Chemical Society | ACS Omega
Produção Nacional
Revisado por pares
Thayssa Tavares da Silva Cunha, Rafaela Ribeiro Silva, Daniel A. Rodrigues, Pedro de Sena Murteira Pinheiro, Thales Kronenberger, Carlos Maurício R. Sant’Anna, François Noël, Carlos Alberto Manssour Fraga,
Most neurodegenerative diseases are multifactorial, and the discovery of several molecular mechanisms related to their pathogenesis is constantly advancing. Dopamine and dopaminergic receptor subtypes are involved in the pathophysiology of several neurological disorders, such as schizophrenia, depression and drug addiction. For this reason, the dopaminergic system and dopamine receptor ligands play a key role in the treatment of such disorders. In this context, a novel series of conformationally ...
Tópico(s): Computational Drug Discovery Methods
2022 - Multidisciplinary Digital Publishing Institute | Biomolecules
Fábio Murteira, Pedro Oliveira, João Miranda, Albina Moreira, Margarida Correira,
DRESS syndrome is a rare and potentially fatal multisystemic reaction that occurs two to six weeks after exposure to certain drugs. It is characterized by fever, eosinophilia, and skin rash. Case of a 37-year-old man, black, with gout (started allopurinol 4 weeks before). He arrived at the Emergency Room complaining of headache, fever, abdominal pain, and scattered maculopapular skin lesions. The conducted study showed elevated transaminases and C-reactive protein, hepatomegaly, and peri-hepatic ...
Tópico(s): Pneumocystis jirovecii pneumonia detection and treatment
2021 - PAGEPress (Italy) | Italian Journal of Medicine
Pedro de Sena Murteira Pinheiro,
Tópico(s): Social and Economic Solidarity
2025 - | Revista Espacialidades
Produção Nacional
Revisado por pares
Gustavo Salgado Pires, Heber Victor Tolomeu, Daniel A. Rodrigues, Lı́dia Moreira Lima, Carlos Alberto Manssour Fraga, Pedro de Sena Murteira Pinheiro,
Tópico(s): Synthetic Organic Chemistry Methods
2025 - Multidisciplinary Digital Publishing Institute | Pharmaceuticals
Produção Nacional
Revisado por pares
Lucas Silva Franco, Marina Amaral Alves, Carlos Maurício R. Sant’Anna, Isadora Tairinne de Sena Bastos, R.C. Barroso, Fanny N. Costa, Fábio Furlan Ferreira, Carlos Alberto Manssour Fraga, Eliezer J. Barreiro, Lı́dia Moreira Lima, Daniel A. Rodrigues, Pedro de Sena Murteira Pinheiro,
Tópico(s): Organic Chemistry Cycloaddition Reactions
2025 - American Chemical Society | ACS Omega
Produção Nacional
Revisado por pares
Lucas Silva Franco, Barbara Jesus, Pedro de Sena Murteira Pinheiro, Carlos Alberto Manssour Fraga,
This work examines the current landscape of drug discovery and development, with a particular focus on the chemical and pharmacological spaces. It emphasizes the importance of understanding these spaces to anticipate future trends in drug discovery. The use of cheminformatics and data analysis enabled in silico exploration of these spaces, allowing a perspective of drugs, approved drugs after 2020, and clinical candidates, which were extracted from the newly released ChEMBL34 (March 2024). This perspective ...
Tópico(s): Metabolomics and Mass Spectrometry Studies
2024 - Multidisciplinary Digital Publishing Institute | Pharmaceuticals
Produção Nacional
Revisado por pares
Maria Letícia de Castro Barbosa, Pedro de Sena Murteira Pinheiro, Raissa Alves da Conceição, José R. Pires, Lucas Silva Franco, Carlos Maurício R. Sant’Anna, Eliezer J. Barreiro, Lı́dia Moreira Lima,
The 4-aminoquinazoline scaffold is a privileged structure in medicinal chemistry. Regioselective nucleophilic aromatic substitution (SNAr) for replacing the chlorine atom at the 4-position of 2,4-dichloroquinazoline precursors is well documented in the scientific literature and has proven useful in synthesizing 2-chloro-4-aminoquinazolines and/or 2,4-diaminoquinazolines for various therapeutic applications. While numerous reports describe reaction conditions involving different nucleophiles, solvents, ...
Tópico(s): Phenothiazines and Benzothiazines Synthesis and Activities
2024 - Multidisciplinary Digital Publishing Institute | Molecules