• Design, synthesis and biological evaluation of 6-aryl-1,6-dihydro-1,3,5-triazine-2,4-diamines as antiplasmodial antifolates

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Metadata

Document Title

Design, synthesis and biological evaluation of 6-aryl-1,6-dihydro-1,3,5-triazine-2,4-diamines as antiplasmodial antifolates

Author

Lourens A.C.U.,Gravestock D.,Van Zyl R.L.,Hoppe H.C.,Kolesnikova N.,Taweechai S.,Yuthavong Y.,Kamchonwongpaisan S.,Rousseau A.L.

Name from Authors Collection

Lourens A.C.U.

Scopus Author ID

9037874300

ORCID ID

NULL

|

Gravestock D.

Scopus Author ID

6601974350

ORCID ID

NULL

|

Van Zyl R.L.

Scopus Author ID

6602539536

ORCID ID

NULL

|

Hoppe H.C.

Scopus Author ID

7103057362

ORCID ID

NULL

|

Kolesnikova N.

Scopus Author ID

24598082400

ORCID ID

NULL

|

Taweechai S.

Scopus Author ID

8253792700

ORCID ID

0000-0001-8286-1645

|

Yongyuth Yuthavong

Scopus Author ID

7005468673

ORCID ID

NULL

|

Sumalee Kamchonwongpaisan

Scopus Author ID

6603458235

ORCID ID

0000-0002-4723-5232

|

Rousseau A.L.

Scopus Author ID

7102240792

ORCID ID

NULL

Affiliations

CSIR Biosciences Meiring Naude Road Pretoria, Gauteng, 0001, South Africa; Pharmaceutical Chemistry, School of Pharmacy, North-West University, Private Bag X6001, Potchefstroom, 2520, South Africa; Syngenta, Jealott's Hill International Research Centre, Bracknell-Berkshire, RG42 6EY, United Kingdom; Pharmacology Division, Department of Pharmacy and Pharmacology, WITS Research Institute for Malaria (WRIM), Faculty of Health Sciences, University of the Witwatersrand, 7 York Road, Parktown, 2193, South Africa; Department of Biochemistry and Microbiology, Rhodes University, Grahamstown, 6140, South Africa; BIOTEC, National Science and Technology Development Agency Thailand Science Park, Pathumthani, 12120, Thailand; Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, Private Bag 3 PO WITS 2050, South Africa

Type

Article

Source Title

Organic and Biomolecular Chemistry

ISSN

14770520

Year

2016

Volume

14

Issue

33

Page

7899-7911

Open Access

All Open Access, Hybrid Gold, Green

Publisher

Royal Society of Chemistry

DOI

10.1039/c6ob01350c

Abstract

The design, synthesis and biological evaluation of a series of 6-aryl-1,6-dihydro-1,3,5-triazine-2,4-diamines is described. These compounds exhibited in vitro antiplasmodial activity in the low nanomolar range against both drug sensitive and drug resistant strains of P. falciparum, with 1-(3-(2,4-dichlorophenoxy)propyl)-6-phenyl-1,6-dihydro-1,3,5-triazine-2,4-diamine hydrochloride identified as the most potent compound from this series against the drug resistant FCR-3 strain (IC50 2.66 nM). The compounds were not toxic to mammalian cells at therapeutic concentrations and were shown to be inhibitors of parasitic DHFR in a biochemical enzyme assay. © 2016 The Royal Society of Chemistry.

Industrial Classification

N/A

Knowledge Taxonomy Level 1

Chemical Science

Knowledge Taxonomy Level 2

Chemistry

Knowledge Taxonomy Level 3

Chemistry

License

CC BY

Rights

Author

Publication Source

Scopus

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