Synthesis, identification and in vitro biological evaluation of some novel 5-imidazopyrazole incorporated pyrazoline and isoxazoline derivatives

Kalaria, Piyush N.; Satasia, Shailesh P.; Raval, Dipak K.

doi:10.1039/c4nj00244j

Cited by 47 publications

(24 citation statements)

References 39 publications

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“…Biological activity assays revealed compound 81 to be potent, with inhibitory activity of 90 % at 100 μg mL −1 compared with the standard drugs rifampicin and isoniazid (Figure 15). [152] …”

Section: Pharmacological Profile Of Isoxazoline Derivativesmentioning

confidence: 99%

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2‐Isoxazolines: A Synthetic and Medicinal Overview

Kumar

Shankar

2020

ChemMedChem

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Isoxazolines are nitrogen‐ and oxygen‐containing five‐membered heterocyclic scaffolds with extensive biological activities. This framework can be readily obtained in good to excellent yields through 1,3‐dipolar cycloaddition between nitrones with alkynes or allenes, aryl/alkyl halides, alkynes, and oxaziridines under mild conditions. This scaffold has been an emerging area of interest for many researchers given their wide range of bioactivities. Herein we review synthetic strategies toward isoxazolines and the role these efforts have had in enhancing the biological activity of natural products and synthetic compounds such as antitubercular agents, COX‐1 inhibitors, COX‐2 inhibitors (e. g., valdecoxib), nicotinic receptor modulators, and MIF inhibitors. With a focus on efforts from 2010 onward, this review provides in‐depth coverage of the design and biological evaluation of isoxazoline systems and their impact on various pathologies.

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Section: Pharmacological Profile Of Isoxazoline Derivativesmentioning

confidence: 99%

“…Furthermore, the above derivatives exhibited outstanding action toward P. falciparum in contrast to quinine (standard drug) having IC 50 =0.268 μM (Figure 16). [152] …”

Section: Pharmacological Profile Of Isoxazoline Derivativesmentioning

confidence: 99%

2‐Isoxazolines: A Synthetic and Medicinal Overview

Kumar

Shankar

2020

ChemMedChem

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“…In continuation of our efforts to synthesize some novel heterocyclic motifs with biological interest [27][28][29][30][31][32][33][34][35][36][37][38][39][40], herein we report the design, synthesis, antimicrobial evaluation, cytotoxicity and genotoxicity of quinoline based 1,2,4-oxadiazole scaffold. Potent 1,2,4-oxadiazole moiety is linked to quinoline moiety at C-3 position to observe the synergistic effect of these rings towards antimicrobial activity.…”

Section: Introductionmentioning

confidence: 98%

Synthesis and biological screening of novel 2-morpholinoquinoline nucleus clubbed with 1,2,4-oxadiazole motifs

Karad

Purohit

Thummar

et al. 2017

European Journal of Medicinal Chemistry

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“…Amongst the numerous heterocyclic organic luminescent materials, pyrazoline and its derivatives have received increasing attention due to their excellent electro-optical properties [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 , 9 , 10 , 11 , 12 , 13 , 14 ] and wide range of applications. For example, they are used in fluorescent probes, organic light-emitting diodes, and many other materials [ 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 ].…”

Section: Introductionmentioning

confidence: 99%

High Solid Fluorescence of a Pyrazoline Derivative through Hydrogen Bonding

et al. 2017

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Pyrazoline and its derivatives often exhibit strong emissions in dilute solutions, but their emission intensity is often dramatically reduced in the solid state due to strong intermolecular interactions between neighboring molecules. In this report, we successfully synthesized a new pyrazoline 4-(3-(4-(decyloxy)phenyl)-1-(2,3,5,6-tetrafluoro-4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-pyrazol-5-yl)-N,N-diethylaniline (PPDPD), into which seven fluorine (F) atoms were incorporated. In the solid state, PPDPD emits a strong blue light at λmax 430 nm with a fluorescence quantum yield of up to 41.3%. Single-crystal analysis showed the presence of intra/intermolecular C-H···F bonds that may impede molecular motion and block the non-radiative decay channel. Compound PPDPD therefore shows high emission efficiency in the solid state.

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Synthesis, identification and in vitro biological evaluation of some novel 5-imidazopyrazole incorporated pyrazoline and isoxazoline derivatives

Cited by 47 publications

References 39 publications

2‐Isoxazolines: A Synthetic and Medicinal Overview

2‐Isoxazolines: A Synthetic and Medicinal Overview

Synthesis and biological screening of novel 2-morpholinoquinoline nucleus clubbed with 1,2,4-oxadiazole motifs

High Solid Fluorescence of a Pyrazoline Derivative through Hydrogen Bonding

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