The present disclosure relates to a macrolide compound as shown by formula I and pharmaceutically acceptable salt thereof. The compound of the present disclosure is an antibacterial agent, and can be used to treat various bacterial and protozoal infections. The present disclosure further relates to the preparation method of the compound and a pharmaceutical composition thereof. ##STR00001##

The invention relates to the synthesis of a therapeutic agent which is effective against American trypanosomiasis (Chagas disease) caused by the protozoa Tripanosoma cruzi and transmitted by blood-sucking insects of the genera Triatoma or Rhodnius. This synthesis method is carried out in one step, in a solid state. It is a clean, simple, economical, rapid, easily implemented method, does not involve acid or base catalysts in the synthesis process, and is also environmentally friendly. It is a synthesis method for producing N-benzyl-2-(2-nitro-1-H-imidazol-1-yl)acetamide from the N-benzyl-2-hydroxyacetamide and 2-nitro-1H-imidazol reaction mixture, using microwave irradiation as an activation source in order to produce the N-benzyl-2-(2-nitro-1H-imidazol-1-yl)acetamide.

The invention pertains to ligands that bind to CD81 and that inhibit or block Plasmodium attachment to CD81, compositions and methods for preventing, inhibiting or treating infection by Plasmodium and ligands that target a Plasmodium binding site on CD81 and methods of making and using them. A series of ligand binding sites on the large extracellular loop of the open conformation of CD81 have been identified. Several important sites were located in regions identified by mutational studies to be the site of Plasmodium binding. Ligands that recognize these sites were identified. Linking together two or three ligands that bind with low or moderate affinities to different structurally unique sites on a target protein were used to generate small molecule ligand conjugates that exhibit very high affinities to their CD81 targets. Hybrid ligand molecules were also designed using fragment-based drug design methods to generate analogs of the ligands that bind more tightly to the protein than the parent compounds. Identification and design of groups of compounds that bind to CD81 for use as therapeutics for treating patients infected by Plasmodium and pathogens that interact with CD81. By binding to CD81, these molecules can block 1) Plasmodium attachment and entry into cells (infection), especially hepatocytes; 2) block or inhibit inflammatory responses caused by Plasmodium, and 3) block or inhibit the induction of other pathologies associated with Plasmodium infection.

Provided is a protein having Toxoplasma immunogenicity, the protein being a cyclophilin mutant protein and consisting of the amino acid sequence as shown in SED 2. Further provided is a nucleic acid that may encode a protein having Toxoplasma immunogenicity, which has the nucleic acid sequence as shown in SEQ ID NO. 1. Further provided is a vaccine, which is obtained by double-digesting a Toxoplasma antigen gene and then linking the same to a prokaryotic expression vector such as pET28a, and transforming the same into a prokaryotic expression engineering strain such as BL21(DE3), thereby inducing the high-efficiency expression thereof, wherein the inducing the high-efficiency expression thereof, wherein the purified protein is a soluble protein which maintains specific immunogenicity thereof.

Provided is a protein having Toxoplasma immunogenicity, the protein being a cyclophilin mutant protein and consisting of the amino acid sequence as shown in SED 2. Further provided is a nucleic acid that may encode a protein having Toxoplasma immunogenicity, which has the nucleic acid sequence as shown in SEQ ID NO. 1. Further provided is a vaccine, which is obtained by double-digesting a Toxoplasma antigen gene and then linking the same to a prokaryotic expression vector such as pET28a, and transforming the same into a prokaryotic expression engineering strain such as BL21(DE3), thereby inducing the high-efficiency expression thereof, wherein the inducing the high-efficiency expression thereof, wherein the purified protein is a soluble protein which maintains specific immunogenicity thereof.

The invention relates inter alia to compounds of the general formula (I) ##STR00001##
in which the A.sub.1-A.sub.4, T, n, W, Q, R.sup.1 and B.sub.1-B.sub.4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.

The application relates to N-(4-fluoro-3-(6-(3-methylpyridin-2-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)phenyl)-2,4-dimethyloxazole-5-carboxamide (Compound I) fumaric acid co-crystals and X-ray amorphous complexes of Compound (I) and fumaric acid. The application also provides methods of making the same; pharmaceutical compositions comprising them; and their use in treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a kinetoplastid parasite, such as leishmaniasis, human African trypanosomiasis and Chagas disease.

##STR00001##

The present invention provides methods for modulating expression of endogenous cellular genes using recombinant zinc finger proteins.

The present disclosure provides genetically altered protozoan parasites comprising a mutation in a bradyzoite formation deficient 1 (BFD1) gene, wherein the mutation inhibits differentiation of the parasite into a bradyzoite. The genetically altered protozoan parasites can be utilized in vaccine compositions and in methods of treating apicomplexan parasite infection.

The present disclosure provides genetically altered protozoan parasites comprising a mutation in a bradyzoite formation deficient 1 (BFD1) gene, wherein the mutation inhibits differentiation of the parasite into a bradyzoite. The genetically altered protozoan parasites can be utilized in vaccine compositions and in methods of treating apicomplexan parasite infection.