Synthesis, Biological Evaluation and Molecular Docking Studies of Novel 1,8-Naphthyridine-3-carboxylic Acid Derivatives as Potential Antimicrobial Agents (Part-1)

Gurjar, Vinod Kumar; Pal, D. R.; Mazumder, Avijit; Mazumder, Rupa

doi:10.36468/pharmaceutical-sciences.621

Cited by 10 publications

(10 citation statements)

References 22 publications

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“…Due to a broad spectrum of biological actions previously mentioned, 1,8-naphthyridine derivatives have gained increasing importance in the fields of medicinal chemistry and drug development. Studies indicate that these compounds have enormous potential for the synthesis of new molecules, which has been associated with the structure–activity relationship in several biological models [ 11 , 12 , 13 , 14 , 15 , 16 ]. Furthermore, molecular modifications can be used to improve the physicochemical properties of these substances, generating compounds with optimized therapeutic effects [ 8 , 9 , 10 ].…”

Section: Discussionmentioning

confidence: 99%

“…Nitrogen-containing heterocycles include both chemically synthesized and naturally occurring compounds such as 1,8-naphthyridine derivatives [ 10 ]. Studies have shown that these compounds have various biological activities such as antibacterial [ 11 ], antifungal [ 12 ], antiviral [ 13 ], anti-inflammatory [ 14 ], antitumor [ 15 ], and analgesic [ 16 ], and are therefore promising candidates for the development of new drugs.…”

Section: Introductionmentioning

confidence: 99%

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Enhancement of Antibiotic Activity by 1,8-Naphthyridine Derivatives against Multi-Resistant Bacterial Strains

et al. 2021

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The search for new antibacterial agents has become urgent due to the exponential growth of bacterial resistance to antibiotics. Nitrogen-containing heterocycles such as 1,8-naphthyridine derivatives have been shown to have excellent antimicrobial properties. Therefore, the purpose of this study was to evaluate the antibacterial and antibiotic-modulating activities of 1,8-naphthyridine derivatives against multi-resistant bacterial strains. The broth microdilution method was used to determine the minimum inhibitory concentration (MIC) of the following compounds: 7-acetamido-1,8-naphthyridin-4(1H)-one and 3-trifluoromethyl-N-(5-chloro-1,8-naphthyridin-2-yl)-benzenesulfonamide. The antibiotic-modulating activity was analyzed using subinhibitory concentrations (MIC/8) of these compounds in combination with norfloxacin, ofloxacin, and lomefloxacin. Multi-resistant strains of Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus were used in both tests. Although the compounds had no direct antibacterial activity (MIC ≥ 1.024 µg/mL), they could decrease the MIC of these fluoroquinolones, indicating synergism was obtained from the association of the compounds. These results suggest the existence of a structure–activity relationship in this group of compounds with regard to the modulation of antibiotic activity. Therefore, we conclude that 1,8-naphthyridine derivatives potentiate the activity of fluoroquinolone antibiotics against multi-resistant bacterial strains, and thereby interesting candidates for the development of drugs against bacterial infections caused by multidrug resistant strains.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Enhancement of Antibiotic Activity by 1,8-Naphthyridine Derivatives against Multi-Resistant Bacterial Strains

et al. 2021

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“…Melting point was recorded on electro thermal CIA9300 melting point apparatus. The Proton nuclear magnetic resonance ( 1 HNMR) to identify the structure and 13 CNMR spectra were recorded on nucleic magnetic resinous model ultra shield 400MHZ, Bruker Co, Germany using TMS as internal reference and DMSO-d6 as solvent . IR spectra were recorded on infrared spectrophotometer model Tensor 27.Bruker Co. Germany by using KBr disc .…”

Section: Materials and Methods 21 Instrumentationmentioning

confidence: 99%

“…The reaction of phenyl hydrazine with chalcones (4,5) afforded compounds (12,13) (scheme-4-) . The IR spectra of these compounds (12,13) showed absorption at (1595 cm -1 and 1591 cm -1 ) for C=N group respectively . H 1 NMR spectra of these compounds showed a single signal at δ 5.31 and δ 5.31 for hydrogen in the pyrazoline ring .…”

Section: Scheme -2 -mentioning

confidence: 97%

“…The quinoline skeleton is often used to design of many synthetic compounds [3]. Quinoline derivatives posses useful biological activities such as anti malarial, anti-inflammatory, antibacterial, anticancer, anti-microbial, anthelmintic, anti-fungal besides wide range of pharmacological activities [4][5][6][7][8][9][10][11][12][13][14]. Chloroquinoline compound has been used as prophylactics to prevent the development of malaria [15].…”

Section: Introductionmentioning

confidence: 99%

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Synthesis biological studies of some new heterocyclic compound derived from 2-chloro-3-formyl quinoline and 4-(benzyl sulfonyl) acetophenone

2020

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A new series of quinoline chalcones have been prepared from condensations of 2-chloro-3-formyl quinoline (1) with 4-(benzothio) acetophenone(2) and 4-(benzyl sulfonyl) acetophenone(3). The reaction of chalcones(4,5) with bromine gives dibromide(6,7). New pyrazoline derivatives were synthesized by condensation of chalcones (4 or 5) with hydrazine hydrate to give (8,9) and with hydrazine hydrate in glacial acetic acid(gla) to give (10,11) and with phenyl hydrazine to give (12,13). The prepared chalcones (4,5) and dibromide(6,7) and pyrazoline derivative (8-13)have been screened for antibacterial activities against two gram positive staphylococcus aureus and staphylococcus epidermidis and two gram negative Escherichia coli and Proteus vulgaris. The synthesized compounds are proven by IR & NMR spectral and physical method.

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A Facile Three‐Component Catalyst‐Free Strategy: Synthesis of Indeno[1,2‐b][1,6]naphthyridine‐1,10(2H)‐dione Derivatives in Water

Zhang²,

et al. 2022

Asian J Org Chem

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A catalyst‐free protocol for synthesizing a new series of indeno[1,2‐b][1,6]naphthyridine‐1,10(2H)‐dione derivatives with good to excellent yields was established based on microwave‐assisted domino reaction of 4‐aminopyridin‐2(1H)‐ones, aldehydes and 1H‐indene‐1,3(2H)‐dione in water. The present approach exhibited useful and green features, such as water as reaction solvent, catalyst‐ and additive‐ free, short reaction time (20–30 min), as well as ease of desired products separation and purification without the need for column chromatography. Also to note, up to four new bonds were formed accompanied by generating water as sole by‐product in this one‐pot procedure.

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Synthesis, Biological Evaluation and Molecular Docking Studies of Novel 1,8-Naphthyridine-3-carboxylic Acid Derivatives as Potential Antimicrobial Agents (Part-1)

Cited by 10 publications

References 22 publications

Enhancement of Antibiotic Activity by 1,8-Naphthyridine Derivatives against Multi-Resistant Bacterial Strains

Enhancement of Antibiotic Activity by 1,8-Naphthyridine Derivatives against Multi-Resistant Bacterial Strains

Synthesis biological studies of some new heterocyclic compound derived from 2-chloro-3-formyl quinoline and 4-(benzyl sulfonyl) acetophenone

A Facile Three‐Component Catalyst‐Free Strategy: Synthesis of Indeno[1,2‐b][1,6]naphthyridine‐1,10(2H)‐dione Derivatives in Water

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