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Academic literature on the topic 'Pyrazolone derivatives'

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Published: 18 May 2024

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Journal articles on the topic "Pyrazolone derivatives"

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Abd-Ella, Aly A., Saoud A. Metwally, Mokhtar A. Abd ul-Malik, Yasser A. El-Ossaily, Fathy M. Abd Elrazek, Safwat A. Aref, Youssra A. Naffea, and Shaban A. A. Abdel-Raheem. "A review on recent advances for the synthesis of bioactive pyrazolinone and pyrazolidinedione derivatives." Current Chemistry Letters 11, no. 2 (2022): 157–72. http://dx.doi.org/10.5267/j.ccl.2022.2.004.

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Oxo derivatives of pyrazolines and pyrazolidines are important heterocyclic compounds due to their unique biological activities and have been widely applied in pharmaceutical and agromedical fields. In this review, we provide an account of some recent advances in the field of pyrazolone chemistry, specifically on the reported synthesis methods of pyrazolinone (3-oxo-1,2-dihydropyrazole) and 3,5-pyrzolidinediones (3,5-dioxotetrahydropyrazoles) derivatives.

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Edrees, Mastoura M. "Synthesis of 4-hydrazinopyrazolo[3,4-d]pyrimidines and their Reactions with Carbonyl Compounds." Journal of Chemical Research 37, no. 1 (January 2013): 6–10. http://dx.doi.org/10.3184/174751912x13543818811749.

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Synthesis of a new 4-hydrazinopyrazolo[3,4- d]pyrimidine was achieved via heating (4,6-dithioxo-1 H-pyrazolo[3,4- d] pyrimidin-3-yl)acetonitrile with hydrazine hydrate. Reactions of the latter product with thiophene-2-carbaldehyde and ethyl hydrazonoacetoacetate analogues afforded the corresponding hydrazone and pyrazole derivatives, respectively. Similarly, condensation of 2-[6-(benzylsulfanyl)-4-hydrazino-1 H-pyrazolo[3,4- d]pyrimidin-3-yl]acetonitrile with thiophene-2-carbaldehyde and ethyl hydrazonoacetoacetate analogues gave the respective hydrazone and pyrazolone derivatives. Alkylation reactions of 2-[4,6-bis(benzylsulfanyl)-1 H-pyrazolo[3,4- d]pyrimidin-3-yl]acetonitrile with arylamines gave the respective 4-( N-arylamino)-6-benzylsulfanylpyrazolo[3,4- d]pyrimidine derivatives.

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Gil-Ordóñez, Marta, Camille Aubry, Cristopher Niño, Alicia Maestro, and José M. Andrés. "Squaramide-Catalyzed Asymmetric Mannich Reaction between 1,3-Dicarbonyl Compounds and Pyrazolinone Ketimines: A Pathway to Enantioenriched 4-Pyrazolyl- and 4-Isoxazolyl-4-aminopyrazolone Derivatives." Molecules 27, no. 20 (October 17, 2022): 6983. http://dx.doi.org/10.3390/molecules27206983.

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A series of N-Boc ketimines derived from pyrazolin-5-ones have been used as electrophiles in enantioselective Mannich reactions with different 1,3-dicarbonyl compounds. This method provides a direct pathway to access the 4-amino-5-pyrazolone derivatives bearing a quaternary substituted stereocenter and containing two privileged structure motifs, the β-diketone and pyrazolinone substructures. The adducts were obtained in excellent yields (up to 90%) and enantioselectivities (up to 94:6 er) by employing a very low loading of 2 mol% of a quinine-derived bifunctional squaramide as an organocatalyst for a wide range of substrates. In addition, the utility of the obtained products was demonstrated through one step transformations to enantioenriched diheterocyclic systems (4-pyrazolyl-pyrazolone and 4-isoxazolyl-pyrazolone), potentially promising candidates for drug discovery.

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Gediz Erturk, Aliye, and Hilal Omerustaoglu. "Synthesis and Cytotoxic Evaluation of Some Substituted 5-Pyrazolones and Their Urea Derivatives." Molecules 25, no. 4 (February 18, 2020): 900. http://dx.doi.org/10.3390/molecules25040900.

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In this paper, a series of new substituted-5-pyrazolones were first synthesized, then formulated by the Vilsmeier–Haack reaction to obtain substituted-4-carbaldehyde-5-pyrazolones. In the final step, when urea was reacted with formulated pyrazolones, we found that, instead of the C=N bond in azomethine form, the compounds tautomerized to form a series of novel pyrazole-4-ylidenemethylurea structures. The structures of these compounds were elucidated by FTIR, 1H, 13C NMR, LC-MS/MS, and elemental analysis methods. The cytotoxic and antioxidant effects of substituted 5-pyrazolones and their pyrazolone-urea derivatives were investigated in metastatic A431 and noncancerous HaCaT human keratinocytes by a mitochondrial activity test. The effects of the compounds on the migration of cancerous and noncancerous cell lines were investigated by using a cell scratch assay. The General Linear Model, Statistical Package for Social Sciences (SPSS v26) was used to determine if there was a statistically significant difference between the control and the treatment groups. Four of the nine compounds showed an antioxidant effect. All 5-pyrazolone-urea compounds showed higher toxicity (p < 0.05) in cancerous A431 cells compared to noncancerous cells at all time points. All compounds also showed a biphasic hormetic effect. Four of the nine compounds inhibited cell migration.

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Pattan, S. R., P. A. Chavan, R. A. Muluk, S. S. Dengale, S. V. Hiremath, K. D. Pansare, S. S. Vetal, and J. S. Pattan. "SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME HETEROCYCLES CONTAINING OXADIAZOLE AND PYRAZOLE RING FOR ANTI-BACTERIAL, ANTI-FUNGAL AND ANTI-TUBERCULAR ACTIVITIES." INDIAN DRUGS 49, no. 03 (March 28, 2012): 18–24. http://dx.doi.org/10.53879/id.49.03.p0018.

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1, 3, 4-oxadiazoles were synthesized by treating pyrazine-2-carbohydrazide with CS2 and alc. KOH and their derivatives were prepared by using R-Cl compounds. pyrazolones were synthesized by treatingpyrazine-2-carbohydrazide with ethyl acetoacetate. The derivatives of pyrazolone were prepared by refluxing pyrazolone with formaldehyde and different substituted secondary amines. All the synthesized compounds were characterized by IR, 1H-NMR and elemental analysis and evaluated for antibacterial, antifungal and antitubercular activities.

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Yang, Kai, Xiaoze Bao, Ye Yao, Jingping Qu, and Baomin Wang. "Iodine-mediated cross-dehydrogenative coupling of pyrazolones and alkenes." Organic & Biomolecular Chemistry 16, no. 34 (2018): 6275–83. http://dx.doi.org/10.1039/c8ob01645c.

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Brogden, Rex N. "Pyrazolone Derivatives." Drugs 32, Supplement 4 (1986): 60–70. http://dx.doi.org/10.2165/00003495-198600324-00006.

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Manojkumar, Parameswaran, Thengungal Ravi, and Gopalakrishnan Subbuchettiar. "Synthesis of coumarin heterocyclic derivatives with antioxidant activity and in vitro cytotoxic activity against tumour cells." Acta Pharmaceutica 59, no. 2 (June 1, 2009): 159–70. http://dx.doi.org/10.2478/v10007-009-0018-7.

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Synthesis of coumarin heterocyclic derivatives with antioxidant activity andin vitrocytotoxic activity against tumour cellsThe aim of the present work was to synthesise coumarinyl heterocycles and to elucidate the potential role of these compounds as antioxidants and cytotoxic agents against Dalton's lymphoma ascites tumour cells (DLA) and Ehrlich ascites carcinoma cells (EAC). The synthesis of coumarin derivatives containing pyrazole, pyrazolone, thiazolidin-4-one, 5-carboxymethyl-4-thiazolidinone and 3-acetyl-1,3,4-oxadiazole ring is reported. 4-Methylcoumarinyl-7-oxyacetic acid hydrazide (1) reacted with arylazopropanes or hydrazono-3-oxobutyrate derivatives to form pyrazole (3a-c) and pyrazolone derivatives (5a-c). Heterocyclisation of Schiff's bases of 1 with thioglycolic acid, thiomalic acid or acetic anhydride afforded novel heterocyclic derivatives 4-thiazolidinones (7a-c), 5-carboxymethyl-4-thiazolidinones (8a-c) and oxadiazoles (9a-c), respectively. Some of the compounds showed promising antioxidant activityin vitroand cytotoxic activity against DLA cells and EAC cells.

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Zhang, Wande, Shah Nawaz, Yue Huang, Wenjing Gong, Xingfu Wei, Jingping Qu, and Baomin Wang. "C-4 benzofuranylation of pyrazolones by a metal-free catalyzed indirect heteroarylation strategy." Organic & Biomolecular Chemistry 19, no. 46 (2021): 10215–22. http://dx.doi.org/10.1039/d1ob01920a.

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A metal-free catalyzed indirect heteroarylation of pyrazolones with 2-(3-hydroxy-3,3-diarylprop-1-yn-1-yl)phenols has been developed, delivering a wide range of novel 4-benzofuran-substituted pyrazolone derivatives.

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Bao, Xiaoze, Xingyue Wang, Jin-Miao Tian, Xinyi Ye, Baomin Wang, and Hong Wang. "Recent advances in the applications of pyrazolone derivatives in enantioselective synthesis." Organic & Biomolecular Chemistry 20, no. 12 (2022): 2370–86. http://dx.doi.org/10.1039/d1ob02426d.

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Dissertations / Theses on the topic "Pyrazolone derivatives"

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Mariappan, G. "Cardioprotective properties of pyrazotone derivatives in myocardial ischemic reperfusion injury." Thesis, University of North Bengal, 2011. http://hdl.handle.net/123456789/1501.

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Vetica, Fabrizio [Verfasser]. "Organocatalytic Asymmetric Synthesis of Isochromanones, Tetranortriterpenoids and Pyrazolone Derivatives / Fabrizio Vetica." München : Verlag Dr. Hut, 2018. http://d-nb.info/1155056213/34.

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Motson, Graham Robert. "Coordination chemistry of 3-(2'-pyridyl) pyrazole derivative ligands." Thesis, University of Bristol, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.391153.

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Nakhai, Azadeh. "Synthetic studies of nitrogen containing heterocycles, particularly pyrazole and benzotriazine derivatives." Stockholm, 2009. http://diss.kib.ki.se/2009/978-91-7409-687-3/.

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Yazici, Ceyda. "Synthesis Of 4-iodopyrazole Derivatives." Master's thesis, METU, 2008. http://etd.lib.metu.edu.tr/upload/3/12609750/index.pdf.

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Pyrazoles have been studied for over a century as an important class of heterocyclic compounds and continue to attract considerable interest due to the broad range of biological activities they possess. The electrophilic cyclization of the acetylenic hydrazones initiated by molecular iodine could provide new ways of synthesizing biologically active 4-iodopyrazole derivatives, which are important precursors for the synthesis of highly substituted pyrazole derivatives. For this reason, we investigated the synthesis of 4-iodopyrazole derivatives, such as 1-aryl- 5-alkyl/aryl-4-iodopyrazoles, starting from phenylhydrazine and ,-acetylenic aldehyde derivatives. Initially, ,-acetylenic aldehydes were synthesized by formylation reaction of corresponding alkynes with DMF. Then, hydrazone derivatives of these aldehydes were prepared by heating them with phenylhydrazine in a neat manner at 55 °
C for 5 h. Finally, acetylenic phenyl hydrazone derivatives were subjected to electrophilic cyclization by treating with excess molecular iodine at 80 °
C for 3 h. Although electrophilic cyclization is commonly used in organic chemistry, it has not been employed for the cyclization of acetylenic phenyl hydrazones to pyrazole derivatives. Under optimized conditions, these reactions afforded 1-aryl-5-alkyl/aryl-4-iodopyrazole derivatives in moderate to good yields as the single or the major product of the reactions. In some cases, 1-aryl-5-alkyl/arylpyrazole derivatives resulted from these reactions as minor products. In conclusion, 4-iodopyrazole derivatives were synthesized for the first time directly from acyclic starting materials, ,-acetylenic phenylhydrazones and iodine, via electrophilic cyclization.

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Rango, Enrico. "PRECLINICAL CHARACTERIZATION OF SFK INHIBITORS, PYRAZOLO[3,4-d]PYRIMIDINE SCAFFOLD-BASED DERIVATIVES, FOR CANCER TREATMENT." Doctoral thesis, Università di Siena, 2021. http://hdl.handle.net/11365/1140389.

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The first part of this thesis essentially focuses on the preclinical characterization of Si306, a pyrazolo[3,4-d]pyrimidine derivative, identified as a very promising anticancer agent. This compound has shown a favorable in vitro and in vivo activity profile against neuroblastoma (NB) and glioblastoma (GBM) models by acting as a competitive inhibitor of c-Src tyrosine kinase. Nevertheless, the good antitumor activity of Si306 is associated with sub-optimal aqueous solubility, which might hinder its further development. In this context, drug delivery systems were developed to overcome the poor aqueous solubility obtaining suitable formulations for their in vivo use in the treatment of NB. Si306 was encapsulated in liposomal nanoparticles: i. Stealth liposomes and ii. Immunoliposomes decorated with AntiGD2 monoclonal antibody, which specifically binds GD2 antigen expressed by NB cells. Both liposomal suspensions resulted stable and showed excellent morphological and physio-chemical properties. The liposomal suspensions exhibited increased cytotoxic activity against different NB cell lines; in particular, AntiGD2-decorated liposomes, due to the interaction with the antigen, showed the ability to bind and be internalized in different NB cells and the cellular association increases proportionally with increasing GD2 antigen expression. The pharmacokinetic (PK) and tissue biodistribution (BD) profiles were evaluated by treating healthy male mice intravenously at two dosages of 5 and 25 mg of Si306/kg of body weight. Higher plasma exposure of Si306 was observed when it is delivered by liposomes compared to Si306 administered in free form. Moreover, an immediate distribution of Si306 followed by a concentration decrease in a time-dependent manner was observed in all organs analyzed. An increased concentration of Si306 was observed in the liver, spleen, and lungs when it is delivered by liposomes. A preliminary PK and BD study on NB orthotopic mouse model demonstrated increased tumor uptake of Si306 when it is encapsulated in liposomes compared to drug-free. Finally, in vivo efficacy and survival studies conducted on orthotopic NB mice models revealed the ability of Si306-loaded immunoliposomes to reduce tumor growth and to significantly increase the survival rate. In the second section, gold nanoparticles (AuNPs) conjugated to Si306 were developed to improve its solubility, but also to increase its ability to cross the blood-brain barrier and to have a therapeutic action against (GBM). This section describes the design, the preparation, and the characterization of AuNPs conjugated with Si306. AuNPs-Si306 showed a good loading efficacy (65%), optimal stability in polar media and human plasma, and a suitable morphological profile. Antitumoral activity of AuNPs-Si306 was evaluated in in vitro GBM model, also in combination with radiotherapy (RT). Results demonstrated that AuNPs had a basal radio-sensitization ability and that AuNPs-Si306, when used in combination with RT, was more effective in inhibiting tumor cell growth with respect AuNPs and free Si306. In the third section, Si409, a pyrazolo[3,4-d]pyrimidine derivative, showed the ability to inhibit key members of SFK involved in Diffuse Large B-cell Lymphoma (DLBCL) and to reduce the proliferation of several B-cell tumor cell lines. Also, low cytotoxic activity of Si409 was measured on healthy human peripheral blood mononuclear cells (PBMCs). Si409 showed to be safe by exhibiting a reduction in hERG current but only at concentrations at least 10-fold higher than the median IC50 value recorded in tumor cell lines. PK studies showed high phase II metabolism caused by glucuronide conjugation, which reduces plasma levels and increases the clearance of Si409. Despite the low plasma levels, the treatment with Si409 in ABC-DLBCL xenograft mouse model revealed a considerable volumetric reduction of the tumor mass suggesting an interesting in vivo pharmacological potency of this compound.

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GRECO, CHIARA. "Synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine derivatives active as SGK1, Fyn and Src kinases inhibitors." Doctoral thesis, Università degli studi di Genova, 2020. http://hdl.handle.net/11567/1001600.

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The pathogenesis of many cancers is characterized by mutations, overexpression and dysregulation of protein kinases. As a result, increasing attention has been directed towards the identification of novel kinase inhibitors for cancer therapy. The work performed here focuses on the synthesis of a series of pyrazolo[3,4-d]pyrimidine derivatives as inhibitors of the serine-threonine kinase SGK1, and the tyrosine kinases Fyn and Src. The first set of compounds are analogues of the in house SGK1 inhibitor SI113 which had previously demonstrated anti-cancer activity. In fact SI113 resulted to be active on various cancer cell lines and in an in vivo hepatocellular carcinoma model. The new set of SI113 analogues are characterized by different anilines, ammines and a morpholine group in C4 and are decorated in C6 with polar chains, i.e. ethanolamine, diethanolamine, ethylene glycol and ethylenediamine. The double bond on the N1 side chain which is essential for the activity of compounds toward SGK1, was maintained. The structures of the second set of compounds, instead, are related to the in house Fyn inhibitor SI308. From previously studies on the first generation of Fyn inhibitors, SI308 was reported as the most potent compound, demonstrating both antiproliferative activity on cancer cell lines and the ability to inhibit protein Tau phosphorylation in a cellular model of Alzheimer’s disease. The new generation of SI308 related compounds present a methyl group at the C6 position and on C3 the phenyl ring is either unsubstituted or presents a methyl group in para position. Preliminary screening using enzyme activity assays demonstrates that some of the novel compounds are active and therefore suitable for further study using in vitro models. It is predicted that subsequent in vitro data will aid in the design of future compounds. Furthermore, previous data on another in house compound SI306, which is active on tyrosine kinase Src, reported promising results on an in vivo xenograft model of neuroblastoma. To further study this biological activity, SI306 was re- synthesized and additional experiments were performed on in vitro models. Testing of this compound on MYCN-amplified neuroblastoma cell lines HTLA-230 and SK-N-BE-2C further confirmed the activity of SI306 and provide increased support for the inhibition of Src as a valid approach for neuroblastoma treatment. Finally, further in vitro studies were performed on of the three previously cited in house pyrazolo[3,4-d]pyrimidines, SI306, SI308 and SI113, using patient derived glioblastoma multiforme (GBM) cell lines. This final set of work was undertaken during a visiting research fellowship period and performed in collaboration with the School of Pharmacy at the University of Nottingham (United Kingdom). Kinase inhibitor activity has been evaluated on series of patient derived GBM cell lines isolated from both the central tumor core (GCE28) and from the invasive margin of the tumor (GIN28 and GIN8). The use of such phenotypically relevant in vitro models represents an important step for GBM drug development and screening. The results gathered using these relevant cell models further demonstrate the anti-cancer activity of the pyrazolo[3,4-d]pyrimidines compounds. Moreover, investigating the compounds in combination with one another reveals that synergy can be achieved and this finding has additional implications for potentially overcoming GBM drug resistance. Additionally, to overcome the low water solubility of our pyrazolo[3,4-d]pyrimidines compounds, formulations of the lead compounds (SI306, SI308 and SI113) were prepared using miniaturized screening process based on inkjet printing technology6. The observed activity of our compounds in vitro taken together with their successful formulation highlight that our kinase inhibitors are attractive candidates for the treatment of GBM.

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Gormen, Meral. "Synthesis Of Ferrocenyl Substituted Pyrazoles." Master's thesis, METU, 2005. http://etd.lib.metu.edu.tr/upload/3/12606358/index.pdf.

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Pyrazoles have been studied for over a century as an important class of heterocyclic compounds and continue to attract considerable interest due to the broad range of biological activities they possess. The incorporation of the essential structural features of pyrazoles with a ferrocene moiety could provide new derivatives with unexpected and/or enhanced biological activities since several ferrocene derivatives have already been shown to be active against a number of tumors. For this reason, we investigated the synthesis of ferrocenyl-substituted pyrazoles, such as 1-alkyl/aryl-5-ferrocenylpyrazoles, by employing the reaction between (2-formyl-1-chlorovinyl)ferrocene and hydrazine derivatives. Although this reaction is known, it was not studied in much detail and the low yields of ferrocenyl pyrazoles were obtained. Thus, we have reinvestigated this reaction and improved the yields of pyrazoles by optimizing the reaction conditions. (2-Formyl-1-chloro vinyl)ferrocene was first reacted with the excess amount (3 equivalents) of hydrazine derivative at 25 0C in dioxane under argon for 2 hours, and the resulting mixture was then heated at 100 0C for 6 hours in the same solvent. Under our optimized conditions, these reactions afforded 1-alkyl/aryl-5-ferrocenylpyrazole derivatives in moderate to good yields as a single or major product of the reaction. In some cases, 1-alkyl/aryl-3-ferrocenylpyrazole derivatives resulted from these reactions as very minor products.

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Pasin, Juliana Saibt Martins. "Atividade antipirética e antiinflamatória de derivados 5-trifluormetil-4,5-diidro-1H-1-carboxiamida pirazol em ratos." reponame:Biblioteca Digital de Teses e Dissertações da UFRGS, 2010. http://hdl.handle.net/10183/28004.

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A febre é um aumento regulado da temperatura corporal central, caracterizada por uma alteração no centro termorregulatório, a qual resulta da interação entre o sistema nervoso central e o imunológico. Enquanto a febre caracteriza lesão celular, infecção e inflamação, ela tem sido considerada o mais importante componente da resposta de fase aguda. Embora existam evidências de que a febre aumenta a defesa do hospedeiro, alguns estudos têm sugerido que o aumento da temperatura central a níveis febris pode ser prejudicial. Portanto, nas situações clínicas nas quais os riscos associados com a febre superam os benefícios, o tratamento antipirético é formalmente indicado. Os derivados pirazolínicos constituem um importante grupo de compostos orgânicos que têm sido extensivamente estudados devido às suas inúmeras atividades biológicas, que incluem atividade antipirética. Recentemente uma série de derivados pirazolínicos inéditos foi avaliada quanto à atividade antiedematogênica e antinociceptiva em camundongos. Estes compostos causam antinocicepção no teste da formalina e no modelo de artrite induzida por adjuvante de Freund, bem como diminuem o edema induzido por carragenina. Dados os efeitos antiinflamatórios descritos para estes compostos, o objetivo do estudo foi investigar o efeito de oito derivados 5-trifluormetil-4,5-diidro- 1H-1-pirazol-1-carboxiamida (TFDPs) sobre a temperatura corporal basal, a febre induzida por S. cerevisiae (0.135 g/Kg, i.p.) e a inflamação peritoneal em ratos Wistar machos de 28 dias de idade. Somente os compostos 3Et- e 3Pr-TFDP (140 e 200 μmol/kg respectivamente, s.c., 4 h após a injeção do S. cerevisiae) atenuaram a febre em 61.0% e 82.4%, respectivamente. Estes dois compostos foram selecionados para a investigação dos mecanismos de ação. Os efeitos sobre a atividade da ciclooxigenase-1 e -2 (COX-1 e COX-2), a oxidação in vitro do 1,1-difenil-2- picrilhidrazil (DPPH), os níveis de TNF-a e IL-1b e influxo de leucócitos na cavidade peritoneal dos ratos injetados com S. cerevisiae foram determinados. Enquanto 3Et- e 3Pr-TFDP não alteraram o aumento nos níveis de TNF-a e IL-1b induzido por S. cerevisiae, o derivado 3Et- TFDP causou uma redução de 42% na contagem de leucócitos na cavidade peritoneal. 3Et- e 3Pr-TFDP não alteraram a atividade da COX-1 e COX-2 in vitro, mas apresentaram atividade antioxidante no ensaio do DPPH, com CI50 de 39.3 (25.0-62.0) mM e 162.9 (135.6-195.7) mM, respectivamente. Em outro grupo de experimentos, foi avaliado o efeito do pré-tratamento dos animais com os compostos 3Et- e 3Pr-TFDP sobre a inflamação peritoneal induzida por S.cerevisiae em ratos. O pré-tratamento com 3Et-TFDP (140 μmol/kg, 5 mL/Kg, s.c.) preveniu significativamente o aumento no influxo de leucócitos, a permeabilidade vascular peritoneal e a atividade da mieloperoxidase (MPO), mas não teve efeito sobre os níveis de TNF-a e IL-1b. Por outro lado, 3Pr-TFDP (200 μmol/kg, 5 mL/Kg, s.c.) não apresentou efeito sobre nenhum desses parâmetros inflamatórios. O presente estudo descreve dois novos derivados pirazolínicos com atividade antipirética, cujos mecanismos de ação não envolvem inibição da COX ou inibição da liberação de citocinas pirogênicas. Além disso, foi demonstrado que o composto 3Et-TFDP apresenta potencial antiinflamatório, atuando sobre o influxo de leucócitos, permeabilidade vascular peritoneal e aumento da atividade da MPO induzidos por S. cerevisiae. Em conjunto, nossos dados sugerem que os derivados pirazolínicos 3Et- e 3Pr-TFDP parecem ser compostos antipiréticos e antiinflamatórios promissores.
Fever is a regulated increase of body core temperature characterized by a raised thermoregulatory set point, which results from the interaction of the central nervous and immune systems. While fever is a hallmark of injury, infection and inflammation, it has also been considered the most important component of acute-phase response. Although there is evidence supporting the idea that fever enhances host defenses, some studies have suggested that raising core temperature to the febrile range may be harmful. Therefore, in the clinical situations in which fever-associated risks outweigh benefits, antipyretic treatment is formally indicated. Pyrazoles constitute an important group of organic compounds that have been extensively studied due to their numerous biological activities. Recently a series of pyrazole derivatives have been screened for antinociceptive and antiedematogenic activity in mice. These compounds cause antinociception in the formalin test and in the Freund's adjuvant (CFA) animal model of arthritis and decrease carrageenin-induced edema. Given the effects reported for these compounds, we decided to investigate the effect of eight 5-hydroxy-5-trifluoromethyl-4,5-dihydro- 1H-1-carboxyamidepyrazoles (TFDPs) on body temperature, baker´s yeast-induced fever and peritoneal inflammation in 28 days-old male Wistar rats. Only 3ethyl- and 3propyl-TFDP (140 and 200 μmol/kg, respectively, s.c., 4 h after S. cerevisiae injection) attenuated baker’s yeastinduced fever by 61.0% and 82.4%, respectively. These two effective antipyretics were selected to investigate the mechanisms of action. The effects on cyclooxygenase-1 and -2 (COX-1 and COX-2) activities, on 1,1-diphenyl-2-picrylhydrazyl (DPPH) oxidation in vitro, on TNF-a and IL- 1b levels and on leukocyte counts in the washes of peritoneal cavities of rats injected with baker’s yeast were determined. While 3ethyl- and 3propyl-TFDP did not reduce baker’s yeastinduced increases of IL-1 or TNF- levels, 3ethyl-TFDP caused a 42% reduction in peritoneal leukocyte count. 3ethyl- and 3propyl-TFDP did not alter COX-1 and COX-2 activities in vitro, but presented antioxidant activity in the DPPH assay with an IC50 of 39.3 (25.0-62.0) mM and 162.9 (135.6-195.7) mM, respectively. In a other set of the experiments, we investigate the effect of 3- ethyl- and 3-propyl-5-hydroxy-5-trifluoromethyl-4,5-dihydro-1H-1-carboxyamidepyrazoles on S.cerevisiae-induced peritoneal inflammation in rats. Pre-treatment with 3ethyl-TFDP (140 μmol/kg, 5 mL/Kg) significantly prevented S.cerevisiae-induced increase in leukocyte influx, peritoneal vascular permeability and myeloperoxidase activity, but had no effect on TNF-a and IL-1b levels. On the other hand, 3propyl-TFDP (200 μmol/kg, 5 mL/Kg) had no effect on these inflammatory parameters. The current study describes two novel antipyretic pyrazole derivatives, whose mechanisms of action do not involve the classic inhibition of the COX pathway or pyrogenic cytokine release. In addition, it is shown that 3ethyl-TFDP presents antiinflammatory potential, since it reduces leukocyte influx, peritoneal vascular permeability and MPO activity. Taken together, our data suggest that the pyrazole derivatives 3ethyl- and 3propyl-TFDP seems a promising antipyretic and anti-inflammatory compounds.

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Crotti, Simone. "Computer assisted synthesis and in-vitro cytotoxic evaluation of new pyrazole-fused isoquinolinoquinones derivatives as PI3K receptor antagonist with promising antitumoral activity." Master's thesis, Alma Mater Studiorum - Università di Bologna, 2016. http://amslaurea.unibo.it/11206/.

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The importance of pyrazole and isoquinoline-5,8-dione scaffolds in medical chemistry is underlined by the high number of drugs currently on trading that contains these active ingredients. Due to their cytotoxic capability, the interest of medicinal chemists in these heterocyclic rings has grown exponentially especially, for cancer therapy. In this project, the first synthesis of pyrazole-fused isoquinoline-5,8-diones has been developed. 1,3-Dipolar cycloaddition followed by oxidative aromatization, established by our research group, has been employed. Screening of reaction conditions and characterization studies about the regioselectivity have been successfully performed. A remote control of regioselectivity, to achieve the two possible regioisomers has been accomplished. Through Molecular Docking studies, Structure-Activity relationship of differently substituted scaffolds containing our central core proved that a family of PI3K inhibitors have been discovered. Finally, in order to verify the promising antitumor activity, a first test of cell viability in vitro on T98G cell line of a solid brain tumor, the Glioblastoma Multiforme, showed cytotoxic inhibition comparable to currently trade anticancer drugs.

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Books on the topic "Pyrazolone derivatives"

1

Wiley, Richard H., and Paul F. Wiley. Pyrazolones, Pyrazolidones, and Derivatives. Wiley & Sons, Incorporated, John, 2009.

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Wiley, Richard H., and Paul F. Wiley. Pyrazolones, Pyrazolidones, and Derivatives. Wiley & Sons, Limited, John, 2007.

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Wiley, Richard H., and Paul F. Wiley. Chemistry of Heterocyclic Compounds, Pyrazolones, Pyrazolidones, and Derivatives. Wiley & Sons, Incorporated, John, 2008.

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Book chapters on the topic "Pyrazolone derivatives"

1

Niedenzu, Kurt, and Swiatoslaw Trofimenko. "Pyrazole derivatives of boron." In Topics in Current Chemistry, 1–37. Berlin, Heidelberg: Springer Berlin Heidelberg, 1986. http://dx.doi.org/10.1007/3-540-15811-1_1.

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Kabi, Arup K., Sattu Sravani, Raghuram Gujjarappa, Aakriti Garg, Nagaraju Vodnala, Ujjawal Tyagi, Dhananjaya Kaldhi, Virender Singh, Sreya Gupta, and Chandi C. Malakar. "Overview on Biological Activities of Pyrazole Derivatives." In Materials Horizons: From Nature to Nanomaterials, 229–306. Singapore: Springer Singapore, 2022. http://dx.doi.org/10.1007/978-981-16-8399-2_7.

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Kang, Hyo Sim, Sun Wha Oh, and Young Soo Kang. "Comparison of Optical Properties of Pyrazoline Derivative Nanoparticles." In Solid State Phenomena, 39–42. Stafa: Trans Tech Publications Ltd., 2007. http://dx.doi.org/10.4028/3-908451-27-2.39.

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Swarts, Steven G., Mei Zhang, Liangjie Yin, Chaomei Liu, Yeping Tian, Yongbing Cao, Michael Swarts, et al. "Antioxidant Properties of Select Radiation Mitigators Based on Semicarbazone and Pyrazole Derivatives of Curcumin." In Oxygen Transport to Tissue XXXII, 291–97. Boston, MA: Springer US, 2011. http://dx.doi.org/10.1007/978-1-4419-7756-4_39.

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Safi, Zaki S., Mohammed H. Rida, and Hassan M. Tamous. "Application of Density Functional Theory to Study the Anticorrosive Effects of Some Pyrazole Derivatives." In Corrosion Science, 107–36. New York: Apple Academic Press, 2023. http://dx.doi.org/10.1201/9781003328513-4.

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Caravatti, G., J. Brüggen, E. Buchdunger, R. Cozens, P. Furet, N. Lydon, T. O'Reilly, and P. Traxler. "Pyrrolo[2,3-d]pyrimidine and Pyrazolo[3,4-d]pyrimidine Derivatives as Selective Inhibitors of the EGF Receptor Tyrosine Kinase." In Anticancer Agents, 231–44. Washington, DC: American Chemical Society, 2001. http://dx.doi.org/10.1021/bk-2001-0796.ch014.

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Angulwar, Jaman A. "Multicomponent Synthesis of 2-Substituted Derivatives of 6-Amino-5-Cyano-1,4-Dihydro-3-Methyl-1,4-Diphenylpyrano-[2,3-C]-Pyrazole Using Knoevenagel and Michael Addition." In Modern Green Chemistry and Heterocyclic Compounds, 113–36. Series statement: Innovations in physical chemistry: monographic series: Apple Academic Press, 2020. http://dx.doi.org/10.1201/9780367276942-4.

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Niedenzu, Kurt, and Swiatoslaw Trofimenko. "Pyrazole Derivatives of Boron." In Structural Chemistry of Boron and Silicon, 1–38. De Gruyter, 1985. http://dx.doi.org/10.1515/9783112620588-001.

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Nandurkar, Deweshri, Kishor Danao, Vijayshri Rokde, Ruchi Shivhare, and Ujwala Mahajan. "Pyrazole Scaffold: Strategies toward the Synthesis and Their Applications." In Strategies Towards the Synthesis of Heterocycles and Their Applications [Working Title]. IntechOpen, 2022. http://dx.doi.org/10.5772/intechopen.108764.

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Pyrazoles have a wide range of applications in medicinal chemistry, drug discovery, agrochemistry, coordination chemistry, and organometallic chemistry. Their popularity has skyrocketed since the early 1990s. Basically, Pyrazole (C3H3N2H) is a simple doubly unsaturated five membered heterocyclic aromatic ring molecule comprising two nitrogen (N) atoms at positions 1- and 2- and three carbon (C) atoms. Pyrazole nucleus is synthesized with various strategies such as multicomponent approach, dipolar cycloadditions, cyclocondensation of hydrazine with carbonyl system, using heterocyclic system and multicomponent approach. A special emphasis is placed on a thorough examination of response processes. Furthermore, the reasons for the increasing popularity of pyrazoles in several fields of science are examined. Pyrazoles have recently been the focus of many techniques, mostly because of how frequently they are used as scaffolds in the synthesis of bioactive chemicals and reactions in various media. The goal of this chapter is to discuss the current developments in synthetic techniques and biological activity related to pyrazole derivatives. The many pharmacological functions of the pyrazole moiety and different synthesis techniques were discussed. This chapter has summarized novel strategies and wide applications of pyrazole scaffold.

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S. Laitonjam, Warjeet, and Nimalini Moirangthem. "Construction of Biologically Active Five- and Six-Membered Fused Ring Pyrimidine Derivatives from 1,3-Diarylthiobarbituric Acids (DTBA)." In Strategies Towards the Synthesis of Heterocycles and Their Applications [Working Title]. IntechOpen, 2022. http://dx.doi.org/10.5772/intechopen.108842.

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Several derivatives of fused pyrimidines were synthesized in maximum yields by using the respective condensation products, namely, 5-ethoxymethylene-1,3-diaryl-2-thiobarbituric acids and 5-phenyl-methylene-1,3-diaryl-2-thiobarbituric acids, which can be obtained from 1,3-diarylthiobarbituric acids (DTBA). These condensation products possessing three electrophilic centres could undergo cyclocondensation with various binucleophiles to give various fused heterocycles of pyrimidine derivatives, such as pyrazolo[3,4-d]pyrimidine-6-thiones, 5,7-diaryl-4-oxo-isoxazolo[5,4-d]pyrimidine-6-thiones, 5-oxo-pyrimido[4,5-d]pyrimidine-7-thiones, 2-thioxo-pyrano[2,3-d]pyrimidine-4-ones, pyrido[2,3-d]pyrimidines, quinazoline-4-oxo-2-thiones.

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Conference papers on the topic "Pyrazolone derivatives"

1

Pratiwi, S., and A. H. Cahyana. "Synthesis of pyrazolone derivatives compound using nanomagnetic Fe3O4 catalyst from waste cooking oil and iron rust and antioxidant activity test." In PROCEEDINGS OF THE 6TH INTERNATIONAL SYMPOSIUM ON CURRENT PROGRESS IN MATHEMATICS AND SCIENCES 2020 (ISCPMS 2020). AIP Publishing, 2021. http://dx.doi.org/10.1063/5.0059243.

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Muškinja, Jovana M., Jelena S. Katanić Stanković, and Zoran R. Ratković. "SYNTHESIS AND ANTIOXIDANT ACTIVITY OF SOME NEW SULFONAMIDE DERIVATIVES." In 1st INTERNATIONAL Conference on Chemo and BioInformatics. Institute for Information Technologies, University of Kragujevac, 2021. http://dx.doi.org/10.46793/iccbi21.351m.

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Sulfonamide derivatives are a very important class of compounds with pronounced biological activities and, for this reason, they have very useful pharmaceutical applications. They are the basis of several groups of drugs and are known as sulfa-drugs. From this point of view, the present study focuses on the synthesis of some novel structural hybrids incorporating two very important groups, sulfonamide, and pyrazoline. The new sulfonamide-based pyrazolines were synthesized in very good yields. The structures of the sulfonamide compounds were confirmed by IR and NMR methods. Synthesized compounds were tested for their antioxidant activities using two different methods, DPPH radical and ABTS radical cation scavenging assays. The results showed relatively good in vitro antioxidant activity.

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Gondek, E., J. Niziol, A. Danel, and J. Sanetra. "Photovoltaic effect based on pyrazole derivatives." In 2009 3rd ICTON Mediterranean Winter Conference (ICTON-MW 2009). IEEE, 2009. http://dx.doi.org/10.1109/ictonmw.2009.5385546.

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Janardhana, K., V. Ravindrachary, P. C. Rajesh Kumar, Yogisha, Bhoja Poojary, K. B. Manjunatha, and Ismayil. "Third Order Optical Nonlinearity of a Pyrazoline Derivative." In THE 10TH ASIAN INTERNATIONAL CONFERENCE ON FLUID MACHINERY. American Institute of Physics, 2011. http://dx.doi.org/10.1063/1.3606354.

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Krunić, Mihajlo J., Jelena Z. Penjišević, Slađana Kostić-Rajačić, Vladimir B. Šukalović, Deana B. Andrić, and Ivana I. Jevtić. "Pyrazole/tacrine derivatives as potential cholinesterase inhibitors." In 2nd International Conference on Chemo and Bioinformatics. Institute for Information Technologies, University of Kragujevac, 2023. http://dx.doi.org/10.46793/iccbi23.567k.

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Two new tacrine/pyrazole conjugates were designed, synthesized, and pharmacologically evaluated for their inhibitory activity toward acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). A scalable and cost-efficient synthetic route was developed, and key reaction steps for the synthesis of compounds 4a,b were nucleophilic substitution of α-aroylketene dithioacetals with tacrine intermediates, followed by cyclocondensation of respective N,S-acetals with hydrazine hydrate. The preliminary pharmacological evaluation revealed high inhibitory activities of 4a,b toward AChE (180 and 259 nM, respectively) and BuChE (51 and 95 nM, respectively) as compared with known inhibitor, tacrine. Overall, both compounds were more efficient BuChE inhibitors while 4a, with a shorter linker connecting tacrine and phenylpyrazole moieties, showed higher inhibitory activity toward both enzymes. Molecular docking analysis strongly corroborated pharmacological results since both compounds interacted favorably with target enzymes. Calculated pharmacokinetic properties (absorption, distribution, metabolism, and excretion (ADME) showed that 4a,b obey Lipinski’s rule of druglikeness and are promising lead compounds for the development of new drug candidates.

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Liu, Xiaobo, Shan Xu, and Yinhua Xiong. "Synthesis of 3-phenyl-1H-pyrazole Derivatives." In 2016 7th International Conference on Education, Management, Computer and Medicine (EMCM 2016). Paris, France: Atlantis Press, 2017. http://dx.doi.org/10.2991/emcm-16.2017.117.

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Cin, Gunseli Turgut, Seda Demirel Topel, Neslihan Nohut Maslakci, Esin Eren, and Aysegul Uygun Oksuz. "Plasma modified chitosan/N-acetyl-2-pyrazoline derivative nanofibers." In 2015 IEEE International Conference on Plasma Sciences (ICOPS). IEEE, 2015. http://dx.doi.org/10.1109/plasma.2015.7179648.

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Priyanka, S., S. Sivapriya, D. Sivakumar, M. Gopalakrishnan, M. Seenivasan, and H. Manikandan. "Synthesis and DFT calculation of novel pyrazole derivatives." In INTERNATIONAL CONFERENCE ON RECENT TRENDS IN APPLIED MATHEMATICAL SCIENCES (ICRTAMS-2020). AIP Publishing, 2021. http://dx.doi.org/10.1063/5.0063016.

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Adel, Mariam H., and Hiba H. Ibraheem. "Synthesis, molecular docking, and anti-tumor activity of pyrazole derivatives." In FIFTH INTERNATIONAL CONFERENCE ON APPLIED SCIENCES: ICAS2023. AIP Publishing, 2024. http://dx.doi.org/10.1063/5.0210692.

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Karpinski, Pawel, Lech Sznitko, Adam Szukalski, Jaroslaw Mysliwiec, Andrzej Miniewicz, Patrick Ferrand, Herve Rigneault, and Sophie Brasselet. "Second harmonic generation and two-photon excitation fluorescence from individual nanocrystals of pyrazoline derivatives." In 2013 Conference on Lasers & Electro-Optics Europe & International Quantum Electronics Conference CLEO EUROPE/IQEC. IEEE, 2013. http://dx.doi.org/10.1109/cleoe-iqec.2013.6801794.

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