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

1

Issued Date

2014-01-15

Resource Type

Article

ISSN

14643405
0960894X

DOI

10.1016/j.bmcl.2013.12.009

Other identifier(s)

2-s2.0-84891846323

Rights

Mahidol University

Rights Holder(s)

SCOPUS

Bibliographic Citation

Bioorganic and Medicinal Chemistry Letters. Vol.24, No.2 (2014), 613-617

Suggested Citation

Legesse Adane, Shweta Bhagat, Minhajul Arfeen, Sonam Bhatia, Rachada Sirawaraporn, Worachart Sirawaraporn, Asit K. Chakraborti, Prasad V. Bharatam Design and synthesis of guanylthiourea derivatives as potential inhibitors of Plasmodium falciparum dihydrofolate reductase enzyme. Bioorganic and Medicinal Chemistry Letters. Vol.24, No.2 (2014), 613-617. doi:10.1016/j.bmcl.2013.12.009 Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/33316

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Title

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

Author(s)

Legesse Adane
 Shweta Bhagat
 Minhajul Arfeen
 Sonam Bhatia
 Rachada Sirawaraporn
 Worachart Sirawaraporn
 Asit K. Chakraborti
 Prasad V. Bharatam

Other Contributor(s)

National Institute of Pharmaceutical Education and Research India, Mohali
 Mahidol University

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.

Keyword(s)

Biochemistry, Genetics and Molecular Biology
 Chemistry
 Pharmacology, Toxicology and Pharmaceutics

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URI

https://repository.li.mahidol.ac.th/handle/123456789/33316

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