Design and synthesis of guanylthiourea derivatives as potential inhibitors of Plasmodium falciparum dihydrofolate reductase enzyme

Legesse AdaneShweta BhagatMinhajul ArfeenSonam BhatiaRachada SirawarapornWorachart SirawarapornAsit K. ChakrabortiPrasad V. BharatamNational Institute of Pharmaceutical Education and Research India, MohaliMahidol University2018-11-092018-11-092014-01-15Bioorganic and Medicinal Chemistry Letters. Vol.24, No.2 (2014), 613-617146434050960894X2-s2.0-84891846323https://repository.li.mahidol.ac.th/handle/20.500.14594/33316A new class of compounds based on S-benzylated guanylthiourea has been designed as potential PfDHFR inhibitors using computer aided methods (molecular electrostatic potential, molecular docking). Several compounds in this class have been synthesized starting from guanylthiourea and alkyl bromides. In vitro studies showed that two compounds from this class are active with the IC50value of 100 μM and 400 nM. © 2013 Elsevier Ltd. All rights reserved.Mahidol UniversityBiochemistry, Genetics and Molecular BiologyChemistryPharmacology, Toxicology and PharmaceuticsDesign and synthesis of guanylthiourea derivatives as potential inhibitors of Plasmodium falciparum dihydrofolate reductase enzymeArticleSCOPUS10.1016/j.bmcl.2013.12.009