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149 Results for Members

Members

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

Researchers at the Faculty of Science and Faculty of Health Sciences of the University of Bamenda pursue...

The Massachusetts General Hospital is a teaching hospital for Harvard University’s medical school and have...

The University of Ghana has a holistic approach to research, innovation and development - focusing on research...

The South African Medical Research Council (SAMRC) has a mandate to improve the health of the country’s...

Researchers at the University of Kansas, and in particular the KU Medical Center, work across a broad range of...

162 Results for Collaborations

Collaborations

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.

A LSTM researcher provided a UCSF researcher with stool and plasma samples from Trichuris-infected children from Ecuador. The UCSF researcher compared the amount of specific factors present in infected vs. uninfected samples.

A McGill University researcher provided a UBC researcher with frozen cell extracts of Cryptosporidium infected cells. The UBC researcher used these extracts to identify potential antigens for use in a vaccine.

A McGill University researcher will provide a UBC researcher with frozen cell extracts of T. cruzi infected cells. The UBC researcher will use these extracts to identify potential antigens for use in a vaccine.

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.