Analogues of thiolactomycin as potential anti-malarial and anti-trypanosomal agents

Jones, Simon Mark, Urch, Jonathan E., Brun, Reto, Harwood, John L. ORCID: https://orcid.org/0000-0003-2377-2612, Berry, Colin ORCID: https://orcid.org/0000-0002-9943-548X and Gilbert, Ian H. 2004. Analogues of thiolactomycin as potential anti-malarial and anti-trypanosomal agents. Bioorganic & Medicinal Chemistry 12 (4) , pp. 683-692. 10.1016/j.bmc.2003.11.023

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Abstract

A series of analogues of the naturally occurring antibiotic thiolactomycin (TLM) have been synthesised and evaluated for their ability to inhibit the growth of the malaria parasite, Plasmodium falciparum. Thiolactomycin is an inhibitor of Type II fatty acid synthase which is found in plants and most prokaryotes, but not an inhibitor of Type I fatty acid synthase in mammals. A number of the analogues showed inhibition equal to or greater than TLM. The introduction of hydrophobic alkyl groups at the C3 and C5 positions of the thiolactone ring lead to increased inhibition, the best showing a fourteenfold increase in activity over TLM. In addition, some of the analogues showed activity when assayed against the parasitic protozoa, Trypanosoma cruzi and Trypanosoma brucei

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Biosciences Pharmacy
Publisher:	Elsevier
ISSN:	0968-0896
Last Modified:	25 Oct 2022 10:07
URI:	https://orca.cardiff.ac.uk/id/eprint/61173

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