Brad Sleebs

Optimisation of 2-(N-phenyl carboxamide) triazolopyrimidine antimalarials with moderate to slow acting erythrocytic stage activity.

Brodie L Bailey, William Nguyen, Anna Ngo, Christopher D Goodman, Maria R Gancheva, Paola Favuzza, Laura M Sanz, Francisco-Javier Gamo, Kym N Lowes, Geoffrey I McFadden, Danny W Wilson, Benoît Laleu, Stephen Brand, Paul F Jackson, Alan F Cowman, Brad E Sleebs

Journal article  |  2021  |  Bioorg Chem

Malaria is a devastating parasitic disease caused by parasites from the genus Plasmodium. Therapeutic resistance has been reported..

High-Throughput Phenotypic Assay to Screen for Anthelmintic Activity on Haemonchus contortus

Aya C Taki, Joseph J Byrne, Tao Wang, Brad E Sleebs, Nghi Nguyen, Ross S Hall, Pasi K Korhonen, Bill CH Chang, Paul Jackson, Abdul Jabbar, Robin B Gasser

Journal article  |  2021  |  PHARMACEUTICALS

Parasitic worms cause very significant diseases in animals and humans worldwide, and their control is critical to enhance health, ..

Late Stage Phosphotyrosine Mimetic Functionalization of Peptides Employing Metallaphotoredox Catalysis

Hao Chen, Runyu Mao, Martin Brzozowski, Nghi H Nguyen, Brad E Sleebs

Journal article  |  2021  |  ORGANIC LETTERS

Access to phosphotyrosine (pTyr) mimetics requires multistep syntheses, and therefore late stage incorporation of these mimetics i..

Optimization of Benzothiazole and Thiazole Hydrazones as Inhibitors of Schistosome BCL-2

William Nguyen, Erinna F Lee, Marco Evangelista, Mihwa Lee, Tiffany J Harris, Peter M Colman, Nicholas A Smith, Luke B Williams, Kate E Jarman, Kym N Lowes, Cecile Haeberli, Jennifer Keiser, Brian J Smith, W Douglas Fairlie, Brad E Sleebs

Journal article  |  2021  |  ACS INFECTIOUS DISEASES

Limited therapeutic options are available for the treatment of human schistosomiasis caused by the parasitic Schistosoma flatworm...

Three Small Molecule Entities (MPK18, MPK334 and YAK308) with Activity against Haemonchus contortus In Vitro

Aya C Taki, Abdul Jabbar, Thomas Kurz, Beate Lungerich, Guangxu Ma, Joseph J Byrne, Marc Pflieger, Yodita Asfaha, Fabian Fischer, Bill CH Chang, Brad E Sleebs, Robin B Gasser

Journal article  |  2021  |  MOLECULES

Due to widespread multi-drug resistance in parasitic nematodes of livestock animals, there is an urgent need to discover new anthe..

Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion

William Nguyen, Madeline G Dans, Anna Ngo, Maria R Gancheva, Ornella Romeo, Sandra Duffy, Tania F de Koning-Ward, Kym N Lowes, Helene Jousset Sabroux, Vicky M Avery, Danny W Wilson, Paul R Gilson, Brad E Sleebs

Journal article  |  2021  |  EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The emerging resistance to combination therapies comprised of artemisinin derivatives has driven a need to identify new antimalari..

Development of an automated assay for accelerated in vitro detection of DNA adduct-inducing and crosslinking agents

Jelena Medan, Brad E Sleebs, Kurt Lackovic, Keith G Watson, Benny J Evison, Don R Phillips, Suzanne M Cutts

Journal article  |  2021  |  BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Current techniques for the identification of DNA adduct-inducing and DNA interstrand crosslinking agents include electrophoretic c..

Synthesis of Acyl Phosphoramidates Employing a Modified Staudinger Reaction

Iain Currie, Brad E Sleebs

Journal article  |  2021  |  ORGANIC LETTERS

A one-step synthesis of acyl phosphoramidates from a variety of functionalized acyl azides has been developed employing trimethyls..

Advances in the discovery and development of anthelmintics by harnessing natural product scaffolds.

HMP Dilrukshi Herath, Aya C Taki, Brad E Sleebs, Andreas Hofmann, Nghi Nguyen, Sarah Preston, Rohan A Davis, Abdul Jabbar, Robin B Gasser

Journal article  |  2021  |  Adv Parasitol

Widespread resistance to currently-used anthelmintics represents a major obstacle to controlling parasitic nematodes of livestock ..

Development and application of a high-throughput screening assay for identification of small molecule inhibitors of the P. falciparum reticulocyte binding-like homologue 5 protein

Brad E Sleebs, Kate E Jarman, Sonja Frolich, Wilson Wong, Julie Healer, Weiwen Dai, Isabelle S Lucet, Danny W Wilson, Alan F Cowman

Journal article  |  2020  |  INTERNATIONAL JOURNAL FOR PARASITOLOGY-DRUGS AND DRUG RESISTANCE

The P. falciparum parasite, responsible for the disease in humans known as malaria, must invade erythrocytes to provide an environ..