Abstract: The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.

Abstract: The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo.

Abstract: The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.

Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo.

Abstract: 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 I A—X—B wherein 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═C—C(═O)—. These compositions and methods have particular utility in the treatment of schistosomiasis, malaria and other infectious diseases.

Abstract: 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 IA--X--Bwherein A is a substituted or unsubstituted homoaromatic ring system comprising one to three rings which bind 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 bind 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.

Abstract: Compositions and methods for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease. The compositions comprise at least one metazoan protease inhibitor which binds to the S2 subsite and at least one of the S1 and S1' subsites of the metazoan parasite protease. The methods comprise administration to a patient infected with a metazoan parasite of at least one metazoan protease inhibitor in an amount effective to inhibit the protease of the metazoan parasite, thereby killing the parasite.

Abstract: The invention relates to synthetic tetrapeptides that contain a peptide blocking group at the amino terminus and an enzyme inhibitor at the carboxy terminus, and their use in the prevention of schistosome parasite infection.

Abstract: The present invention is a composition of matter composed essentially of a purified homogeneous thiol proteinase secreted by Entamoeba histolytica trophozoites. In purified homogeneous form the neutral thiol proteinase has a subunit molecular weight of about 56,000.+-.4,000, a neutral pH optimum, and an isoelectric point of about 6. The purified neutral thiol proteinase of the present invention can be obtained by using anion exchange and chromatofocusing Fast Protein Liquid Chromatography (FPLC) to purify the major neutral proteinase from secretions of axenically cultured Entamoeba histolytica trophozoites.The homogeneous neutral thiol proteinase of the present invention is immunogenic. It is useful as a serodiagnostic reagent for identifying the presence of antibodies in the sera of individuals exposed to Entamoeba histolytica trophozoites. The purified homogeneous enzyme can be used in ELISA assays or in other standard immunoassays.