Sign in
Back
Design and synthesis of guanylthiourea derivatives as potential inhibitors of Plasmodium falciparum dihydrofolate reductase enzyme
Journal article   Peer reviewed

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

Legesse Adane, Shweta Bhagat, Minhajul Arfeen, Sonam Bhatia, Rachada Sirawaraporn, Worachart Sirawaraporn, Asit K. Chakraborti and Prasad V. Bharatam
Bioorganic & medicinal chemistry letters, Vol.24(2), pp.613-617
15/01/2014
DOI: https://doi.org/10.1016/j.bmcl.2013.12.009
PMID: 24361001

Abstract

Chemistry Chemistry, Medicinal Chemistry, Organic Life Sciences & Biomedicine Pharmacology & Pharmacy Physical Sciences Science & Technology
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 IC50 value of 100 mu M and 400 nM. (C) 2013 Elsevier Ltd. All rights reserved.

Metrics

1 Record Views

Details