Search Results - "Fraga, Carlos AM"

Antihyperalgesic effects of a novel muscarinic agonist (LASSBio-873) in spinal nerve ligation in rats by Mendes, Thaiana CF, Antunes, Fernanda, Trachez, Margarete M, Nascimento Jr, Nailton M, Fraga, Carlos AM, Barreiro, Eliezer J, Zapata-Sudo, Gisele, Sudo, Roberto T

“…Summary New chemicals or adjuvants with analgesic effects on chronic pain are needed and clinically relevant due to the limited number of effective compounds…”
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Discovery of novel analgesic and anti-inflammatory 3-arylamine-imidazo[1,2- a]pyridine symbiotic prototypes by Lacerda, Renata B., de Lima, Cleverton K.F., da Silva, Leandro L., Romeiro, Nelilma C., Miranda, Ana Luisa P., Barreiro, Eliezer J., Fraga, Carlos A.M.

“…We describe herein the discovery of LASSBio-1135 ( 3a) as a novel in vivo antinociceptive and anti-inflammatory symbiotic prototype that act as selective…”
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Discovery of Novel Orally Active Tetrahydro-Naphthyl-N-Acylhydrazones with In Vivo Anti-TNF-[alpha] Effect and Remarkable Anti-Inflammatory Properties by Cordeiro, Natália M, Freitas, Rosana H. C. N, Fraga, Carlos A. M, Fernandes, Patricia D

“…LASSBio-1524 was designed as inhibitor of the IKK-[beta] (kappa [beta] kinase inhibitor) enzyme, which participates in the activation of the nuclear factor…”
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Medicinal chemistry of N-acylhydrazones: new lead-compounds of analgesic, antiinflammatory and antithrombotic drugs by Fraga, Carlos A M, Barreiro, Eliezer J

“…In this article we provide an overview on the medicinal chemistry of new bioactive N-acylhydrazone (NAH) derivatives designed through the structural…”
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New insights into pharmacological profile of LASSBio-579, a multi-target N-phenylpiperazine derivative active on animal models of schizophrenia by Neves, Gilda, Antonio, Camila B., Betti, Andresa H., Pranke, Mariana A., Fraga, Carlos A.M., Barreiro, Eliezer J., Noël, François, Rates, Stela M.K.

“…► The N-phenylpiperazine LASSBio-579 is effective in a model of sensoriomotor gating. ► LASSBio-579 is a multi-target ligand with potential antipsychotic…”
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LASSBio-1422: a new molecular scaffold with efficacy in animal models of schizophrenia and disorders of attention and cognition by Betti, Andresa H, Antonio, Camila B, Pompeu, Thais E.T, Martins, Thaise S, Herzfeldt, Vivian, Stolz, Eveline D, Fraga, Carlos A.M, Barreiro, Eliezer, Noël, François, Rates, Stela M.K

“…Aiming to identify new antipsychotic lead-compounds, our group has been working on the design and synthesis of new N-phenylpiperazine derivatives. Here, we…”
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Design, synthesis and analgesic properties of novel conformationally-restricted N-acylhydrazones (NAH) by Kümmerle, Arthur E., Vieira, Marina M., Schmitt, Martine, Miranda, Ana L.P., Fraga, Carlos A.M., Bourguignon, Jean-Jacques, Barreiro, Eliezer J.

“…A set of six azaheterocycles were designed as conformationnaly-constrained N-acylhydrazones and tested as analgesics…”
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LASSBio-1829 Hydrochloride: Development of a New Orally Active N-Acylhydrazone IKK2 Inhibitor with Anti-inflammatory Properties by Guedes, Isabella A., Freitas, Rosana H. C. N., Cordeiro, Natália M., Nascimento, Thaís S. do, Valerio, Tayna S., Fernandes, Patrícia D., Dardenne, Laurent E., Fraga, Carlos A. M.

“…Inhibitor of nuclear factor κB kinase 2 (IKK2) is suggested to be a potential target for the development of novel anti‐inflammatory and anticancer drugs. In…”
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Microwave-assisted synthesis and structure–activity relationships of neuroactive pyrazolo[3,4- b]pyrrolo[3,4- d]pyridine derivatives by Nascimento-Júnior, Nailton M., Mendes, Thaiana C.F., Leal, Daniella M., Corrêa, Claudia Maria N., Sudo, Roberto T., Zapata-Sudo, Gisele, Barreiro, Eliezer J., Fraga, Carlos A.M.

“…The microwave assisted hetero Diels–Alder synthesis and the sedative profile of heterotricyclic pyrazolo[3,4- b]pyrrolo[3,4- d]pyridine derivatives ( 1a– 1f),…”
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LASSBio-294, A Compound With Inotropic and Lusitropic Activity, Decreases Cardiac Remodeling and Improves Ca2+ Influx Into Sarcoplasmic Reticulum After Myocardial Infarction by Costa, Daniele G., da Silva, Jaqueline S., Kümmerle, Arthur E., Sudo, Roberto T., Landgraf, Sharon S., Caruso-Neves, Celso, Fraga, Carlos A.M., de Lacerda Barreiro, Eliezer J., Zapata-Sudo, Gisele

“…Background Myocardial infarction (MI) is commonly associated with cardiac hypertrophy, reduced Ca2+ uptake into the sarcoplasmic reticulum (SR) and impaired…”
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Understanding the Structural Basis of ALDH-2 Inhibition by Molecular Docking by Ferreira, Thayssa T S C, Fraga, Carlos A M

“…The ALDH-2 enzyme has been identified as an important therapeutic target for the development of new drugs for the treatment of cocaine addiction. Several…”
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Novel thienylacylhydrazone derivatives inhibit platelet aggregation through cyclic nucleotides modulation and thromboxane A sub(2 synthesis inhibition) by Brito, Fernanda CF, Kummerle, Arthur E, Lugnier, Claire, Fraga, Carlos AM, Barreiro, Eliezer J, Miranda, Ana LP

“…The aim of this study has been to investigate the antiplatelet activity of a new series of thienylacylhydrazone derivatives analogous to the lead compound…”
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Pharmacological Characterization of (3-Thienylidene)-3,4-Methylenedioxybenzoylhydrazide: A Novel Muscarinic Agonist With Antihypertensive Profile by Zapata-Sudo, Gisele, Pereira, Sharlene L., Beiral, Hellen J.V., Kummerle, Arthur E., Raimundo, Juliana M., Antunes, Fernanda, Sudo, Roberto T., Barreiro, Eliezer J., Fraga, Carlos A.M.

“…Background Several new bioactive compounds of the N-acylhydrazone class were developed from the safrole, a Brazilian natural product obtained from sassafras…”
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Determination of the cardioactive prototype LASSBio-294 and its metabolites in dog plasma by LC–MS/MS: Application for a pharmacokinetic study by Braga, Rodolpho C., Tôrres, Andréa C.B., Persiano, Camille B., Alves, Rosângela O., Fraga, Carlos A.M., Barreiro, Eliezer J., de Oliveira, Valéria

“…In this work we describe the evaluation of the pharmacokinetics of a novel cardioactive compound of the N-acylhydrazone class, LASSBio-294, using…”
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Structural insights into IKKβ inhibition by natural products staurosporine and quercetin by Avila, Carolina M., Romeiro, Nelilma C., Sant’Anna, Carlos M.R., Barreiro, Eliezer J., Fraga, Carlos A.M.

“…This work describes the structural basis of the IKKβ inhibition by staurosporine and quercetin in ATP binding site. This Letter describes the results of two…”
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Design of new dopamine D2 receptor ligands: Biosynthesis and pharmacological evaluation of the hydroxylated metabolite of LASSBio-581 by Pazini, Francine, Menegatti, Ricardo, Sabino, José R., Andrade, Carolina H., Neves, Gilda, Rates, Stela M.K., Noël, François, Fraga, Carlos A.M., Barreiro, Eliezer J., de Oliveira, Valéria

“…The biosynthesis of the p-hydroxylated metabolite of LASSBio-581 by Cunninghamella echinulata and its pharmacological evaluation is reported. LASSBio-581 is a…”
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