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N-Heterocycles
Published in Navjeet Kaur, Metals and Non-Metals, 2020
Pyrazolones are used in drugs and are of pharmacological importance, for they exhibit a number of medically useful properties—anti-fungal, anti-microbial, anti-bacterial, anti-mycobacterial, anti-tumor, anti-platelet, anti-inflammatory, anti-depressant, gastric secretion stimulatory as well as anti-filarial. They also work as substrates for pigments, dyes, chelating agents and pesticides [1–3]. Moreover, pyrazolones act as inhibitors against CDK2, with remarkable activity against a number of human tumor cell lines, cannabinoid type-1 (CB1) receptor antagonists, and against tissue-nonspecific alkaline phosphatase (TNAP). In pesticide chemistry, they have come to be used as fungicides, insecticides and herbicides. Pyrazole moiety is a core structure of a wide range of biologically active compounds such as blockbuster drugs like celecoxib and sildenafil (viagra). Whereas celecoxib exhibits anti-arthritic and analgesic activities and is a powerful COX-2 inhibitor, sildenafil (viagra) is a FDA approved drug used to treat erectile dysfunction [4–5].
Greener Synthesis of Potential Drugs
Published in Ahindra Nag, Greener Synthesis of Organic Compounds, Drugs and Natural Products, 2022
Renata Studzińska, Renata Kołodziejska, Daria Kupczyk
Pyrazole derivatives are ubiquitous in organic molecules with valuable biological functions. In recent years, a variety of new pyrazole derivatives have been discovered with enriched bioactivities such as the reversal activity to fluconazole resistance [55], antimicrobial activity [56], anticancer activity [57], antiproliferative activity [58], ALK5 kinase inhibitory activity [59], and antioxidation activity [60]. Not surprisingly, the green synthesis of pyrazoles and their derivatives keeps receiving interest.
Exploration of type II and III collagen binding interactions with short peptide-phenyl pyrazole conjugates via docking, molecular dynamics and laboratory experiments
Published in Soft Materials, 2023
Lucy R. Hart, Charlotta G. Lebedenko, Beatriz G. Goncalves, Mia I. Rico, Dominic J. Lambo, Diego S. Perez, Ipsita A. Banerjee
It has also been reported that compounds containing a pyrazole moiety such as 1-(4-(tert-butyl) benzyl)-N-(4-methoxyphenyl)-3-phenyl-1H-pyrazole-5-carboxamide (Pyr-C) have been shown to promote osteogenic differentiation in MC3T3-E1 cells.[26] In another study, it was shown that small molecules such as Fmoc-glycyl-(N-benzyl)-pyrazole-isothiazole-tert-butyl carboxylate-1,1-dioxide that contain protected amino acids conjugated with pyrazole-isothiazole derivatives formed stable, homogenous nanofibers upon electrospinning and may potentially be used for biomedical applications.[27] Furthermore, pyrazole-derivatives possess several desirable pharmacological properties including antitumor, anti-inflammatory, and analgesic activity.[28]
Eco-friendly one-pot synthesis of some new pyrazolo[1,2-b]phthalazinediones with antiproliferative efficacy on human hepatic cancer cell lines
Published in Green Chemistry Letters and Reviews, 2018
Huda R. M. Rashdan, Sobhi M. Gomha, Marwa S. El-Gendey, Maher A. El-Hashash, Abdel Mohsen M. Soliman
Identification of novel structures may be used in designing potent, new, less toxic and selective anticancer agents remains a major challenge for medical chemistry researchers. The 1,2,3-triazole-based heterocyclic compounds have been well exploited for the generation of many medicinal scaffolds exhibiting anti-HIV(1), antibacterial (2) inhibitors of galectin-3 (3) activities, etc. Moreover, researchers reported 1,2,3-triazole derivatives that exhibited anticancer activities with excellent IC50 and IG50 (4–10). On the other hand, pyrazole and pyrazole derivatives have drawn great attention of the researchers through the past few decades due to their high therapeutic importance as anti-inflammatory (11), antiglaucoma (12), antiviral (13), antimicrobial (14), antidiabetic (15) activities, etc. Moreover, pyrazole prodrugs have also been reported to possess significant anticancer activity (16–20). Also, fused phthalazines are considered as effective therapeutically active compounds; they possess a wide range of pharmaceutical applications such as anticancer (21, 22), anticonvulsant (23, 24), antimicrobial (25), antifungal (26) and anti-inflammatory (27) activities. Hence, the development of new methods for the synthesis of pyrazoles, triazoles and phthalazines continues to be an active area of research. Nevertheless, multi-component reactions were considered as an excellent tool for synthesis of complex heterocycles owing to their advantages of the structure diversity, simpler procedures, intrinsic atom economy, energy saving and reduced waste (28–34).
Pharmacoinformatics-based strategy in designing and profiling of some Pyrazole analogues as novel hepatitis C virus inhibitors with pharmacokinetic analysis
Published in Egyptian Journal of Basic and Applied Sciences, 2023
Stephen Ejeh, Adamu Uzairu, Gideon A. Shallangwa, Stephen E. Abechi, Muhammad Tukur Ibrahim
Pyrazoles are nitrogen-containing five-membered heterocyclic molecules that are well-known. Historically, nitrogen-containing molecules and their analogues have proved extremely useful as medicinal treatments. Pyrazole and their analogues are the most potent bioactive classes, with a variety of biochemical actions and its ring is an important synthesis pathway in the pharmaceutical sector because of its broad variety of biological effects. Several medications have a heterocyclic moiety as their primary structure [15,16].