Microwave assisted synthesis, antimalarial screening and structure-activity-relationship exploration of some phenylthiazolyl-triazine derivatives against dihydrofolate reductase

作者：Sahu Supriya^*; Ghosh Surajit K; Ghoshal Anirban; Kalita Junmoni; Gahtori Prashant; Bhattacharyya Divya R

来源：Medicinal Chemistry Research, 2016, 25(12): 2916-2923.

DOI：10.1007/s00044-016-1714-8

• Microwave
• Thiazole
• Triazine
• Antimalarial
• Docking

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 A mu g/mL and 50 A mu g/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.

• 出版日期2016-12