Target Guided Synthesis of 5-Benzyl-2,4-diamonopyrimidines: Their Antimalarial Activities and Binding Affinities to Wild Type and Mutant Dihydrofolate Reductases from Plasmodium falciparum

• Main Authors: Chawanee Sirichaiwat, Chakapong Intaraudom, Sumalee Kamchonwongpaisan, Jarunee Vanichtanankul, Yodhathai Thebtaranonth, Yongyuth Yuthavong
• Other Authors: Thailand National Center for Genetic Engineering and Biotechnology
• Format: Article
• Published: 2018
• Subjects: Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics
• Online Access: https://repository.li.mahidol.ac.th/handle/123456789/21232
• Institution: Mahidol University

The resistance to pyrimethamine (PYR) of Plasmodium falciparum arising from mutation at position 108 of dihydrofolate reductase (pfDHFR) from serine to asparagine (S108N) is due to steric interaction between the bulky side chain of N108 and C1 atom of the 5-p-C1 aryl group of PYR, which consequently...