Microwave assisted synthesis, antimalarial screening and structure–activity-relationship exploration of some phenylthiazolyl-triazine derivatives against dihydrofolate reductase
作者： Supriya Sahu Supriya Sahu , SK Ghosh , Anirban Ghoshal Anirban Ghoshal , Junmoni Kalita Junmoni Kalita , Prashant Gahtori Prashant Gahtori
DOI: 10.1007/S00044-016-1714-8
关键词: In vitro 、 Docking (molecular) 、 Structure–activity relationship 、 Triazine 、 Thiazole 、 Chemistry 、 Plasmodium falciparum 、 Wild type 、 Dihydrofolate reductase 、 Stereochemistry 、 General Pharmacology, Toxicology and Pharmaceutics 、 Organic chemistry
摘要: 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 structural requirement existing antimalarial antifolates. A comparative analysis revealed that compounds synthesized using procedure gave better yield and minimized reaction time with respect conventional procedure. Hybrid screened for their in vitro activity against chloroquine-sensitive (3D-7) strain Plasmodium falciparum at 5 µg/mL 50 µg/mL dose level. An insight into structure–activity-relationship gained by docking them crystal structure wild type dihydrofolate reductase-thymidylate synthase.
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