Glycerol Mediated Synthesis, Biological Evaluation, and Molecular Docking Study of 4‐(1<i>H</i>‐pyrazol‐4‐yl)‐polyhydroquinolines as Potent Antitubercular Agents

Jamale, Dattatraya K.; Undare, Santosh S.; Valekar, Navanath J.; Sarkate, Aniket P.; Kolekar, Govind B.; Anbhule, Prashant V.

doi:10.1002/jhet.3438

Cited by 19 publications

(6 citation statements)

References 66 publications

(37 reference statements)

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“…With a minimal inhibitory concentration of 1.6 μg/mL, the compounds (210h) and (210k), showed significant antitubercular efficacy. (Scheme 43) [58] Viswanadh Nalla et al created a series of 20 novel chromone embedded [1,2,3]-triazoles derivatives using a simple and convenient synthesis technique starting with 2-hydroxy acetophenone. To synthesize the target derivative, Copper sulphate pentahydrate, sodium ascorbate, and distilled water were added progressively to a stirred solution of azide and aliphatic/aromatic alkynes in t-butanol.…”

Section: Ms Komal Saini Has Been Working As Anmentioning

confidence: 99%

See 1 more Smart Citation

A Comprehensive Examination of Heterocyclic Scaffold Chemistry for Antitubercular Activity

Bendi,

Yadav,

Saini

et al. 2024

Chemistry & Biodiversity

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Tuberculosis is a communicable disease which affects humans particularly the lungs and is transmitted mainly through air. Despite two decades of intensive research aimed at understanding and combating tuberculosis, persistent biological uncertainties continue to hinder progress. Nowadays, heterocyclic compounds have proven themselves in effective treatment of tuberculosis because of their wide range of biological and pharmacological activities. Antituberculosis or antimycobacterial agents encompass a broad array of compounds utilized singly or in conjunction to combat Mycobacterium infections, spanning from tuberculosis to leprosy. Here, we summarize the synthesis of various heterocyclic compounds which includes the greener synthetic route as well as use of nano compounds as catalyst along with their anti TB activities.

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Section: Ms Komal Saini Has Been Working As Anmentioning

confidence: 99%

“…With a minimal inhibitory concentration of 1.6 μg/mL, the compounds (210h) and (210k), showed significant antitubercular efficacy. (Scheme 43) [58] …”

Section: Chemistry Of Different Heterocycle Scaffolds As Antitubercul...mentioning

confidence: 99%

A Comprehensive Examination of Heterocyclic Scaffold Chemistry for Antitubercular Activity

Bendi,

Yadav,

Saini

et al. 2024

Chemistry & Biodiversity

View full text Add to dashboard Cite

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“…Jamale et al reported the preparation of 4-(1Hpyrazol-4-yl)-polyhydroquinoline derivatives 114 by one-pot four component Hantzsch condensation reaction (Scheme 32). [72] The reaction involved 1,3-diphenyl-1H-pyrazole-4-carbaldehydes 111, alkyl acetoacetate 112, ammonium acetate 113, dimedone 106 and promoted by glycerol in an efficient manner by conventional heating at 95 °C for 2 h.…”

Section: Synthesis Using Metal Free Approachmentioning

confidence: 99%

Recent Advances in Green Synthesis of Functionalized Quinolines of Medicinal Impact (2018‐Present)

Yadav

Bhalla

2022

ChemistrySelect

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The synthetic chemists are awakening to make substantial development in finding safer drugs against the rising communicable and non‐communicable type of diseases. By replacing traditional methods to more sustainable and greener approaches, multicomponent reactions are the rapid and efficient tool for the synthesis of organic molecules of structural diversity and complexity. Heterocyclic chemistry transforms small set of precursors into series of molecules by multicomponent domino reactions. This review covers recent trends of last five years (2018–2022) in construction of potentially drug‐like quinoline derivatives. The methods discussed here are preferable over conventional approaches being inexpensive, consuming lesser reaction time, atom economical, saving energy and manpower while avoiding toxic reagents/materials, chemical wastes and are environmental/occupational benign. The contributions covered here involve metallic, metal free strategies and other catalytic pathways including nanoparticles, ionic liquids and photocatalysis which are operationally safe and reliable.

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“…Jamale et al (17) showed that their polyhydroquinoline derivatives had significant potential as an antimicrobial. Some of the compounds were effective against Mycobacterium tuberculosis, which is an extremely difficult microorganism to eradicate.…”

Section: Antimicrobial Activitymentioning

confidence: 99%

Synthesis of the Polyhydroquinoline Derivative 4-(2-Chloro-Phenyl)-2,7,7-Trimethyl5-oxo-1,4,5,6,7,8-Hexahydroquinoline-3-Carboxylic Acid Ethyl Ester: Antimicrobial and Enzyme Modulator

Machado

Trento

Pinelli

et al. 2021

Preprint

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Multicomponent reactions are extremely relevant in green chemistry. They offer better conditions than traditional synthesis and are, therefore, used for many organic modifications. Recently, the synthesis of polyhydroquinolines has received much attention for its high pharmacological potential. In the present study, a polyhydroquinoline derivative was synthesized without the use of catalysts or solvents. The results of nuclear magnetic resonance and infrared spectroscopy demonstrated that the molecule was successfully synthesized. The molecule presents significant results of antimicrobial activity for the bacteria tested in the serial dilution method. It also increased the clotting time by 25.66 seconds for the highest dose and 12.66 seconds for the other doses tested. Prior incubation with the dose of 125 mg reduced the thrombolytic activity to 73%. The 125, 100, and 50 mg doses previously incubated with Bothrops moojeni venom inhibited approximately 30% of the phospholipase activity. The molecule was also able to reduce the cytotoxicity induced by proteases significantly. In conclusion, the molecule presents several biological properties, which highlights its pharmaceutical potential.

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Glycerol Mediated Synthesis, Biological Evaluation, and Molecular Docking Study of 4‐(1H‐pyrazol‐4‐yl)‐polyhydroquinolines as Potent Antitubercular Agents

Cited by 19 publications

References 66 publications

A Comprehensive Examination of Heterocyclic Scaffold Chemistry for Antitubercular Activity

A Comprehensive Examination of Heterocyclic Scaffold Chemistry for Antitubercular Activity

Recent Advances in Green Synthesis of Functionalized Quinolines of Medicinal Impact (2018‐Present)

Synthesis of the Polyhydroquinoline Derivative 4-(2-Chloro-Phenyl)-2,7,7-Trimethyl5-oxo-1,4,5,6,7,8-Hexahydroquinoline-3-Carboxylic Acid Ethyl Ester: Antimicrobial and Enzyme Modulator

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