1,8-Naphthyridines VII. New substituted 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides and their isosteric analogues, exhibiting notable anti-inflammatory and/or analgesic activities, but no acute gastrolesivity

Roma, G.; Grossi, Giancarlo; Braccio, Mario Di; Piras, Daniela; Ballabeni, Vigilio; Tognolini, Massimiliano; Bertoni, Simona; Barocelli, Elisabetta

doi:10.1016/j.ejmech.2007.10.010

Cited by 64 publications

(24 citation statements)

References 9 publications

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“…Quinoline derivatives are largely used in the pharmaceutical chemistry owing to the wide range of applications. Quinoline derivatives possess various biological activities such as antiviral , anticancer , antibacterial , antifungal , anti‐obesity , anti‐inflammatory , antimalarial , antituberculosis , hypnotic , antischizophrenic , anti‐protozoal , anti‐cholesterol , anthelmintic , and analgesic activities , and these activities were demonstrated in drug molecules, which are shown in Figure . At present, a wide range of microorganism such as fungi, viruses, and bacteria are becoming resistant against drugs that are used to treat infectious diseases.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Biological andIn SilicoStudy of Fluorine‐Containing Quinoline Hybrid Thiosemicarbazide Analogues

Patel

Prajapati

et al. 2019

Journal of Heterocyclic Chem

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A novel series of fluorine‐containing quinoline hybrid thiosemicarbazide analogues (8a–8l) were synthesized and tested for their biological activities. The antibacterial results demonstrated that compounds 8d and 8l [minimal inhibitory concentration (MIC) 62.5 μg/mL] were shown to have higher biological activity than ampicillin against Escherichia coli. Compound 8b (MIC 25 μg/mL) was shown to have the highest activity than was ampicillin against Staphylococcus aureus. The antifungal results demonstrated that compound 8j (MIC 100 μg/mL) has shown good activity. Most of the targeted compounds have shown potent antimalarial activity. Compounds 8d (0.19 μg/mL), 8g (0.30 μg/mL), 8h (0.36 μg/mL), 8k (0.10 μg/mL), 8l (0.28 μg/mL), 8k (0.10 μg/mL), and 8l (0.28 μg/mL) have notable activity than does the reference drug quinine. Compounds 8d (0.27 μg/mL), 8g (0.30 μg/mL), and 8k (0.17 μg/mL) have shown excellent activity against chloroquine‐resistant strain. The MTT assay performed on peripheral blood lymphocyte cultures showed a high percentage of lymphocyte viability [8d (99.64), 8g (99.46), 8h (98.83), and 8k (99.51)] at a maximum dose (10 μg/mL), depicting no cytotoxicity of these compounds on human lymphocytes in vitro. A molecular docking study was performed on Pf‐DHFR‐TS inhibitor. A molecular dynamics study has shown compound 8g to have better affinity with protein. ADME‐Tox and pharmacophore study of synthesized compounds suggested prediction of active site.

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Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Biological andIn SilicoStudy of Fluorine‐Containing Quinoline Hybrid Thiosemicarbazide Analogues

Patel

Prajapati

et al. 2019

Journal of Heterocyclic Chem

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“…Among these heterocyclic compounds 1,8‐naphthyridine derivatives possess broad range of useful biological properties establish in therapeutic and medicinal research. 1,8‐Naphthyridine scaffolds possess broad spectrum of beneficial pharmacological activities that include anti‐inflammatory , anti‐HIV , antimicrobial , and antitumor activities . 1,8‐Naphthyridine derivatives have also exhibited potential applications in neurological disorders such as Alzheimer's disease .…”

Section: Introductionmentioning

confidence: 99%

Green Synthesis of Fused Imidazo[1,2‐a][1,8]naphthyridine Derivatives Catalyzed by DABCO under Solvent‐Free Solid‐State Conditions and Their Biological Evaluation

Sonyanaik

Shyam

Sakram

2018

Journal of Heterocyclic Chem

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An efficient and eco‐friendly methodology has been developed for the construction of fused imidazo[1,2‐a][1,8]naphthyridine derivatives in the presence of 1,4‐diazabicyclo[2.2.2]octane, and involving various substituted heterocyclic amines with phenacyl bromide under solvent‐free solid‐state condition obtained the corresponding compounds (5a–g, 7a–f) in short reaction time with high yield which is the important features of this protocol. All newly synthesized products were evaluated for their antibacterial and fungal activities. All these compounds displayed good antibacterial and antifungal activity. In predominantly, compounds 7e, 7d, and 5d demonstrate the highest antibacterial and antifungal activities. Furthermore, in silico molecular docking studies results were well complemented to the antimicrobial activity.

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“…Quinolines and their derivatives are present in natural products, play significant role in medicinal chemistry as antibacterial [8], antimalarial [9], antiallergenic [10] and anti-inflammatory agents [11]. Plasmoquine, primaquine and chloroquine are well known marketed antimalarial drugs that contain quinoline core in their structure.…”

Section: Introductionmentioning

confidence: 99%

Solvent-free microwave assisted synthesis of morpholine–piperidine–pyrrolidine annulated quinoline-naphthyl based chalcones and their antimicrobial activity

et al. 2016

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A new series of 2-morpholine-piperidine-pyrrolidine substituted quinoline based chalcones have been synthesized by conventional and microwave irradiation methods. All synthesized compounds were characterised by IR, 1 H and 13 C NMR, mass spectrometry, and elemental analysis. The products were evaluated in vitro for antibacterial activity against two bacterial strains (Staphylococcus aureus, Escherichia coli) and antifungal activity against two fungal strains (Aspergillus flavus, Candida metapsilosis). 2-Piperidine substituted quinoline chalcones demonstrated high antimicrobial activity.

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1,8-Naphthyridines VII. New substituted 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides and their isosteric analogues, exhibiting notable anti-inflammatory and/or analgesic activities, but no acute gastrolesivity

Cited by 64 publications

References 9 publications

Design, Synthesis, and Biological andIn SilicoStudy of Fluorine‐Containing Quinoline Hybrid Thiosemicarbazide Analogues

Design, Synthesis, and Biological andIn SilicoStudy of Fluorine‐Containing Quinoline Hybrid Thiosemicarbazide Analogues

Green Synthesis of Fused Imidazo[1,2‐a][1,8]naphthyridine Derivatives Catalyzed by DABCO under Solvent‐Free Solid‐State Conditions and Their Biological Evaluation

Solvent-free microwave assisted synthesis of morpholine–piperidine–pyrrolidine annulated quinoline-naphthyl based chalcones and their antimicrobial activity

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