Abstract
In this study, a microwave-assisted methodology was first attempted to facilitate the synthesis of hybrid phenylthiazolyl-triazine derivatives. These two nuclei were clubbed together based on the structural requirement of existing antimalarial antifolates. A comparative analysis revealed that compounds synthesized using microwave-assisted procedure gave better yield and minimized the reaction time with respect to the conventional procedure. Hybrid compounds were screened for their in vitro antimalarial activity against chloroquine-sensitive (3D-7) strain of Plasmodium falciparum at 5 µg/mL and 50 µg/mL dose level. An insight into the structure–activity-relationship of the synthesized compounds was gained by docking them in the crystal structure of wild type Plasmodium falciparum dihydrofolate reductase-thymidylate synthase.
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Acknowledgment
The financial support from the Department of Biotechnology (DBT), New Delhi, India is gratefully acknowledged [grant no. BCIL/NER-BPMC/2013-541 (BT/330/NE/TBP/2012 dated 29 April 2013)] and the authors also are thankful to S.A.I.F., Punjab University, Chandigarh, India for providing spectroscopic data.
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Sahu, S., Ghosh, S.K., Ghoshal, A. et al. Microwave assisted synthesis, antimalarial screening and structure–activity-relationship exploration of some phenylthiazolyl-triazine derivatives against dihydrofolate reductase. Med Chem Res 25, 2916–2923 (2016). https://doi.org/10.1007/s00044-016-1714-8
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DOI: https://doi.org/10.1007/s00044-016-1714-8