Antileishmanial and Antitrypanosomal Activity of Synthesized Hydrazones, Pyrazoles, Pyrazolo[1,5-a]-Pyrimidines and Pyrazolo[3,4-b]- Pyridine

Figarella, Katherine; Marsiccobetre, Sabrina; Galindo-Castro, Iván; Urdaneta, Neudo; Herrera, Julio; Canudas, Nieves; Galarraga, Elier

doi:10.2174/1573407213666170405121810

Cited by 14 publications

(8 citation statements)

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“…Pyrazole derivatives were prepared and tested for their in vitro antiparasitic activity against promastigotes of Leishmania mexicana (Bel 21) and epimastigotes of Trypanosoma cruzi (DM28) using a modified MTT assay. Only 474 displayed selectivity on L. mexicana with a SI of 3, however, the IC 50 obtained here was around four times higher (25 μM) [ 371 ]. A new series of pyrazole derivatives were prepared and tested in vitro for their anti-leishmanial activity.…”

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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“…Pyrazole is a five‐membered heterocyclic compound containing two nitrogen atoms in positions 1 and 2. Various pharmacological and biological activities have been reported for pyrazoles, including sodium channel blocker, [1] antiglaucoma, [2] antitubercular, [3] antiviral, [4] anti‐inflammatory, [5] antioxidant, [6] anticancer, [7–14] antialzheimer, [15–19] antidiabetic, [20–23] antimalarial, [24–26] antiparkinson, [27–29] antileishmanial and antitrypanosomal [30] . For example, compound 1 as an antialzheimer, [15] compound 2 as an antidiabetic, [20] fezolamine ( 3 ) as an antidepressant drug, [31] lozanolac ( 4 ) as an anti‐inflammatory, [32] rimonabant ( 5 ) as a antiobesity drug [33] and difenamizole ( 6 ) as an analgesic drug [34] are known ( Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Preparation of New Spiropyrazole, Pyrazole and Hydantoin Derivatives and Investigation of Their Antioxidant and Antibacterial Activities.

Ghasempour

Asghari

Tajbakhsh

et al. 2021

Chemistry & Biodiversity

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In this study, the synthesis of new spiropyrazoles, pyrazole and hydantoin heterocycles is reported by three component reactions of parabanic acids, hydrazine derivatives, and phenacyl bromides in the presence of triphenylphosphine as a nucleophile and triethylamine as a base in good to high yields (69–91 %). Evaluation of the synthesized compounds revealed a good to excellent antioxidant activities (37.6–96.2 %) using DPPH inhibitory potency. Among these compounds, hydantoin derivatives displayed higher antioxidant activities (93.7–96.2 %) comparing with spiropyrazoles and pyrazoles. The obtained results showed that Cl and Br substituents on the phenyl ring increased antioxidant activities of the related heterocycles. The antibacterial activities of the synthesized compounds were examined against two Gram‐negative (Escherichia coli and Pseudomonas aeruginosa) and two Gram‐positive (Staphylococcus aureus and Bacillus subtilis) bacteria. Among the synthesized heterocycles, 2‐[1,3‐dimethyl‐2,5‐dioxo‐4‐(2‐oxo‐2‐phenylethyl)imidazolidin‐4‐yl]hydrazine‐1‐carbothioamide exhibited the excellent antibacterial activity against both Gram‐positive and Gram‐negative bacteria.

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“…The condensation of 6-substituted 3-formylchromones 156 with equimolar amounts of aromatic primary hydrazines in refluxing THF occurs through 1,2-addition reaction at the formyl group to afford the respective hydrazones 157 ( Scheme 54 ). On the other hand, using prolonged heating, the reaction evolved to the formation of 1-aryl-4-(2-hydroxybenzoyl)pyrazoles 158 ( Scheme 54 ), via 1,4-addition reaction with pyrone ring-opening and subsequent recyclization and proton transfer mechanism [ 108 , 109 ]. Both compounds 157 and 158 were screened for their cytotoxic effect against brine shrimps ( Artemia salina ), presenting IC 50 values of 83–262 μM, considerably higher than the positive control podophyllotoxin (IC 50 = 5.8 μM).…”

Section: Miscellaneousmentioning

confidence: 99%

“…The IC 50 values found were 6–53 μM for L. mexicana and 4–174 μM for T. cruzi, higher than the positive control miltefosine (IC 50 values of 4.7 μM for L. mexicana and 2.3 μM for T. cruzi ). The most promising compound against both strains was derivative 157 (R 1 = H, R 2 = 2,4-(NO 2 ) 2 ), non-substituted on the chromone unit and bearing a 2,4-dinitrophenyl moiety linked to the hydrazone [ 109 ].…”

Section: Miscellaneousmentioning

confidence: 99%

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Synthesis of Chromone-Related Pyrazole Compounds

Santos

Silva

2017

Molecules

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Chromones, six-membered oxygen heterocycles, and pyrazoles, five-membered two-adjacent-nitrogen-containing heterocycles, represent two important classes of biologically active compounds. Certain derivatives of these scaffolds play an important role in medicinal chemistry and have been extensively used as versatile building blocks in organic synthesis. In this context, we will discuss the most relevant advances on the chemistry that involves both chromone and pyrazole rings. The methods reviewed include the synthesis of chromone-pyrazole dyads, synthesis of chromone-pyrazole-fused compounds, and chromones as starting materials in the synthesis of 3(5)-(2-hydroxyaryl)pyrazoles, among others. This review will cover the literature on the chromone and pyrazole dual chemistry and their outcomes in the 21st century.

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Antileishmanial and Antitrypanosomal Activity of Synthesized Hydrazones, Pyrazoles, Pyrazolo[1,5-a]-Pyrimidines and Pyrazolo[3,4-b]- Pyridine

Cited by 14 publications

References 0 publications

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Preparation of New Spiropyrazole, Pyrazole and Hydantoin Derivatives and Investigation of Their Antioxidant and Antibacterial Activities.

Synthesis of Chromone-Related Pyrazole Compounds

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