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Drug Design Strategies, Modes of Action, Synthesis and Industrial Challenges Behind Trifluoromethylated New Chemical Entities

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Open Access
Article Type Review Article
Subject Medicine Group
OCLC JBRES Record
Leitao EPT* and Sobral LMS
Issue: Volume5-Issue2
Pages: 159-213
Received: 2024-01-10
Accepted: 2024-02-13
Published: 2024-02-15

Abstract

Medicinal plants have been an inspiration source for developing new chemical entities, providing diverse chemical structures and modes of action for medicinal chemistry strategies. Modern medicinal chemistry approaches promote functional group changes to improve NCE’s biological activity. Incorporating the trifluoromethyl (-CF3) group into organic compounds is crucial in modern drug design. It may affect the compound's lipophilicity, solubility, stability, molecular conformation, and pKa, changes that may lead to the discovery of new medicines to treat diseases of our times. For this reason, this chemical transformation is currently a hot topic in the organic chemistry field. Chemists are competing to develop better methods to carry out this transformation efficiently, less hazardously, and cost-effectively. The high number of annual scientific publications on trifluoromethylation evidences the competition. This review profiles 21 trifluoromethylated New Chemical Entities (NCE) selected in December 2020 from the GlobalData database, mainly in late stages of clinical trials (Phase II and III) or already in the commercial phase, containing one or two -CF3 groups in para or meta positions of benzene, or a pyridine ring. Synthetic approaches, therapeutic applications, and manufacturing industrial challenges are provided.

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© 2024 Leitão EPT, et al. Distributed under Creative Commons CC-BY 4.0 Creative CommonsAttribution

How to cite this article

Leitao EPT, Sobral LMS. Drug Design Strategies, Modes of Action, Synthesis and Industrial Challenges Behind Trifl uoromethylated New Chemical Entities. J Biomed Res Environ Sci. 2024 Feb 15; 5(2): 159-213. doi: 10.37871/jbres1883, Article ID: JBRES1883, Available at: https://www.jelsciences.com/articles/jbres1883.pdf

Subject area(s)

Pharmaceutica Analytica ActaTherapeuticsPharmacology

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