Recent advances in the synthesis of pyrazoline derivatives from chalcones as potent pharmacological agents: A comprehensive review

• Published in: Results in Chemistry Vol. 7; p. 101326
• Main Authors: Shekhar Yadav, Chandra, Azad, Iqbal, Rahman Khan, Abdul, Nasibullah, Malik, Ahmad, Naseem, Hansda, Dhananjoy, Nusrat Ali, Saud, Shrivastav, Kajal, Akil, Mohd, Lohani, Minaxi B.
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01-01-2024; Elsevier
• Subjects: Anticancer; Antimalarial; Antimicrobial, Antitubercular; Antioxidant; Antiviral; Chalcones; Heterocyclic; Pyrazoline; Antimalarial; AAPH; MIC; MCF-7; EAC; MAO-B; Antioxidant; Pyrazoline; IL-6; Chalcones; Antimicrobial, Antitubercular; IC50; XO; K-562; Antiviral; Hep-G2; AID; Anticancer; Heterocyclic
• ISSN: 2211-7156; 2211-7156
• DOI: 10.1016/j.rechem.2024.101326

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The pyrazoline scaffold plays a vital role in heterocyclic chemistry as a fundamental building block in both organic and medicinal chemistry. A pyrazoline scaffold is composed of an endocyclic double bond, two nitrogen atoms, and five different types of bonds. It is a significant chemical fragment and exhibits various bioavailabilities, allowing the synthesis of a range of diverse compounds with promising biological potential. Over the past decade, extensive research efforts have been devoted to investigating the therapeutic potentials of pyrazoline scaffolds, encompassing their antibacterial, anti-inflammatory, analgesic, cytotoxic, and anti-tumor activities. Moreover, in the presence of a unique chemical structure, pyrazolines have made it easier to produce new substitutions with low toxicity as compared to their natural analogue. The current review focuses on the recent progress in the synthesis of pyrazoline scaffolds from chalcones, with an emphasis on their possible biological functions. The study identifies a diverse range of pyrazoline derivatives that exhibit promising biological properties and have been successfully reported in various studies. The primary objective is to determine the chemical groups and structural modifications that enhance their bioactivity, low toxicity, and handling. Furthermore, the review explores the bioavailability, synthetic challenges, and progress made in utilising pyrazoline derivatives in pharmaceutical and synthetic chemistry from 2017 to 2023. The different biological potentials of various substituted pyrazolines are reported here such as 1,4-dimethylpiperazine, 2-(2-methyl-1H-benzo[d]imidazol-1-yl)acetohydrazide, 1-methyl-4-phenylpiperazine, 4,5-dihydrooxazole, 2H-chromen-2-one, 2-(4-chlorophenyl)-5-methyl-4,5-dihydrooxazole, benzo[d]thiazole, ethoxybenzene, and 1-bromo-4N,N-dimethylaniline. The review also discusses the effects of different functional groups, such as OCH3, OH, NO2, CF3, and halogens, added to different positions of the pyrazoline scaffold.