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Title: Design and synthesis of guanylthiourea derivatives as potential inhibitors of Plasmodium falciparum dihydrofolate reductase enzyme
Authors: Legesse Adane
Shweta Bhagat
Minhajul Arfeen
Sonam Bhatia
Rachada Sirawaraporn
Worachart Sirawaraporn
Asit K. Chakraborti
Prasad V. Bharatam
National Institute of Pharmaceutical Education and Research India, Mohali
Mahidol University
Keywords: Biochemistry, Genetics and Molecular Biology;Chemistry;Pharmacology, Toxicology and Pharmaceutics
Issue Date: 15-Jan-2014
Citation: Bioorganic and Medicinal Chemistry Letters. Vol.24, No.2 (2014), 613-617
Abstract: A 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.
ISSN: 14643405
Appears in Collections:Scopus 2011-2015

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