Synthesis and antimalarial potential of some novel quinoline-pyrazolopyridine derivatives

Saini, Deepika; Jain, Sandeep; Kumar, Ajay; Jain, Neelam

doi:10.17179/excli2016-677

Cited by 3 publications

(2 citation statements)

References 12 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In agreement with the current research, Saini et al 49 studied the antimalarial potential of quinoline-pyrazolo pyridine derivatives. Mosquitocidal results revealed that the synthesized 4,7-dichloroquinoline was highly toxic to developmental stages of malarial and dengue vectors providing LC 50 values ranging from 4.408 µM/mL (larva I) to 7.958 µM/mL (pupa) for the chosen malaria vector and 5.016 µM/mL (larva I) to 10.669 µM/mL (pupa) for the dengue vector (Table 2 ).…”

Section: Resultssupporting

confidence: 87%

Synthesis of new series of quinoline derivatives with insecticidal effects on larval vectors of malaria and dengue diseases

Murugan

Panneerselvam

Subramaniam

et al. 2022

Sci Rep

View full text Add to dashboard Cite

Mosquito borne diseases are on the rise because of their fast spread worldwide and the lack of effective treatments. Here we are focusing on the development of a novel anti-malarial and virucidal agent with biocidal effects also on its vectors. We have synthesized a new quinoline (4,7-dichloroquinoline) derivative which showed significant larvicidal and pupicidal properties against a malarial and a dengue vector and a lethal toxicity ranging from 4.408 µM/mL (first instar larvae) to 7.958 µM/mL (pupal populations) for Anopheles stephensi and 5.016 µM/mL (larva 1) to 10.669 µM/mL (pupae) for Aedes aegypti. In-vitro antiplasmodial efficacy of 4,7-dichloroquinoline revealed a significant growth inhibition of both sensitive strains of Plasmodium falciparum with IC50 values of 6.7 nM (CQ-s) and 8.5 nM (CQ-r). Chloroquine IC50 values, as control, were 23 nM (CQ-s), and 27.5 nM (CQ-r). In vivo antiplasmodial studies with P. falciparum infected mice showed an effect of 4,7-dichloroquinoline compared to chloroquine. The quinoline compound showed significant activity against the viral pathogen serotype 2 (DENV-2). In vitro conditions and the purified quinoline exhibited insignificant toxicity on the host system up to 100 µM/mL. Overall, 4,7-dichloroquinoline could provide a good anti-vectorial and anti-malarial agent.

show abstract

Section: Resultssupporting

confidence: 87%

Synthesis of new series of quinoline derivatives with insecticidal effects on larval vectors of malaria and dengue diseases

Murugan

Panneerselvam

Subramaniam

et al. 2022

Sci Rep

View full text Add to dashboard Cite

show abstract

“…[21] Furthermore, the pyrazole core is present in several useful clinical molecules with varied therapeutic activities [22][23][24][25][26][27] (Figure 1). On the other hand, cyanopyridine skeleton is considered to be of great value in medicinal chemistry due to their various biological applications, particularly PIM-1 kinase inhibitory, [28] antidepressant, [29] anticancer, [30][31][32][33] anti-inflammatory, [34] antiviral, [35] anti-Alzheimer, [36] antimalarial, [37] and antimicrobial. [38] We have obtained promising anticancer activities from heterocyclic compounds that we have synthesized in recent years.…”

mentioning

confidence: 99%

Preparation, DFT calculations, docking studies, antioxidant, and anticancer properties of new pyrazole and pyridine derivatives

Zebbiche

Şekerci

Boulebd

et al. 2022

J Biochem & Molecular Tox

View full text Add to dashboard Cite

Seven novel pyrazole derivatives (4a-g) and four novel starting compounds incorporating substituted pyridine moieties were synthesized successfully. Cell viability assay for the tested compounds was performed, and the inhibitory concentrationlogarithmic 50 (LogIC 50 ) values of the compounds were calculated after a 24-h treatment. Four of the examined compounds (3d, 3g, 4f, and 4g) showed comparable cytotoxic activity against CaCo-2 compared to the standard drug docetaxel at 0.1 and 1 μM concentrations.Although the LogIC 50 of docetaxel was −0.678 μM for CaCo-2 cells at 24 h, the LogIC 50 values of compounds were −0.794, −0.567, −0.657, and −0.498 μM, respectively. Five of the compounds (2d, 2g, 3d, 3g, and 4e) showed comparable cytotoxic activity against MCF-7 at 0.1 μM concentration compared to docetaxel (p < 0.05). Docking studies revealed the compounds have a good affinity to the active site of the human topoisomerase II β enzyme. The antioxidant capacities of all compounds were determined using both 1,1-diphenyl-2-picrylhydrazyl and metal chelation methods. Although the compounds did not show significant antioxidant activity, relatively effective are compounds 3c, 3d, and 3g, which are hydrazine derivatives with approximately 50% antioxidant activity of standard antioxidants at concentrations of 62.5 and 125 μg/ml.

show abstract

Synthesis, Characterization and Antimalarial–antimicrobial Studies of Some Novel Derivatives of Chloroquinoline Based Pyrazoles

Sonker¹,

Pathak²

2018

IND. DRU.

View full text Add to dashboard Cite

The prime aim of the present investigation was to synthesize a series of novel derivatives of pyrazole based quinolines by the reaction of substituted chalcones and characterized them by their physical and spectral data. All the compounds were confirmed by TLC and melting point. The structures of the synthesized compounds have been established on the basis of IR, 1 H NMR, EIMS spectral analysis and elemental analysis. The synthesized target compounds were screened for their anti-malarial activity using Vero cell line (C1008; Monkey kidney fibroblast) against Plasmodium falciparum (3D7 strain) with the standard and SI was measured by using IC50 and CC50 of tested compounds. Additionally, the synthesized compounds were evaluated for their in vitro antimicrobial activity against two each gram positive, gram negative and antifungal strains.

show abstract

Synthesis and antimalarial potential of some novel quinoline-pyrazolopyridine derivatives

Cited by 3 publications

References 12 publications

Synthesis of new series of quinoline derivatives with insecticidal effects on larval vectors of malaria and dengue diseases

Synthesis of new series of quinoline derivatives with insecticidal effects on larval vectors of malaria and dengue diseases

Preparation, DFT calculations, docking studies, antioxidant, and anticancer properties of new pyrazole and pyridine derivatives

Synthesis, Characterization and Antimalarial–antimicrobial Studies of Some Novel Derivatives of Chloroquinoline Based Pyrazoles

Contact Info

Product

Resources

About