Synthesis and pharmacological activity of derivatives of quinoline and condensed quinolines

Граник, В. Г.; Zhidkova, A. M.; Kiselev, S. S.; Глушков, Р. Г.; Polezhaeva, A. I.; Mashkovskii, M. D.

doi:10.1007/bf00777630

Cited by 7 publications

(3 citation statements)

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“…Compounds containing an isatin moiety are most widely used as antiParkinsonian (Knö lker & Reddy, 2002), antifungal (Granik et al, 1978) and anticancer agents (Marko et al, 2001). Additionally, isatin derivatives find applications in chemistry of transition metal catalysts for uniform polymerization and in luminescence chemistry (Grandberg et al, 1968).…”

Section: Structure Descriptionmentioning

confidence: 99%

5-Fluoro-1-(prop-2-en-1-yl)-2,3-dihydro-1H-indole-2,3-dione

Qachchachi¹,

Mague

Rodi³

et al. 2017

IUCr Data

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The asymmetric unit of the title compound, C11H8FNO2, consists of two independent molecules having different conformations and associated through pairwise C—H...F hydrogen bonds. These units form `stairstep' stacks along theb-axis directionviaπ–π stacking interactions between dihydroindole moieties, with interplanar spacings of 3.578 (3) and 3.627 (3) Å. The stacks are tied together by weak C—H...O hydrogen bonds.

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Section: Structure Descriptionmentioning

confidence: 99%

5-Fluoro-1-(prop-2-en-1-yl)-2,3-dihydro-1H-indole-2,3-dione

Qachchachi¹,

Mague

Rodi³

et al. 2017

IUCr Data

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“…7 Quinoline nucleus occurs abundantly in many synthetic materials. 8 Many of these have been known to exhibit antiviral, 9 anti-fungal, 10 antibacterial, 11 Antiallergenic, 12 hypocholesterolemia 13 and hypovolemic 14 etc. activities.…”

Section: Introductionmentioning

confidence: 99%

An Expeditious Approach to the Synthesis of Novel Quinolino and Diazacino Condensed Analogues of Azepino [3, 2-b] Carbazole-2-one of Medicinal Interest

Agrawal¹,

Dwivedi²,

Kishore³

et al. 2022

IJPER

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Background: Quinolino and diazacino are important heterocyclics moiety, which have been reported to possess various activities such as antiallergenic, antifungal, hypocholesterolemic, antibacterial and antiviral activities. The activities of these compounds were related to inhibition of bacterial dehydrogenase enzyme which is one of the important targets studied for designing of antimicrobial drugs. Further, molecular docking approached is used in the present study for confirming potent molecules. Objectives: Aim of the study is to synthesize a series of quinolino and diazacino condensed analogues and evaluation of their anti-microbial activity. Methods: Quinolino and diazacino condensed analogues of azepino [3, 2-b] carbazole-2-one were synthesized by Friedel-Craft acylation and Pfitzinger reaction. Structures of synthesized compounds were characterized by FTIR and HNMR and were evaluated for antimicrobial activity by in-vitro bacterial dehydrogenase activity agar well diffusion assay. Further, in order to determine the binding affinity, molecular docking of synthesized compounds was also performed using bacterial (3NUH of E. coli) and fungal proteins (1FI4). In addition, bacterial dehydrogenase inhibitory activity of most active compound was performed using MTT assay. Results: Synthesized compounds (3, 4 and 6) caused impressive antibacterial and antifungal activities in-vitro assay when compared to the ciprofloxacin and fluconazole. And molecular docking studies also revealed that the synthesized compounds 3, 4 and 6 exhibits good to excellent affinity towards target microbial proteins. Conclusion: Synthesized compounds (3, 4 and 6) hold substantial antibacterial potential and require further exploration to establish them as therapeutic candidates in clinical management.

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“…Heterocyclic chemistry has wide array of biologically active compounds isolated from natural sources or synthesized in the laboratory, such as coumarins [10][11][12] , quinolines 13,14 , triazoles 15 and phenolics 16,17 etc. They are also if present as a part of giant molecule, imparting significant activity to these molecules.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Physicochemical Analysis of some Mannofuranoside Derivatives with Potent Antimicrobial Activity

Hassan¹,

Nasibullah²,

Ahmad³

et al. 2017

Orient. J. Chem

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We have synthesized protected mannofuranose as a glycosyl donor and some heterocyclic moieties as glycosyl acceptor. Coupling of glycosyl donor and acceptor by glycosylation, results in the formation of mannofuranoside derivatives. Antimicrobial potential of synthesized compounds were tested against five different human pathogenic bacteria and two fungi by using microdilution method. Interestingly, all synthesized mannofuranoside derivatives gave antimicrobial activity. Cumulatively, inhibitory concentration (IC 50 ) against bacteria were found to be in the range of 84.28-309.43 μg/ml, while, IC 50 against fungus were in the range of 0.59-3.82 mg/ml. Ampicillin and Fluconazole were used as positive control. Further, physicochemical parameters of synthesized mannofuranoside derivatives were analyzed using in-silico approach. Fortunately, none of our synthesized mannofuranoside derivatives gave violation of Lipinski's Rule of Five. Thus, we can safely state that these synthesized mannofuranoside derivatives could be considered as potential anti-microbial drug candidates.

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Synthesis and pharmacological activity of derivatives of quinoline and condensed quinolines

Cited by 7 publications

References 1 publication

5-Fluoro-1-(prop-2-en-1-yl)-2,3-dihydro-1H-indole-2,3-dione

5-Fluoro-1-(prop-2-en-1-yl)-2,3-dihydro-1H-indole-2,3-dione

An Expeditious Approach to the Synthesis of Novel Quinolino and Diazacino Condensed Analogues of Azepino [3, 2-b] Carbazole-2-one of Medicinal Interest

Synthesis, Characterization and Physicochemical Analysis of some Mannofuranoside Derivatives with Potent Antimicrobial Activity

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