TY - JOUR
T1 - Fluorinated scaffolds for antimalarial drug discovery
AU - Upadhyay, Charu
AU - Chaudhary, Monika
AU - De Oliveira, Ronaldo N.
AU - Borbas, Aniko
AU - Kempaiah, Prakasha
AU - Singh, Poonam
AU - Rathi, Brijesh
N1 - Funding Information:
The Science and Engineering Research Board, Government of India, is acknowledged for financial support [ECR/2015/000478]. The Department of Science and Technology, Government of India, is also acknowledged for the financial support (DST/TDT/AGRO-54/2019). Finally, C Upadhyay is very thankful to the Council of Scientific and Industrial Research (CSIR), New Delhi, for providing financial assistance with whom she is a Junior Research Fellow.
Publisher Copyright:
© 2020, © 2020 Informa UK Limited, trading as Taylor & Francis Group.
PY - 2020/6/2
Y1 - 2020/6/2
N2 - Introduction: The unique physicochemical properties and chemical diversity of organofluorine compounds have remarkably contributed for their wide utility in the area of pharmaceuticals, materials and agrochemicals. The noteworthy characteristics of fluorine include high electron affinity, lipophilicity and bioavailability, extending the half-life of the drugs. The incorporation of fluorine substituents, particularly trifluoromethyl groups, into organic molecules has led to their high potency against various diseases, including malaria. Hence, organofluorinated molecules offer valuable avenues for the design of new drug candidates against malaria. Areas covered: In this review, the authors discuss the importance of fluorine substituents present in the chemical compounds, and their potential applications for antimalarial drug discovery. Expert opinion: Fluorinated molecules represent a reliable strategy to develop new antimalarial drugs. Fluorine or fluorinated groups have been identified as a promising precursor, and their presence in approximately twenty-five percent of approved drugs is notable. Selective fluorination of chemical entities has the potential to be applied not only to improve the activity profile against the malaria parasite, but could be extrapolated for favorable pharmacological applications. Hazardous reagents such as HF, F2 and SF4 used for fluorination, are not considered as safe, and therefore, this process remains challenging, particularly for the pharmaceutical industry.
AB - Introduction: The unique physicochemical properties and chemical diversity of organofluorine compounds have remarkably contributed for their wide utility in the area of pharmaceuticals, materials and agrochemicals. The noteworthy characteristics of fluorine include high electron affinity, lipophilicity and bioavailability, extending the half-life of the drugs. The incorporation of fluorine substituents, particularly trifluoromethyl groups, into organic molecules has led to their high potency against various diseases, including malaria. Hence, organofluorinated molecules offer valuable avenues for the design of new drug candidates against malaria. Areas covered: In this review, the authors discuss the importance of fluorine substituents present in the chemical compounds, and their potential applications for antimalarial drug discovery. Expert opinion: Fluorinated molecules represent a reliable strategy to develop new antimalarial drugs. Fluorine or fluorinated groups have been identified as a promising precursor, and their presence in approximately twenty-five percent of approved drugs is notable. Selective fluorination of chemical entities has the potential to be applied not only to improve the activity profile against the malaria parasite, but could be extrapolated for favorable pharmacological applications. Hazardous reagents such as HF, F2 and SF4 used for fluorination, are not considered as safe, and therefore, this process remains challenging, particularly for the pharmaceutical industry.
KW - Antimalarials
KW - drug Discovery
KW - fluorinated artemisinin
KW - lipophilicity
KW - organofluorinated
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U2 - 10.1080/17460441.2020.1740203
DO - 10.1080/17460441.2020.1740203
M3 - Review article
C2 - 32202162
AN - SCOPUS:85082412209
SN - 1746-0441
VL - 15
SP - 705
EP - 718
JO - Expert Opinion on Drug Discovery
JF - Expert Opinion on Drug Discovery
IS - 6
ER -