Synthesis and evaluation of α-thymidine analogues as novel antimalarials

…, KS Wilson, D González-Pacanowska…

Index: Cui, Huaqing; Carrero-Lerida, Juana; Silva, Ana P. G.; Whittingham, Jean L.; Brannigan, James A.; Ruiz-Perez, Luis M.; Read, Kevin D.; Wilson, Keith S.; Gonzalez-Pacanowska, Dolores; Gilbert, Ian H. Journal of Medicinal Chemistry, 2012 , vol. 55, # 24 p. 10948 - 10957

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Citation Number: 18

Abstract

Plasmodium falciparum thymidylate kinase (Pf TMPK) is a key enzyme in pyrimidine nucleotide biosynthesis. 3-Trifluoromethyl-4-chloro-phenyl-urea-α-thymidine has been reported as an inhibitor of Mycobacterium tuberculosis TMPK (Mt TMPK). Starting from this point, we designed, synthesized and evaluated a number of thymidine analogues as antimalarials. Both 5′-urea-α-and β-thymidine derivatives were moderate inhibitors of Pf ...