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157 Results for Members

Members

The Congolese Foundation for Medical Research (FCRM) was created in November 2008. Its mission is to...

FIND (Foundation for Innovative New Diagnostics) is an international non-profit organization that enables the...

The Global Alliance for Livestock Veterinary Medicines (GALVmed), formerly the Global Alliance for Livestock...

Paris-Sud University is dedicated to high-level research, focused on understanding the world, backing student...

The Malaria Consortium focuses on six main disease areas, creating tailored, evidence-based solutions that...

The University of Bamako, through its Faculty of Medicine, conducts research on and offers special training in...

166 Results for Collaborations

Collaborations

Johnson & Johnson Research & Development will provide a University of Toronto researcher with its Jump-stARter library. The researcher will screen the library against C. elegans to identify inhibitors of a unique metabolic pathway found in parasitic worms.

Johnson & Johnson Research & Development will provide WEHI researchers with its Jump-stARter library to screen against P. falciparum in vitro.

Johnson & Johnson Research & Development will provide a Washington University in St. Louis (WUSTL) researcher with its Jump-stARter library to screen against a Mycobacterium tuberculosis enzyme demonstrated to be essential for the growth and virulence of the bacterium.

KCCR and Northeastern University researchers explored grant opportunities together, developed exchange between students, and conducted collaborative lab projects.

A KCCR researcher provided Stanford University researchers with stool samples to support the researchers’ helminth diagnostic product development and testing.

University of Kansas developed formulations of Kineta’s antiviral.

170 Results for Assets

Assets

Hit-to-Lead Data, synthesis and assessment of buparvaquone prodrugpravaquone has been shown to be active agrainst VL (visceral leishmaniasis). I's in vivo activity appeared to be limited due to its poor solubility.
Data from Hit to Lead series against human African trypanosomiasis including in vitro activity and early ADME properties. The majority of compounds released in this dataset from DNDi of 4926 compounds were identified by screening of combinatorial libraries of two structural classes, 2-aryl-5-aminomethyloxazoles and N-substituted pyridylamidoximes, prepared by SCYNEXIS, Inc. for in vitro activity against Trypanosoma brucei. Based on activity observed in these screening activities, Hit-to-Lead and Lead Optimization programs were conducted opposite these two series and additional SAR was developed for in vitro anti-parasitic activity, physicochemical and in vitro ADME properties. Work in both series was suspended upon determination that the structural requirements for good in vitro anti-parasitic activity were inconsistent with structural requirements for good potential for in vivo activity. More specifically, in both series, compounds with good in vitro anti-parasitic activity tended to be lipophilic, metabolically unstable and of limited aqueous solubility. In addition to these two series, a number of small sets of compounds based on reported in vitro parasitic activity are reported, such as the pyrazolopyrimidines series. These compounds were found to be poorly selective for in vitro anti-parasitic activity and were cytotoxic in mammalian cells, hence were not further pursued.
Fenarimol as starting point for SAR investigations aimed at improving activity against T.cruzi and developing compounds suitable for in vivo characterisation. Lead Optimization of the fenarimol series for the treatment of Chagas disease SAR studies of triaryl scaffold led to the preparation of very active, low nM, easily synthesized T. cruzi inhibitors. Physicochemical and PK profiling as part of the optimisation cycle facilitated rapid identification of compounds suitable for profiling in infected mouse models. The lead compound supressed parasitemia to negligible levels after daily dosing for 20 days. Further optimisation of medicinal chemistry parameters such as oral exposure and selectivity over the CyP3A4/5 receptor linked to adverse drug-drug interactions in man and a limitation of the 'conazole' family of human anti-fungals was limited within the triaryl framework of the initial hit. A scaffold-hopping exercise was undertaken to explore further SAR opportunities to address these issues. Replacement of one aromatic ring by a variety of cyclic amines led to the discovery of an extensive family of novel, potent T.cruzi inhibitors.
Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei BS427 by a whole cell viability based high-throughput screening campaign. DNDi data is made available herewith freely to third parties. Use of these data anywhere in the world is therefore not subject to any licensing terms.
Selection and optimisation of hits from a high throughput phenotypic screen against Trypanosoma cruzi: HTS follow-up and early Lead Optimisation. Keenan et al. Selection and optimisation of hits from a high throughput phenotypic screen against Trypanosoma cruzi.