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A new series of 1,3,5-trisubstituted 2-pyrazoline derivatives (3a–l) are synthesized in good to excellent yields from the corresponding chalcones (1a–h) and acid hydrazides (2a–e) in polyethylene glycol-400 (PEG-400) as a green reaction medium. The newly synthesized 2-pyrazoline derivatives are screened for their antibacterial and antifungal activi...
Citations
... Pyrazoles are a class of bioactive compounds with diverse pharmacological effects such as anticancer [18,19], antiviral [20,21], antifungal [22], antibacterial [23], anti-inflammatory [24], antioxidant activities [25]. Moreover, hydrazine-coupled pyrazole derivatives are shown to have promising antimalarial and antileishmanial activities [26][27][28]. ...
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.
... The 1,3,5-trisubstituted 2-pyrazolines' antioxidant activity is also assessed using the OH and DPPH assays. The 1,3,5-trisubstituted 2-pyrazolines were shown to be effective antioxidants and to exhibit strong radical scavenger activity [78] (Fig. 50). ...
... Attributable to the increased microbial resistance brought on by antibiotic usage [4][5][6], against microorganisms. Therefore, there is an urgent need to create new, more potent antibacterial drugs [7][8][9][10][11][12]. ...
Reactant solubility, which dictates achievable concentrations, and the stability of reaction intermediates (excited states), solvents modulate the potential energy landscape and influence reaction rates. Consequently, solvent selection is pivotal in optimizing process productivity, economic feasibility, and environmental footprint. At present, organic synthesis pivots around the idea of sustainability. In particular, PEG‐400, a popular solvent and phase transfer catalyst, is considered greener as it can be reused several times without significant loss in its catalytic activity, which checks the box regarding sustainability. This review highlights the emerging potential of Polyethylene Glycol 400 (PEG‐400) as a dual‐threat agent in sustainable organic synthesis. We explore its efficacy as a catalyst, promoting various reactions under mild conditions and often eliminating the need for traditional metal catalysts. Additionally, PEG‐400's role as a green solvent is addressed, emphasizing its biodegradability, low toxicity, and ability to facilitate reactions without hazardous Volatile Organic Compounds (VOCs). The review examines recent research on PEG‐400 mediated reactions, showcasing its effectiveness in diverse transformations, thus exploring the potential of PEG 400 as a facilitator for heterocycle synthesis in both multicomponent reactions and stepwise approaches. It identifies exciting research directions that promise to expand the boundaries of polymer‐based solvents in heterocyclic chemistry.
Pyrazole-bearing compounds are known for their diverse pharmacological effects including potent antileishmanial and antimalarial activities. Herein, some hydrazine-coupled pyrazole derivatives were successfully synthesized and their structures were verified by employing elemental microanalysis, FTIR, and ¹ H NMR techniques. The in vitro antileishmanial and in vivo antimalarial activities of the synthesized pyrazole derivatives ( 9–15 ) were assessed using the clinical isolate of the Leishmania aethiopica strain and mice infected with Plasmodium berghei ANKA strain, respectively. The result revealed that compound 13 displayed superior antipromastigote activity (IC 50 = 0.018) that was 174- and 2.6-fold more potent than the standard drugs miltefosine (IC 50 = 3.130) and amphotericin B deoxycholate (IC 50 = 0.047). The molecular docking study conducted on Lm-PTR1 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 synthesis of safe and effective antileishmanial and antimalarial agents.
