Synthesis and Antimicrobial Evaluation of Some New Pyrazole Derivatives Containing Thiazole Scaffolds

Patil, Sachin; Suryavanshi, Manjusha B.; Nagargoje, Deepak R.; Kokate, Siddhant V.

doi:10.3390/ecsoc-25-11661

Cited by 5 publications

(21 citation statements)

References 33 publications

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“…and Aspergillus sp. strains [ 28 , 29 ]. Compounds 69 , 70 , 72 , and 74 showed inferior activities (MICs = 1.9–7.8 µg/mL) against S. aureus MTCC 96 and MTCC 2940, Micrococcus luteus MTCC 2470, K. planticola MTCC 530, E. coli MTCC 739, and P. aeruginosa MTCC 2453, compared to ciprofloxacin (MIC = 0.9 µg/mL).…”

Section: Structure–activity Relationships In Antimicrobial Thiazole-b...mentioning

confidence: 99%

“…Compounds 69 , 70 , 72 , and 74 showed inferior activities (MICs = 1.9–7.8 µg/mL) against S. aureus MTCC 96 and MTCC 2940, Micrococcus luteus MTCC 2470, K. planticola MTCC 530, E. coli MTCC 739, and P. aeruginosa MTCC 2453, compared to ciprofloxacin (MIC = 0.9 µg/mL). Compounds 75 – 86 showed superior activities (MICs = 3.9–18.5 µg/mL) against S. aureus , E. coli , and P. aeruginosa , compared to chloramphenicol (MICs = 24.6–32.8 µg/mL) [ 28 , 29 ].…”

Section: Structure–activity Relationships In Antimicrobial Thiazole-b...mentioning

confidence: 99%

“…Antibiofilm activity was favorably influenced by substitution with 8-bromocoumarin and benzo[ f ]coumarin heterocycles. The presence of benzothiazole moiety ( 69 – 74 ), which is known for its toxicity, could halt any future progress towards leader molecules [ 28 , 29 ].…”

Section: Structure–activity Relationships In Antimicrobial Thiazole-b...mentioning

confidence: 99%

“… The general structures for the series discussed, containing thiazole and pyrazole rings: 2-(pyrazol-4-yl)-methylylidenehydrazinyl-thiazoles ( a ), 2-(pyrazol-1-yl)-thiazoles ( b ), 2-(pyrazol-1-ium-1-yl)-thiazoles ( c ), and 5-(pyrazol-3-yl)-thiazoles ( d ) [ 28 , 29 , 30 , 31 , 32 , 33 , 34 ]. …”

Section: Figurementioning

confidence: 99%

See 3 more Smart Citations

An Overview of the Structure–Activity Relationship in Novel Antimicrobial Thiazoles Clubbed with Various Heterocycles (2017–2023)

Ungureanu,

Tiperciuc,

Nastasă

et al. 2024

Pharmaceutics

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Antimicrobial resistance is an increasing problem for global public health. One of the strategies to combat this issue is the synthesis of novel antimicrobials through rational drug design based on extensive structure–activity relationship studies. The thiazole nucleus is a prominent feature in the structure of many authorized antimicrobials, being clubbed with different heterocycles. The purpose of this review is to study the structure–activity relationship in antimicrobial thiazoles clubbed with various heterocycles, as reported in the literature between 2017 and 2023, in order to offer an overview of the last years in terms of antimicrobial research and provide a helpful instrument for future research in the field.

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Section: Structure–activity Relationships In Antimicrobial Thiazole-b...mentioning

confidence: 99%

Section: Structure–activity Relationships In Antimicrobial Thiazole-b...mentioning

confidence: 99%

Section: Structure–activity Relationships In Antimicrobial Thiazole-b...mentioning

confidence: 99%

Section: Figurementioning

confidence: 99%

See 2 more Smart Citations

An Overview of the Structure–Activity Relationship in Novel Antimicrobial Thiazoles Clubbed with Various Heterocycles (2017–2023)

Ungureanu,

Tiperciuc,

Nastasă

et al. 2024

Pharmaceutics

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“…We can quote the amidine which is a dual nucleophile due to the presence of two nitrogen atoms [2] and was known as a perfect precursors for the synthesis of a wide variety of pharmaceuticals and biologically active heterocyclic systems [2][3][4]. Indeed, they have some interesting therapeutic properties such as anti-inflammatory [5,6], antimicrobial [7], antiparasitic [8], antibacterial [9,10], anticancer [11,12], antiprotozoal [13], antifungal [14], antidepressant [15,16], anti-Parkinson [17] and antitumor activities [18].…”

Section: Introductionmentioning

confidence: 99%

Antioxidant activity, Dielectric and Electrical Properties of N-benzyl-N'-(5-methyl-1H-pyrazol-3-yl) propanimidamide.

Louiz,

Labiadh,

Abderrahim

et al. 2023

Preprint

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This article mainly focuses on recent advances in the study of the interesting electronic and biological powers of the N-benzyl-N'-(5-methyl-1H-pyrazol-3-yl) propanimidamide. The selected amidine has been previously synthesized, characterized in a previous publication and we present in this research the study of the antioxidant application, electrical activity and dielectric studies of the cristal. In this context, the amidine and the corresponding imidate were compared with ascorbic acid as a reference and showed an interesting antioxidant power, especially in Ferrous ion chelating (FIC) activity and Hydroxyl Radical (OH.) Scavenging. We also studied electrical activity as a function of frequency, impedance and alternating conductivity. The obtained results showed that the compound can be used in order to complex and impedance spectroscopy showed that synthesized amidine is a good short-range proton conductor. Impedance measurements approve the input of the resistive grain frontier on the conduction mechanism. Then, it evidences the existence of many electrical relaxation phenomena in the studied sample. The dielectric constant is temperature dependent indicating that the crystal is a polar dielectric compound and the dipole orientation is governed by increasing temperature.

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Synthesis, antileishmanial, antimalarial evaluation and molecular docking study of some hydrazine-coupled pyrazole derivatives

Berhe,

Birhan,

Beshay

et al. 2024

BMC Chemistry

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Pyrazole-bearing compounds are known for their diverse pharmacological effects including potent antileishmanial and antimalarial activities. Herein, some hydrazine-coupled pyrazoles were successfully synthesized and their structures were verified by employing elemental microanalysis, FTIR, and 1H NMR techniques. The in vitro antileishmanial and in vivo antimalarial activities of the synthesized pyrazole derivatives (9–15) were evaluated against Leishmania aethiopica clinical isolate and Plasmodium berghei infected mice, respectively. The result revealed that compound 13 displayed superior antipromastigote activity (IC50 = 0.018) that was 174- and 2.6-fold more active than the standard drugs miltefosine (IC50 = 3.130) and amphotericin B deoxycholate (IC50 = 0.047). The molecular docking study conducted on Lm-PTR1, complexed with Trimethoprim was acquired from the Protein Data Bank (PDB ID:2bfm), justified the better antileishmanial activity of compound 13. Furthermore, the target compounds 14 and 15 elicited better inhibition effects against Plasmodium berghei with 70.2% and 90.4% suppression, respectively. In conclusion, the hydrazine-coupled pyrazole derivatives may be considered potential pharmacophores for the preparation of safe and effective antileishmanial and antimalarial agents.

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Synthesis and Antimicrobial Evaluation of Some New Pyrazole Derivatives Containing Thiazole Scaffolds

Cited by 5 publications

References 33 publications

An Overview of the Structure–Activity Relationship in Novel Antimicrobial Thiazoles Clubbed with Various Heterocycles (2017–2023)

An Overview of the Structure–Activity Relationship in Novel Antimicrobial Thiazoles Clubbed with Various Heterocycles (2017–2023)

Antioxidant activity, Dielectric and Electrical Properties of N-benzyl-N'-(5-methyl-1H-pyrazol-3-yl) propanimidamide.

Synthesis, antileishmanial, antimalarial evaluation and molecular docking study of some hydrazine-coupled pyrazole derivatives

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