Compositions and methods for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease, wherein there is employed at least one compound of formula Iwherein A is a substituted or unsubstituted homoaromatic or heteroaromatic ring system comprising one to three rings which binds to at least one of the S2, S1 and S1' subsites; B is a substituted or unsubstituted homoaromatic or heteroaromatic ring system comprising one to three rings which binds to at least one of the S1', S1 and S2 subsites; and X is --C.dbd.C--C(.dbd.O)--. These compositions and methods have particular utility in the treatment of schistosomiasis, malaria, and other infectious diseases.

The Regents of the University of California

Inhibitors of metazoan parasite proteases

Compositions and methods are disclosed for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease, wherein there is employed at least one compound of formula Iwherein A is a substituted or unsubstituted heteroaromatic ring system comprising one to three rings which binds to at least one of the S2, S1 and S1' subsites; B is a substituted or unsubstituted homoaromatic ring system comprising one to three rings which binds to at least one of the S1', S1 and S2 subsites; and X is --C.dbd.C--C(.dbd.O)--. These compositions and methods have particular utility in the treatment of schistosomiasis, malaria and other infectious diseases.

Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.

schistosomiasis/protease

Inhibitors of metazoan parasite proteases

Inhibitors of metazoan parasite proteases

Cysteine protease inhibitors for the treatment of parasitic diseases

O mais completo banco de dados de ervas medicinais apoiado pela ciência