- 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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- Solvent-free and montmorillonite K10-catalyzed domino reactions for the synthesis of pyrazoles with alkynylester as a dual synthon
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A highly regioselective, solvent-free and montmorillonite K10 clay-catalyzed domino process with an unprecedented ring-closing C-C bond-formation reaction is described for the synthesis of a new class of 1,3,4-trisubstituted and 1,4-disubstituted pyrazole
- Annes, Sesuraj Babiola,Ramesh, Subburethinam,Saritha, Rajendhiran,Shankar, Bhaskaran,Subramanian, Saravanan
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supporting information
p. 2388 - 2393
(2020/05/13)
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- Anti-inflammatory effect of a new piperazine derivative: (4-methylpiperazin-1-yl)(1-phenyl-1H-pyrazol-4-yl)methanone
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Aims: This study investigates the anti-nociceptive and anti-inflammatory effects of new piperazine compound (LQFM182) as well as the toxicity acute in vitro. Main methods: To evaluate the anti-nociceptive activity, the acetic acid-induced abdominal writhing test, tail flick test and formalin-induced pain test were used. The anti-inflammatory activity was evaluated using the models of paw oedema and pleurisy induced by carrageenan and some inflammatory parameters were evaluated, including cell migration, myeloperoxidase enzyme activity and the levels of TNF-α and IL-1β cytokines in pleural exudate. The acute oral systemic toxicity of LQFM182 in mice was evaluated through the neutral red uptake (nru) assay. Key findings: LQFM182 (50, 100 or 200?mg/kg, p.o.) decreased the number of writhings induced by acetic acid in a dose-dependent manner, and an intermediate dose (100?mg/kg, p.o.) reduced the paw licking time of animals in the second phase of the formalin test. Furthermore, LQFM182 (100?mg/kg, p.o.) reduced oedema formation at all hours of the paw oedema induced by carrageenan test and in pleurisy test reduced cell migration from the reduction of polymorphonuclear cells, myeloperoxidase enzyme activity and the levels of pro-inflammatory cytokines IL-1β and TNF-α. Therefore, it was classified in GHS category 300?50??2000?mg/kg. Significance: Reduction of the TNF-α and IL-1β levels.
- Batista, Daniel C.,Silva, Daiany P. B.,Florentino, Iziara F.,Cardoso, Carina S.,Gon?alves, Merita P.,Valadares, Marize C.,Li?o, Luciano M.,Sanz, Germán,Vaz, Boniek G.,Costa, Elson A.,Menegatti, Ricardo
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p. 217 - 226
(2017/10/06)
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- NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE
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The present invention relates to piperidine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
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Page/Page column 72
(2009/10/01)
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- Inhibitors of 15-hydroxyprostaglandin dehydrogenase for stimulating pigmentation of the skin or skin appendages
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Inhibitors of 15-hydroxyprostaglandin dehydrogenase (15-PGDH), for example tetrazole, styrylpyrazole, phenylfuran, phenylthiophene, phenylpyrrazole, pyrazolecarboxamide, 2-thioacetamide and azo compounds, are useful for promoting or stimulating pigmentati
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Page/Page column 62-63
(2010/10/19)
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- A novel series of potent and selective small molecule inhibitors of the complement component C1s
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Activation of the classical pathway of complement has been implicated in disease states such as hereditary angioedema, ischemia-reperfusion injury and acute transplant rejection. The trypsin-like serine protease C1s represents a pivotal upstream point of
- Subasinghe, Nalin L.,Ali, Farah,Illig, Carl R.,Rudolph, M. Jonathan,Klein, Scott,Khalil, Ehab,Soll, Richard M.,Bone, Roger F.,Spurlino, John C.,DesJarlais, Renee L.,Crysler, Carl S.,Cummings, Maxwell D.,Morris Jr., Philip E.,Kilpatrick, John M.,Babu, Y. Sudhakara
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p. 3043 - 3047
(2007/10/03)
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- Synthesis of Heterocycles from 4-(2-Hydroxybenzoyl)-1-phenylpyrazole
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4-(2-Hydroxybenzoyl)-1-phenylpyrazole (1) has been used in the synthesis of benzofuran (2), coumarin (5) and benzisoxazole (9).
- Coutinho, Dionysia L. M.,Fernandes, Peter S.
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- The Direct Carboxylation of Pyrazoles
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Various pyrazole-4-carboxylic acids 4 were obtained by a direct carboxylation reaction of pyrazoles 1 with excess, oxalyl chloride.
- Chiriac, C. I.
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p. 753 - 755
(2007/10/02)
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