Search Results - "FRAGA, Carlos A. M"

The Methylation Effect in Medicinal Chemistry by Barreiro, Eliezer J, Kümmerle, Arthur E, Fraga, Carlos A. M

“…Barreiro et al examine the impact methylation has in medicinal chemistry. Methyl groups are active with regard to metabolism…”
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Design, Synthesis, and Pharmacological Evaluation of N‑Acylhydrazones and Novel Conformationally Constrained Compounds as Selective and Potent Orally Active Phosphodiesterase‑4 Inhibitors by Kümmerle, Arthur E, Schmitt, Martine, Cardozo, Suzana V. S, Lugnier, Claire, Villa, Pascal, Lopes, Alexandra B, Romeiro, Nelilma C, Justiniano, Hélène, Martins, Marco A, Fraga, Carlos A. M, Bourguignon, Jean-Jacques, Barreiro, Eliezer J

“…Among a small series of tested N-acylhydrazones (NAHs), the compound 8a was selected as a selective submicromolar phosphodiesterase-4 (PDE4) inhibitor…”
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Cytotoxic and Antiproliferative Activity of LASSBio-2208 and the Attempts to Determine Its Drug Metabolism and Pharmacokinetics In Vitro Profile by Pillpe-Meza, Raysa Magali, Gouveia, Wesley Leandro, Barbosa, Gisele, Fraga, Carlos A M, Barreiro, Eliezer J, Lima, Lidia Moreira

“…Inappropriate expression of histone deacetylase (HDAC-6) and deregulation of the phosphatidylinositol 3-kinase (PI3K) signalling pathway are common aberrations…”
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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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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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Duvelisib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Phosphoinositide 3-Kinases by Rodrigues, Daniel A, Sagrillo, Fernanda S, Fraga, Carlos A M

“…Duvelisib (Copiktra ) is a dual inhibitor of phosphoinositide 3-kinases (PI3Kδ and PI3Kγ). In 2018, duvelisib was first approved by the Food and Drug…”
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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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Design, Synthesis, and Pharmacological Evaluation of Novel N‑Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors by Rodrigues, Daniel A, Ferreira-Silva, Guilherme À, Ferreira, Ana C. S, Fernandes, Renan A, Kwee, Jolie K, Sant’Anna, Carlos M. R, Ionta, Marisa, Fraga, Carlos A. M

“…This manuscript describes a novel class of N-acylhydrazone (NAH) derivatives that act as histone deacetylase (HDAC) 6/8 dual inhibitors and were designed from…”
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Design, Synthesis, and Pharmacological Profile of Novel Fused Pyrazolo[4,3-d]pyridine and Pyrazolo[3,4-b][1,8]naphthyridine Isosteres:  A New Class of Potent and Selective Acetylcholinesterase Inhibitors by Barreiro, Eliezer J, Camara, Celso A, Verli, Hugo, Brazil-Más, Leonora, Castro, Newton G, Cintra, Wagner M, Aracava, Yasco, Rodrigues, Carlos R, Fraga, Carlos A. M

“…A new family of tacrine (THA) analogues (7−9, 12), containing the azaheterocyclic pyrazolo[4,3-d]pyridine or pyrazolo[3,4-b][1,8]naphthyridine systems as…”
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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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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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Discovery of Novel Orally Active Tetrahydro-Naphthyl-N-Acylhydrazones with In Vivo Anti-TNF-α 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-β (kappa β kinase inhibitor) enzyme, which participates in the activation of the nuclear factor κB (NF-κB)…”
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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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Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents by Carvalho, Samir A., Feitosa, Larisse O., Soares, Márcio, Costa, Thadeu E.M.M., Henriques, Maria G., Salomão, Kelly, de Castro, Solange L., Kaiser, Marcel, Brun, Reto, Wardell, James L., Wardell, Solange M.S.V., Trossini, Gustavo H.G., Andricopulo, Adriano D., da Silva, Edson F., Fraga, Carlos A.M.

“…We report herein the synthesis and trypanocidal profile of new (E)-cinnamic N-acylhydrazones (NAHs) designed by exploiting molecular hybridization between the…”
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Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives by Kümmerle, Arthur E., Raimundo, Juliana M., Leal, Carla M., da Silva, Givanildo S., Balliano, Tatiane L., Pereira, Mariano A., de Simone, Carlos A., Sudo, Roberto T., Zapata-Sudo, Gisele, Fraga, Carlos A.M., Barreiro, Eliezer J.

“…In this report we disclose the synthesis, vasodilatory activity, and identification of bioactive conformation of new N-acylhydrazone and N-methyl-…”
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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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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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Design and synthesis of 3,4-methylenedioxy-6-nitrophenoxyacetylhydrazone derivatives obtained from natural safrole: New lead-agents with analgesic and antipyretic properties by Bezerra-Netto, Heleno J.C., Lacerda, Daniel I., Miranda, Ana Luisa P., Alves, Hélio M., Barreiro, Eliezer J., Fraga, Carlos A.M.

“…The discovery of the new powerful analgesic and long-lasting antipyretic N-acylhydrazone prototype LASSBio-891 is reported. In this work, we reported the…”
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N -acylhydrazone derivative ameliorates monocrotaline-induced pulmonary hypertension through the modulation of adenosine AA2R activity by Alencar, Allan K.N, Pereira, Sharlene L, da Silva, Flavia E, Mendes, Luiza V.P, Cunha, Valéria do M.N, Lima, Lidia M, Montagnoli, Tadeu L, Caruso-Neves, Celso, Ferraz, Emanuelle B, Tesch, Roberta, Nascimento, José H.M, Sant'Anna, Carlos M.R, Fraga, Carlos A.M, Barreiro, Eliezer J, Sudo, Roberto T, Zapata-Sudo, Gisele

“…Abstract Background Pulmonary arterial hypertension (PAH) is a disease that results in right ventricular (RV) dysfunction. While pulmonary vascular disease is…”
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Novel potent imidazo[1,2-a]pyridine-N-Glycinyl-hydrazone inhibitors of TNF-α production: in vitro and in vivo studies by Lacerda, Renata B, Sales, Natália M, da Silva, Leandro L, Tesch, Roberta, Miranda, Ana Luisa P, Barreiro, Eliezer J, Fernandes, Patricia D, Fraga, Carlos A M

“…In this work, we describe the design, synthesis and pharmacological evaluation of novel imidazo[1,2-a]pyridine-N-glycinyl-hydrazone derivatives (1a-k) intended…”
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