Search Results - "Kümmerle, Arthur E."

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…”
Get full text

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…”
Get full text

Quinolone-N-acylhydrazone hybrids as potent Zika and Chikungunya virus inhibitors by Marra, Roberta K.F., Kümmerle, Arthur E., Guedes, Guilherme P., Barros, Caroline de S., Gomes, Rafaela S.P., Cirne-Santos, Claudio C., Paixão, Izabel Christina N.P., Neves, Amanda P.

“…[Display omitted] •Quinolone-N-acylhydrazone hybrids were tested against arbovirus Zika (ZIKV) and Chikungunya (CHIKV)•The compounds exhibited excellent…”
Get full text

Antiprotozoal agents: How have they changed over a decade? by Fernandes, Vitória de Souza, Rosa, Rafael, Zimmermann, Lara A., Rogério, Kamilla R., Kümmerle, Arthur E., Bernardes, Lilian S. C., Graebin, Cedric S.

“…Neglected tropical diseases are a diverse group of communicable diseases that are endemic in low‐ or low‐to‐middle‐income countries located in tropical and…”
Get full text

Novel Co III complexes containing fluorescent coumarin-N-acylhydrazone hybrid ligands: Synthesis, crystal structures, solution studies and DFT calculations by Areas, Esther S., Bronsato, Bruna Juliana da S., Pereira, Thiago M., Guedes, Guilherme P., Miranda, Fábio da S., Kümmerle, Arthur E., da Cruz, Antônio G.B., Neves, Amanda P.

Get full text

Beneficial effects of a novel agonist of the adenosine A2A receptor on monocrotaline‐induced pulmonary hypertension in rats by Alencar, Allan K N, Pereira, Sharlene L, Montagnoli, Tadeu L, Maia, Rodolfo C, Kümmerle, Arthur E, Landgraf, Sharon S, 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

“…Background and Purpose Pulmonary arterial hypertension (PAH) is characterized by enhanced pulmonary vascular resistance, right ventricular hypertrophy and…”
Get full text

Structure-Based Discovery of Thiosemicarbazone Metalloproteinase Inhibitors for Hemorrhage Treatment in Snakebites by Ferreira, Francis B, Pereira, Thiago M, Souza, Dayane L. N, Lopes, Daiana S, Freitas, Vitor, Ávila, Veridiana M. R, Kümmerle, Arthur E, Sant’Anna, Carlos Mauricio R

“…The venoms of snakes are composed by many toxins, which are responsible for various toxic effects including intense pain, bleeding disorders, and local tissue…”
Get full text

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-…”
Get full text

Access to 4‑Alkylaminopyridazine Derivatives via Nitrogen-Assisted Regioselective Pd-Catalyzed Reactions by Blaise, Emilie, Kümmerle, Arthur E, Hammoud, Hassan, de Araújo-Júnior, João Xavier, Bihel, Frédéric, Bourguignon, Jean-Jacques, Schmitt, Martine

“…3-Substituted, 6-substituted, and unsymmetrical 3,6-disubstituted 4-alkylaminopyridazines were prepared from a sequence of three chemo- and regioselective…”
Get full text

MICROWAVE-ASSISTED SYNTHESIS AND PKA DETERMINATION OF UMBELLIFERONE: AN EXPERIMENT FOR THE UNDERGRADUATE ORGANIC CHEMISTRY LABORATORY by Pereira, Thiago, Franco, Daiana, Vitório, Felipe, Amaral, Ronaldo, Ponzoni, Aparecida, Kümmerle, Arthur

“…A synthetic procedure for obtaining the fluorescent coumarin umbelliferone (7-hydroxycoumarin) and its spectral parameters were fully developed aiming at an…”
Get full text

New Palladacycle-Derived Acylhydrazones as Pre-catalysts in Mirozoki-Heck Coupling and Oxyarylations by Leão, Raquel A C, Pinho, Vagner D, Coelho, Artur S, Kümmerle, Arthur E, Costa, Paulo R R

“…New acylhydrazone-based palladacycles are prepared and evaluated as pre-catalysts in Mirozoki-Heck and oxyarylation reactions…”
Get full text

Structural insights into cholinesterases inhibition by harmane β-carbolinium derivatives: A kinetics – molecular modeling approach by Torres, Juliana M., Lira, Aline F., Silva, Daniel R., Guzzo, Lucas M., Sant’Anna, Carlos M.R., Kümmerle, Arthur E., Rumjanek, Victor M.

“…[Display omitted] ► The inhibition kinetics of cholinesterases by β-carbolinium salts were determined. ► A molecular modeling study of its enzyme–ligand…”
Get full text

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…”
Get full text

MAOS and medicinal chemistry: some important examples from the last years by Nascimento-Júnior, Nailton M, Kümmerle, Arthur E, Barreiro, Eliezer J, Fraga, Carlos A M

“…This review aims to highlight microwave-assisted organic synthesis as applied to medicinal chemistry in the last years, showing some reactions performed under…”
Get full text

The Discovery of Protheolysis Targeting Chimeras (PROTACs), Evolution, Design and Perspectives in Modulating Inflammatory Diseases by Caruso, Lucas, M. Pereira, Thiago, E. Kümmerle, Arthur

“…Currently, most drugs have their mode of action based on occupation-oriented pharmacology (proteins modulation through temporary inhibition by association and…”
Get full text

Synthesis and Evaluation of Antiproliferative Activity, Topoisomerase IIα Inhibition, DNA Binding and Non-Clinical Toxicity of New Acridine–Thiosemicarbazone Derivatives by Sousa, Gleyton, de Almeida, Maria C. F, Lócio, Lucas L, dos Santos, Vanda L, Bezerra, Daniel P, Silva, Valdenizia R, de Almeida, Sinara M. V, Simon, Alice, Honório, Thiago da S, Cabral, Lucio M, Castro, Rosane N, de Moura, Ricardo O, Kümmerle, Arthur E

“…In this study, we report the synthesis of twenty new acridine–thiosemicarbazone derivatives and their antiproliferative activities. Mechanisms of action such…”
Get full text

Novel CoIII complexes containing fluorescent coumarin-N-acylhydrazone hybrid ligands: Synthesis, crystal structures, solution studies and DFT calculations by Areas, Esther S., Bronsato, Bruna Juliana da S., Pereira, Thiago M., Guedes, Guilherme P., Miranda, Fábio da S., Kümmerle, Arthur E., da Cruz, Antônio G.B., Neves, Amanda P.

“…A series of new CoIII complexes of the type [Co(dien)(L1−L3)]ClO4 (1–3), containing fluorescent coumarin-N-acylhydrazonate hybrid ligands,…”
Get full text

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…”
Get full text

Cytotoxicity evaluation and DNA interaction of Ru II -bipy complexes containing coumarin-based ligands by de Almeida, Patrícia S V B, de Arruda, Henrique Jefferson, Sousa, Gleyton Leonel S, Ribeiro, Felipe Vitório, de Azevedo-França, José Aleixo, Ferreira, Larissa A, Guedes, Guilherme P, Silva, Heveline, Kummerle, Arthur E, Neves, Amanda P

“…Although there are various treatment options for cancer, this disease still has caused an increasing number of deaths, demanding more efficient, selective and…”
Get more information

A proposed molecular basis for the selective resveratrol inhibition of the PGHS-1 peroxidase activity by Kümmerle, Arthur E., Sperandio da Silva, Gilberto M., Sant’Anna, Carlos M.R., Barreiro, Eliezer J., Fraga, Carlos A.M.

“…This work describes the theoretical basis of the selective inhibition of the prostaglandin endoperoxide H 2 synthase (PGHS)-1 peroxidase site promoted by the…”
Get full text