- Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021) - Possible effects on phosphodiesterase
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This study describes the synthetic route and molecular computational docking of LQFM 021, as well as examines its biological effects and toxicity. The docking studies revealed strong interaction of LQFM 021 to phosphodiesterase-3 (PDE-3). In isolated arte
- Martins, Daniella Ramos,Pazini, Francine,Alves, Vinicius De Medeiros,De Moura, Soraya Santana,Liao, Luciano Morais,De Magalhaes, Mariana Torquato Quezado,Valadares, Marize Campos,Andrade, Carolina Horta,Menegatti, Ricardo,Rocha, Matheus Lavorenti
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- Synthesis of pyrazole-carboxamides and pyrazole-carboxylic acids derivatives: Simple methods to access powerful building blocks
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Hybrid systems containing pyrazole moiety show a wide spectrum of biological activities. To access novel hybrids with pyrazole ring, in this work we synthesized twenty pyrazole-carboxylic acids and twenty pyrazole-carboxamides, using simple synthetic methods, to be used as building blocks in the development of new structures.
- Dos Santos, Maurício Silva,Ferreira, Byanca Silva,Silva, Rafaela Corrêa,Souto, Bernardo Araújo
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p. 335 - 343
(2021/09/07)
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- A Convenient Synthesis of Pyrazole-imidazoline Derivatives by Microwave Irradiation
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A series of 28 hybrids pyrazole-imidazolines 1a–n and 2a–n were synthesized by a new methodology using microwave irradiation, in short time (20–30?min), in low power (50–70?W), and in 34–92% yield. Among all methodologies evaluated, no side products were obtained. All derivatives were completely characterized by FT–IR, 1H and 13C NMR, GC–MS, and HRMS.
- de S. Rosa, Getúlio,Souto, Bernardo A.,Pereira, Cynthia N.,Teixeira, Bruna C.,dos Santos, Maurício S.
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p. 1825 - 1830
(2019/04/30)
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- HETEROGENEOUS COPPER-CATALYZED AEROBIC OXIDATIVE CONVERSION OF AROMATIC ALDEHYDES TO CORRESPONDING NITRILES
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The present invention relates to a method of aerobic oxidative converting aromatic aldehyde to nitrile. More specifically, the present invention relates to a method of aerobic oxidative conversion of an aromatic aldehyde to nitrile using a heterogeneous copper catalyst, and optimization of reaction conditions applied thereto. The method can obtain nitrile at high yield with respect to various substrates by synthesizing nitrile, e.g., benzonitrile from aromatic aldehyde, e.g., benzaldehyde and an ammonia source, e.g., ammonia water under an oxygen condition by using TEMPO (2,2,6,6-tetramethylpiperidine 1-oxyl) and a heterogeneous copper catalyst (Cu@C) obtained by pyrolyzing HKUST-1, i.e., a type of a metal-organic framework, and enables the heterogeneous copper catalyst to be reused at least three or more times without significant loss of catalytic activities since the heterogeneous copper catalyst maintains structure thereof even under the presence of the ammonia source.COPYRIGHT KIPO 2018
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Paragraph 0174-0177; 0180; 0181
(2018/07/31)
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- HETEROGENEOUS COPPER-CATALYZED AEROBIC OXIDATIVE CONVERSION OF ALCOHOLS TO CORRESPONDING NITRILES
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The present invention refers to a method relates to knight reel aerobic oxidation conversion to alcohol (Aerobic oxidative conversion), metal - organic framework is provided electromagnetic wave is pyrolytically cracking using non-uniform copper catalyst (Cu ? C) and TEMPO HKUST-a 1, alcohol (e.g., benzyl alcohol) aromatic aldehyde (e.g., benzaldehyde) aromatic 1 difference after conversion into ammonia source (e.g., ammonia) manner won - port (One-a pot) aromatic aldehydes (e.g., benzo knight reel) added into knight reel by switching, high yield various substrate results in obtaining uniform copper catalyst in the presence of ammonia source knight reel and said holding structure even a significant catalyst activity may be reused without loss to at least 3 or more times, using alcohol knight reel aerobic to non-uniform copper catalyzed oxidative cycle, and applied to the optimization of the reaction conditions are disclosed. (by machine translation)
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Paragraph 0104-0111; 0199
(2018/10/03)
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- Synthesis and antileishmanial evaluation of 1-aryl-4-(4,5-dihydro-1H- imidazol-2-yl)-1H-pyrazole derivatives
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A series of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (4a-g) and 5-amino-1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (5a-g) were synthesized and evaluated in vitro against three Leishmania species: L. amazonensis, L. braziliensis and L. infantum (L. chagasi syn.). The cytotoxicity was assessed. Among the derivatives examined, six compounds emerged as the most active on promastigotes forms of L. amazonensis with IC50 values ranging from 15 to 60 μM. The reference drug pentamidine presented IC 50 = 10 μM. However, these new compounds were less cytotoxic than pentamidine. Based on these results, the more promising derivative 5d was tested further in vivo. This compound showed inhibition of the progression of cutaneous lesions in CBA mice infected with L. amazonensis relative to an untreated control.
- Dos Santos, Mauricio S.,Oliveira, Mariana L.V.,Bernardino, Alice M.R.,De Leo, Rosa M.,Amaral, Veronica F.,De Carvalho, Flavia T.,Leon, Leonor L.,Canto-Cavalheiro, Marilene M.
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p. 7451 - 7454
(2012/02/03)
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