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The Strathprints institutional repository is a digital archive of University of Strathclyde's Open Access research outputs. Strathprints provides access to thousands of Open Access research papers by University of Strathclyde researchers, including by researchers from the Department of Computer & Information Sciences involved in mathematically structured programming, similarity and metric search, computer security, software systems, combinatronics and digital health.

The Department also includes the iSchool Research Group, which performs leading research into socio-technical phenomena and topics such as information retrieval and information seeking behaviour.

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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.