An efficient one-pot synthesis and in vitro antimicrobial activity of new pyridine derivatives bearing the tetrazoloquinoline nucleus

Mungra, Divyesh C.; Patel, Manish P.; Patel, Ranjan G.

doi:10.3998/ark.5550190.0010.e06

Cited by 13 publications

(11 citation statements)

References 3 publications

(3 reference statements)

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“…In past reports, the existence of some drawbacks, such as harsh conditions, toxic organic solvents, long reaction times, high costs, difficult reuse, low product yields, and eco-unfriendly catalysts have limited the use of these methods [19][20][21][22][23][24][25][26]. Therefore, this paper reports a novel, simple, and efficient strategy for the preparation of pyrimidine and pyridine derivatives with anticarcinogenic potential, without solvent, under microwave irradiation, and using magnetic cobalt ferrite nanoparticles as the catalyst.…”

Section: Docking Analysismentioning

confidence: 99%

“…In light of the importance of DHPM derivatives, several improved methods have been reported for the preparation of these compounds using various catalysts [19][20][21][22]. Although multiple methods have been reported for preparing functionalized pyridine derivatives [23][24][25][26], most require multiple steps, a large excess of expensive reagents, long reaction times, toxic solvents, and forceful reaction conditions.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis, cytotoxic assessment, and molecular docking studies of 2,6-diaryl-substituted pyridine and 3,4- dihydropyrimidine-2(1H)-one scaffolds

et al. 2020

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Cancer is one of the main global health problems. In order to develop novel antitumor agents, we synthesized 3,4-dihydropyrimidine-2(1H)-one (DHPM) and 2,6-diaryl-substituted pyridine derivatives as potential antitumor structures and evaluated their cytotoxic effects against several cancer cell lines. An easy and convenient method is reported for the synthesis of these derivatives, employing cobalt ferrite (CoFe 2 O 4 @SiO 2 -SO 3 H) magnetic nanoparticles under microwave irradiation and solvent-free conditions. The structural characteristics of the prepared nanocatalyst were investigated by FTIR, XRD, SEM, and TGA techniques. In vitro cytotoxic effects of the synthesized products were assessed against the human breast adenocarcinoma cell line (MCF-7), gastric adenocarcinoma (AGS), and human embryonic kidney (HEK293) cells via MTT assay. The results indicated that compound 4r (DHPM derivative) was the most toxic molecule against the MCF-7 cell line (IC 50 of 0.17 μg/mL). Moreover, compounds 4j and 4r (DHPM derivatives) showed excellent cytotoxic activities against the AGS cell line, with an IC 50 of 4.90 and 4.97 μg/mL, respectively. Although they are pyridine derivatives, compounds 5g and 5m were more active against the MCF-7 cell line. Results showed that the candidate compounds exhibited low cytotoxicity against HEK293 cells. The kinesin Eg5 inhibitory potential of the candidate compounds was evaluated by molecular docking. The docking results showed that, among the pyridine derivatives, compound 5m had the most free energy of binding (–9.52 kcal/mol) and lowest Ki (0.105 μM), and among the pyrimidine derivatives, compound 4r had the most free energy of binding (–7.67 kcal/mol) and lowest Ki (2.39 μM). Ligand-enzyme affinity maps showed that compounds 4r and 5m had the potential to interact with the Eg5 binding site via H-bond interactions to GLU116 and GLY117 residues. The results of our study strongly suggest that DHPM and pyridine derivatives inhibit important tumorigenic features of breast and gastric cancer cells. Our results may be helpful in the further design of DHPMs and pyridine derivatives as potential anticancer agents.

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Section: Docking Analysismentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis, cytotoxic assessment, and molecular docking studies of 2,6-diaryl-substituted pyridine and 3,4- dihydropyrimidine-2(1H)-one scaffolds

et al. 2020

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“…Such properties may play important role in developing new antimicrobial drugs [11,12]. Another pyridine derivative -2-amino-3-cyanopyridine -was found to have antibacterial [13], antimicrobial [14,15], antifungal [16], cardiotonic [17], analgesic [18], and antiinflammatory [19] properties and was effective against lung cancer [20]. The studies showed that induction of apoptosis was related with the antimicrobial mechanism and the antibacterial effect occurred through apoptosis [21].…”

Section: Introductionmentioning

confidence: 99%

Removal of Fluoride from Drinking Water Using Protonated Glycerol Diglycidyl Ether Cross-Linked Chitosan Beads

Pathirannehe¹,

Fernando²,

Rajapakse³

2021

ChChT

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In this study, physically and chemically modified chitosan; protonated glycerol diglycidyl ether cross-linked chitosan beads (GDCLCB/H+) were prepared and characterized using FTIR and SEM. The optimum defluoridation capacity (DC) of GDCLCB/H+ was observed at the initial F- ion concentration of 15 mg/l, adsorbent dosage of 0.6 g, contact time of 30 min and pH of the solution was in the range of 5–7 at 303 ± 2 K. The equilibrium adsorption data fitted well with Langmuir and Freundlich isotherm models. The maximum adsorption capacity (q0), obtained from Langmuir isotherm for F-adsorption was found to be 2000 mg/kg, which was significantly higher than that of unmodified chitosan (192.3 mg/kg) and most of the chitosan-based sorbents reported in the literature. Water samples collected from Medawachchiya, Sri Lanka, were treated with the adsorbents and the results suggested that GDCLCB/H+ could be used as an effective defluoridation agent.

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“…Pyridine derivatives are currently an important group of organic compounds that have therapeutic and pharmacological properties. 1 They are used as antibacterial, 2,3 antimicrobial, 4,5 antifungal, 6 cardiotonic, 7 analgesic, 8 antiinflammatory 9 and anti-lung cancer 10 agents. The pyridine moiety is found in structurally simple drugs like isoniazid I, 11 ethionamide II, 12 amrinone III, 13 bupicomide IV, 14 pinacidil V, 15 torasemide VI and omeprazole VII 16 (Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Synthesis of novel bis(dihydropyridine) and terpyridine derivatives

Hebishy¹,

Abdelhamid²,

Elwahy³

2018

Arkivoc

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A synthesis of novel bis(cyanopyridones) by the reaction of the appropriate bis(cyanoacetamide) with the corresponding arylidenmalononitrile in the presence of basic catalysts was reported. In some cases, the corresponding bis(2-cyano-3-arylacrylamide) derivatives were isolated from these reactions as single products. The multicomponent strategy for the synthesis of the target compounds was also investigated. The utility of bis(cyanoacetamides) as building blocks for novel bisquinolinones was also studied.

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An efficient one-pot synthesis and in vitro antimicrobial activity of new pyridine derivatives bearing the tetrazoloquinoline nucleus

Cited by 13 publications

References 3 publications

Synthesis, cytotoxic assessment, and molecular docking studies of 2,6-diaryl-substituted pyridine and 3,4- dihydropyrimidine-2(1H)-one scaffolds

Synthesis, cytotoxic assessment, and molecular docking studies of 2,6-diaryl-substituted pyridine and 3,4- dihydropyrimidine-2(1H)-one scaffolds

Removal of Fluoride from Drinking Water Using Protonated Glycerol Diglycidyl Ether Cross-Linked Chitosan Beads

Synthesis of novel bis(dihydropyridine) and terpyridine derivatives

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