Synthesis and evaluation of antibacterial and antifungal activities of new (Z)-3-bromo-4-(1,3-diaryl-1H-pyrazol-4-yl)but-3-en-2-ones and 4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-1,3-diaryl-1H-pyrazoles

Pundeer, Rashmi; Sushma, .; Kiran, Vijay; Sharma, Chetan; Aneja, K. R.; Prakash, Om

doi:10.1007/s00044-013-0480-0

Cited by 17 publications

(6 citation statements)

References 46 publications

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“…Pyrazole exhibits a wide range of pharmacological activities such as antioxidant, antifungal, antitubercular, antimalarial, antiproliferative, anticancer, anti-inflammatory, and antimicrobial activities. In addition to this, heterocyclic hybrids of pyrazole derivatives have been reported − as they display an antifungal activity profile.…”

Section: Introductionmentioning

confidence: 99%

New 1,2,3-Triazole-Appended Bis-pyrazoles: Synthesis, Bioevaluation, and Molecular Docking

et al. 2021

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The present work describes design of a small library of new 1,2,3-triazole-appended bis-pyrazoles by using a molecular hybridization approach, and the synthesized hybrids were evaluated for their antifungal activity against different fungal strains, namely, Candida albicans, Cryptococcus neoformans, Candida glabrata, Candida tropicalis, Aspergillus niger, and Aspergillus fumigatus. All the compounds exhibited broad-spectrum activity against the tested fungal strains with excellent minimum inhibitory concentration values. The molecular docking study against sterol 14α-demethylase (CYP51) could provide valuable insights into the binding modes and affinity of these compounds. Furthermore, these compounds were also evaluated for their antioxidant activity, which also resulted in promising data.

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Section: Introductionmentioning

confidence: 99%

New 1,2,3-Triazole-Appended Bis-pyrazoles: Synthesis, Bioevaluation, and Molecular Docking

et al. 2021

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“…Heating a mixture of ( Z )‐3‐bromo‐4‐(1,3‐diaryl‐1 H ‐pyrazol‐4‐yl)‐3‐buten‐2‐ones 205 and phenyl hydrazine in acetic acid resulted in the production of the 3,4′‐bipyrazole derivatives 206 in 75–85 % yields (Scheme 52). [103] The bipyrazoles 206 showed in vitro antibacterial and antifungal activities closely related with the standard antibiotics ciprofloxacin and fluconazole.…”

Section: Synthetic Routes To Bipyrazolesmentioning

confidence: 99%

Synthetic Routes to Bioactive Bipyrazole Derivatives

Dawood

Abbas

2021

ChemistrySelect

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The synthetic routes to six differently connected bipyrazole systems 1,1′‐, 1,3′‐ and 1,4′‐, 3,3′‐, 3,4′‐ and 4,4′‐bipyrazoles are thoroughly reported. Two main synthetic platforms are outlined; i) cyclocondensation reactions of tetraketones or pyrazoles having difunctional moieties with hydrazines, or pyrazolyl‐hydrazines with difunctional substrates, ii) 1,3‐dipolar cycloaddition of nitrilimines with bis‐olefines, or bis‐nitrilimines with activated alkenes and alkynes. Many of the reported bipyrazoles have potent applications; in pharmaceutical and material science areas.

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“…Pyrazole and its derivatives are potent medicinal scaffolds, and they exhibit a large spectrum of biological activities against infectious diseases. They showed antibacterial and antifungal, antitubercular, anticancer, antioxidant, anti‐inflammatory and antipyretic activities. Quinoline tethered azole hybrids are important pharmacophores that possess a wide range of biological activities .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of New 1,2,3‐Triazolyl‐Pyrazolyl‐Quinoline Derivatives as Potential Antimicrobial Agents

et al. 2020

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A new series of 4-{1-phenyl-4-[(4-phenyl-1,2,3-triazol-1-yl)methyl]pyrazol-3-yl}quinoline (7a-l) have been synthesized by a click reaction of 4-(4-(azidomethyl)-1-phenyl-1H-pyrazol-3-yl) quinoline (5a-d) with a substituted ethynylbenzene. The newly synthesized 1,2,3-triazolyl-pyrazolyl-quinoline derivatives were evaluated for biological activity against Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388), (Gram negative strains), Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178) (Gram positive strains) and in vitro antifungal activity against Candida albicans (NCIM 3100) and Aspergillus niger (ATCC 504). Five 1,2,3-triazolyl-pyrazolyl-quinoline derivatives, 7d, 7 g, 7 h, 7k and 7 l exhibited good antifungal activity against A. niger with MIC 62.5 μg/mL. The compounds 7 h, 7k and 7 l were further evaluated for ergosterol inhibition assay against A. niger cell sample at 62.5 μg/mL concentration. Upon analysis of the sterol inhibition assay, it was revealed that, the ergosterol biosynthesis has decreased in the fungal samples treated with the 1,2,3-triazolyl-pyrazolyl-quinoline derivatives. Thus antimicrobial activity suggested that, these compounds could aid and assist in the development of lead compounds to treat microbial infections.

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Synthesis and evaluation of antibacterial and antifungal activities of new (Z)-3-bromo-4-(1,3-diaryl-1H-pyrazol-4-yl)but-3-en-2-ones and 4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-1,3-diaryl-1H-pyrazoles

Cited by 17 publications

References 46 publications

New 1,2,3-Triazole-Appended Bis-pyrazoles: Synthesis, Bioevaluation, and Molecular Docking

New 1,2,3-Triazole-Appended Bis-pyrazoles: Synthesis, Bioevaluation, and Molecular Docking

Synthetic Routes to Bioactive Bipyrazole Derivatives

Synthesis and Biological Evaluation of New 1,2,3‐Triazolyl‐Pyrazolyl‐Quinoline Derivatives as Potential Antimicrobial Agents

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