Product name
Therapy of trypanosome infectionsSummary
Synthetic compounds active against selected protozoae and with almost immeasureable mamalian cytotoxicityOrganization name
IMG Innovations-Management GmbHProfile
Up to 50,000 deaths are registered yearly although Chagas disease is curable if treatment occurs in the acute phase. In addition, severe side effects can be associated with commercially available Chagas therapeutics (Benznidazole, Nifurtimox); vaccines or other methods of Chagas prophylaxis are unknown.
Natural compounds with naphthalene or biphenyl substructures and interesting, pharmaceutically useful properties (e.g. naphthyl isoquinolines) have often been isolated from marine as well as terrestrial organisms in the past. They served as models for two compound classes, which are easily accessible by total synthesis and for which pronounced activities against trypanosomes have been found in cell vitality assays.
Advantages
- Simple totally synthetic procedures giving high yields; compatible with various substitution patterns and therefore appropriate for the synthesis of larger compound libraries
- Synthesis can be carried out atropo-selectively; any unwanted atropoisomeric side product can be recovered, if necessary
- Distinct in vitro activity of the lead structure (IC50 = 4.7 μM)
- Significant specificity against selected protozoae; almost immeasurable cytotoxicity of the lead structure toward non-infected mammalian cells
- Partially additional activity against leishmaniasis or antiviral activity (for trypanosomial secondary infection as a result of low immunity, e.g. after HIV primary infection)
- As low-molecular-weight natural compound for chemical defence purposes expectedly good "drug likeness"
- Scalable procedures to chemically synthesise the enantiomerically pure pharmaceutical agents
- Quantitative structure-activity profiles of a multitude of variously substituted derivatives against infected rat L-6 myoblasts
Patents granted, additional applications pending. This product is offered by IMG.
Contact
Dr. Andreas Kirschfeld
kirschfeld(at)img-rlp.de
About IMG
The IMG Innovations-Management GmbH is a subsidiary of the Investment and Economic Development Bank of Rhineland-Palatinate GmbH. It offers a multitude of services for the realisation and commercialisation of innovations and inventions including intellectual property protection and license brokerage. It is the primary contact point regarding all matters of technology and knowledge transfer within the German state of Rhineland-Palatinate. Within the framework of the Scientific Patent Network Rhineland-Palatinate it forms the connection between scientists and university administrations and provides universities and research institutions with all prerequisites to bring research results to the market on a fast track. Within the Scientific Patent Network the IMG is the leading service provider offering as a proficient partner a professional intellectual property management to all associated universities and institutions.
Description File
UMZ013_016_chagas_e2a47a635.pdf
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