Inhibitors of the plasmodial surface anion channel as antimalarials
Inventors
Desai, Sanjay A. • Pillai, Ajay D.
Assignees
US Department of Health and Human Services
Publication Number
US-8618090-B2
Publication Date
2013-12-31
Expiration Date
2029-07-15
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Abstract
Disclosed are inhibitors of the plasmodial surface anion channel (PSAC) inhibitors and the use thereof in treating or preventing malaria in an animal such as a human, comprising administering an effective amount of an inhibitor or a combination of inhibitors. An example of such an inhibitor is a compound of formula I, Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein.
Core Innovation
The invention provides inhibitors of the plasmodial surface anion channel (PSAC) and their use in treating or preventing malaria in animals, including humans, by administering an effective amount of one or more of the specified compounds or their pharmaceutically acceptable salts. The compounds include those represented by certain chemical formulas, wherein various substituents are defined and may be combined in effective ways, including combinations of different compounds.
Malaria is a major infectious disease caused by Plasmodium parasites with significant health and economic impact worldwide, especially in African children under five years old. There currently is no effective vaccine, and existing antimalarial drugs face resistance. Thus, there is a need for new treatments that can overcome these challenges.
PSAC plays a key role in the malaria parasite's survival by modifying red blood cell permeability to essential nutrients. It is a unique channel with distinct properties and is located on the surface of infected red blood cells, which allows direct drug access and reduces the likelihood of resistance via drug extrusion. The invention targets PSAC with novel inhibitors that block nutrient uptake necessary for parasite growth, providing a method to prevent or treat malaria. Notably, combinations of these inhibitors exhibit synergistic parasite killing effects.
Claims Coverage
The patent includes one independent claim that defines a method for providing prophylaxis or treatment against malaria using specific compounds.
Use of compounds of formula I for malaria prophylaxis or treatment
Administering an effective amount of compounds of formula I with defined substituents or pharmaceutically acceptable salts to an animal to provide malaria prophylaxis or treatment.
The independent claim covers a method of administering effective amounts of specified compounds of formula I for malaria prevention or treatment, encompassing various defined substituents and including pharmaceutically acceptable salts.
Stated Advantages
The compounds used in combination exhibit synergistic killing of parasites, enhancing antimalarial efficacy beyond additive effects.
Documented Applications
Use of compounds of formulae I, IV, and V, alone or in combination, for the preparation of medicaments to prevent or treat malaria in animals, including humans.
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