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The Strathprints institutional repository is a digital archive of University of Strathclyde research outputs.

Strathprints serves world leading Open Access research by the University of Strathclyde, including research by the Strathclyde Institute of Pharmacy and Biomedical Sciences (SIPBS), where research centres such as the Industrial Biotechnology Innovation Centre (IBioIC), the Cancer Research UK Formulation Unit, SeaBioTech and the Centre for Biophotonics are based.

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Salicylanilide inhibitors of toxoplasma gondii

Fomovska, Alina and Wood, Richard and Mui, E. and Dubey, J.P. and Ferreira, Leandra and Hickman, Mark and Lee, Patricia and Leed, Susan and Auschwitz, Jennifer and Welsh, William and Sommerville, Caroline and Woods, Stuart and Roberts, Craig and Mcleod, Rima (2012) Salicylanilide inhibitors of toxoplasma gondii. Journal of Medicinal Chemistry, 55 (19). pp. 8375-8391. ISSN 0022-2623

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Abstract

Toxoplasma gondii ( T. gondii ) is an apicomplexan parasite that can cause eye disease, brain disease, and death, especially in congenitally infected and immune-compromised people. Novel medicines effective against both active and latent forms of the parasite are greatly needed. The current study focused on the discovery of such medicines by exploring a family of potential inhibitors whose antiapicomplexan activity has not been previously reported. Initial screening efforts revealed that niclosamide, a drug approved for anthelmintic use, possessed promising activity in vitro against T. gondii . This observation inspired the evaluation of the activity of a series of salicylanilides and derivatives. Several inhibitors with activities in the nanomolar range with no appreciable in vitro toxicity to human cells were identified. An initial structure-activity relationship was explored. Four compounds were selected for evaluation in an in vivo model of infection, and two derivatives with potentially enhanced pharmacological parameters demonstrated the best activity profiles.