Synthesis and evaluation against Leishmania amazonensis of novel pyrazolo[3,4- d ]pyridazinone- N -acylhydrazone-(bi)thiophene hybrids

Jacomini, Andrey P.; Silva, Michael J. V.; Silva, Raí G. M.; Gonçalves, Davana S.; Volpato, Hélito; Basso, Ernani A.; Paula, Fávero Reisdorfer; Nakamura, Celso Vataru; Sarragiotto, María Helena; Rosa, Fernanda A.

doi:10.1016/j.ejmech.2016.08.048

Cited by 53 publications

(37 citation statements)

References 25 publications

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“…A new series of pyrazolo[3,4- d ]pyridazin-7-one derivatives were synthesised and evaluated for their in vitro anti-leishmanial activity against Leishmania amazonensis promastigote and axenic amastigote forms. The results showed that compound 469 exhibit better anti-leishmanial activity with IC 50 3.63 and 2.32 μM, against the promastigote form and axenic amastigote form, respectively [ 366 ].…”

Section: Pharmacological Activitiesmentioning

confidence: 99%

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

et al. 2018

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Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.

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Section: Pharmacological Activitiesmentioning

confidence: 99%

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

et al. 2018

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“…After performing the in silico structure-based experiments, eight ( 1 ( a - b ) - 4 ( a - b ) ) promising molecules have been selected for further studies. The physicochemical descriptors, like molecular weight (MW), hydrogen bond donor (HBD), hydrogen bond acceptor (HBA), the logarithmic partition coefficient in octanol/water, and logP (lipophilicity) have been analyzed to evaluate the drug-like properties of the molecules ( Jacomini et al, 2016 ). In silico ADMET (Adsorption, Distribution, Metabolism, Excretion, and Toxicity) predictions of all molecules are evaluated using DS 2.5 software to support the biological results.…”

Section: Methodsmentioning

confidence: 99%

Alkylated benzimidazoles: Design, synthesis, docking, DFT analysis, ADMET property, molecular dynamics and activity against HIV and YFV

Srivastava

Gupta

Naaz

et al. 2020

Computational Biology and Chemistry

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“…A well devoid of the studied compounds as a negative control was included in the study. Concentrations were tested in triplicates, incubated at 24 °C and evaluated after 24, 48 and 72 h. Afterwards, hemocytometer lamella and 0.4% tripan blue dye were used for observing results and counting the number of promastigotes ( 16 17 18 ).…”

Section: Methodsmentioning

confidence: 99%

Synthesis and antileishmanial activity of antimony (V) complexes of hydroxypyranone and hydroxypyridinone ligands

et al. 2018

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A novel series of antimony (V) complexes with the hydroxypyranone and hydroxypyridinone ligands were synthesized and characterized by 1HNMR, FT-IR and electron spin ionization mass spectroscopic (ESI-MS) techniques. The synthesis process involved protection of hydroxyl group followed by the reaction of the intermediate with primary amines and finally deprotection. All compounds were evaluated for in vitro activities against the amastigote and promastigote forms of Leishmania major. Most of the synthesized compounds exhibited good antileishmanial activity against both forms of L. major. IC50 values of the most active compounds; 9d, 9d and 9e, after 24, 48 and 72 h against amastigote model were 15, 12.5 and 5.5 μg/mL, respectively. 9e, 11 and 9e inhibited the promastigote form of parasite after 24, 48 and 72 h with IC50 values of 10, 2 and 1 μg/mL, respectively.

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Synthesis and evaluation against Leishmania amazonensis of novel pyrazolo[3,4- d ]pyridazinone- N -acylhydrazone-(bi)thiophene hybrids

Cited by 53 publications

References 25 publications

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Alkylated benzimidazoles: Design, synthesis, docking, DFT analysis, ADMET property, molecular dynamics and activity against HIV and YFV

Synthesis and antileishmanial activity of antimony (V) complexes of hydroxypyranone and hydroxypyridinone ligands

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