Bioactive Fused Pyrazoles Inspired by the Adaptability of 5-Aminopyrazole Derivatives: Recent Review

Molecules, Год журнала: 2025, Номер 30(2), С. 366 - 366

Опубликована: Янв. 17, 2025

Heterocyclic compounds, especially those containing the pyrazole moiety, are highly significant in organic chemistry and possess remarkable diverse biological properties. The 5-aminopyrazole derivatives key starting materials for synthesis of numerous bioactive compounds such as pyrazolopyridine, pyrazolopyrimidine, pyrazoloquinazoline, pyrazolotriazine derivatives. Many inspired by a wide spectrum activities medicinal applications antioxidants, anticancer agents, enzyme inhibitors, antimicrobials, anti-tuberculosis activities. This review summarizes recently reported methods fused pyrazole-based based on within last 5 years (2020 to present). One important goals this is illustrate future strategies design, development, utilization products potent drugs.

Язык: Английский

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Synthesis of novel series of pyrazolo[1,5-a]pyrimidines target PIM-1 kinase

Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 142412 - 142412

Опубликована: Апрель 1, 2025

Язык: Английский

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Synthesis of new bis(pyrazolo[1,5- a ]pyrimidines) linked to different spacers with potential MurB inhibitory activity utilizing 1 H -pyrazole-3,5-diamines

Synthetic Communications, Год журнала: 2024, Номер unknown, С. 1 - 13

Опубликована: Ноя. 17, 2024

Recently, there has been an increased interest in developing new antibacterial agents that target the MurB inhibition, which is necessary for bacterial survival. We developed a two-step tandem protocol to synthesize 15 bis(pyrazolo[1,5-a]pyrimidines), are attached alkane cores by amide linkages. The involved reacting appropriate bis(2-cyanoacetamides) with dimethylformamide-dimethylacetal toluene at 80 °C 3-4 h. crude bis(2-cyano-3-(dimethylamino)acrylamides) was collected, then reacted 3,5-diamino-1H-pyrazoles. reaction gave desired products 82-92% yields after 5-6 h of heating reflux pyridine. Bis(2,7-diamino-3-(4-methoxybenzyl)pyrazolo[1,5-a]pyrimidine-6-carboxamides) demonstrated comparable efficacy ciprofloxacin. Their MIC and MBC ranged from 2.8-3.0 5.7-6.0 µM, respectively, against S. aureus E. coli. Moreover, these displayed promising inhibitory activity IC50 ranging 7.8 8.0 µM.

Язык: Английский

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Benzo[6,7]cyclohepta[1,2-d]pyrazolo[1,5-a]pyrimidines: Regioselective Synthesis of a Novel Ring System, DFT-based NMR Prediction, Local Reactivity Indexes, and MEP Analysis

Journal of Molecular Structure, Год журнала: 2024, Номер unknown, С. 140030 - 140030

Опубликована: Сен. 1, 2024

Язык: Английский

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Current scenario of pyrazole hybrids with anti‐breast cancer therapeutic applications

Archiv der Pharmazie, Год журнала: 2024, Номер 357(10)

Опубликована: Июнь 29, 2024

Breast cancer stands as the leading cause of cancer-related deaths among women globally, but current therapy is restricted to serious adverse effects and multidrug resistance, necessitating exploration novel, safe, efficient anti-breast chemotherapeutic agents. Pyrazoles exhibit excellent potential for utilization effective agents due their ability act on various biological targets. Particularly, pyrazole hybrids demonstrated advantage targeting multiple pathways, some them, which are exemplified by larotrectinib (pyrazolo[1,5-a]pyrimidine hybrid), can be applied breast therapy. Thus, hold great promise useful therapeutic interventions cancer. The aim this review summarize scenario with in vitro and/or vivo potential, along modes action structure-activity relationships, covering articles published from 2020 present, streamline development rational, safe candidates.

Язык: Английский

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Preparation and evaluation of pyrazolo[1,5-a] pyrimidine azo disperse dyes as colored materials in dyeing onto polyester fabrics

Pigment & Resin Technology, Год журнала: 2024, Номер unknown

Опубликована: Дек. 14, 2024

Purpose This study aims to prepare some disperse dyes based on pyrazole derivatives and fully evaluate their use as azo-disperse linked with pyrazolo[1,5-a] pyrimidine. dye polyester fabric at different conditions (pH time) a depth of 4% using high-temperature pressure process in water. Design/methodology/approach The were created by dissolving enaminone glacial acetic acid fusing sodium acetate reflux for 6 h. chemical structure the produced was studied elemental analysis, Fourier-transform infrared spectroscopy, 1H NMR 13C spectroscopic analytical methods. dyeing Dispersed 14–16 under diverse comprehensively investigated this work. Findings prepared Organic found be highly functional suitable type technique. High color strength is possessed materials dyed Disperse 14–16. Even low alkaline conditions, these exhibited strong affinity fabric, changing just little response pH changes. hue samples varied from beige reddish brown yellowish because coupler moieties. Originality/value important it offers novel that may used polyethylene terephthalate fibers exhibit remarkable brightness levelness. It also viable solution creating variety colors fabrics.

Язык: Английский

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Machine Learning-Based QSAR Classifications for PIM Kinases Inhibition Prediction: Towards the Neoplastic in Silico Drug Design

Advances in Science, Technology & Innovation/Advances in science, technology & innovation, Год журнала: 2024, Номер unknown, С. 99 - 109

Опубликована: Янв. 1, 2024

Язык: Английский

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Synthesis of novel pyridine and pyrazolyl pyridine conjugates with potent cytotoxicity against HepG2 cancer cells as PIM-1 kinase inhibitors and caspase activators

RSC Advances, Год журнала: 2024, Номер 14(53), С. 39381 - 39394

Опубликована: Янв. 1, 2024

Novel pyridine and pyrazolyl derivatives were synthesized characterized with potent cytotoxicity against HepG2 cancer cells as PIM-1 kinase inhibitors caspase activators.

Язык: Английский

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