Abstract: The invention provides methods and compositions for inhibiting CD38 activity, and methods of treating or preventing various disorders associated with CD38 activity.

Abstract: Compounds of formula (I) or formula (II), compositions and methods useful for treating and/or preventing a fungal infections are provided. wherein the substituents are as defined in the appended claims.

Abstract: The invention provides methods and compositions for inhibiting CD38 activity, and methods of treating or preventing various disorders associated with CD38 activity.

Abstract: The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)—The values and preferred values of the variables in Structural Formula I are defined herein.

Abstract: The invention provides methods and compositions for inhibiting CD 38 activity, and methods of treating or preventing various disorders associated with CD38 activity.

Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.

Abstract: The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)—The values and preferred values of the variables in Structural Formula I are defined herein.

Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.

Abstract: One aspect of the present invention relates to a polymeric material. The invention also relates to a method of making the aforementioned polymer comprising extracting a fungus, wherein the fungus is, for example, an endophytic fungus, such as CR873. The invention further relates to a bioplastic composition comprising the aforementioned polymer.

Abstract: Disclosed are triaryl cationic compounds that exhibit broad spectrum antibiotic and antifungal activity, pharmaceutical compositions containing the compounds, and methods of treating bacterial and fungal infections using the compounds. The compounds were initially isolated by screening a 25,000-member bacterial artificial chromosome (BAC) library of environmental (eDNA) from soil. At least one clone produced a dark brown melanin-like compound that was found to have antibiotic activity. The compounds were isolated and synthesized de novo. From within the positive clone, a single open reading frame that shares extensive sequence similarity with members of the 4-hydroxyphenylpyruvate family of enzymes was found to be necessary and sufficient to confer the production of at least one of the subject compounds on E. coli.

Abstract: Disclosed are triaryl cationic compounds that exhibit broad spectrum antibiotic and antifungal activity, pharmaceutical compositions containing the compounds, and methods of treating bacterial and fungal infections using the compounds. The compounds were initially isolated by screening a 25,000-member bacterial artificial chromosome (BAC) library of environmental (eDNA) from soil. At least one clone produced a dark brown melanin-like compound that was found to have antibiotic activity. The compounds were isolated and synthesized de novo. From within the positive clone, a single open reading frame that shares extensive sequence similarity with members of the 4-hydroxyphenylpyruvate family of enzymes was found to be necessary and sufficient to confer the production of at least one of the subject compounds on E. coli.

Abstract: The invention relates to the human protein FRAP, and in particular to the FKBP12-rapamycin binding domain thereof and to the ternary complex formed by the FRB domain, rapamycin and FKBP12. A new crystalline composition comprising the ternary complex, coordinates defining its three dimensional structure in atomic detail, and uses thereof are disclosed.

Abstract: Disclosed are triaryl cationic compounds that exhibit broad spectrum antibiotic and antifungal activity, pharmaceutical compositions containing the compounds, and methods of treating bacterial and fungal infections using the compounds. The compounds were initially isolated by screening a 25,000-member bacterial artificial chromosome (BAC) library of environmental (eDNA) from soil. At least one clone produced a dark brown melanin-like compound that was found to have antibiotic activity. The compounds were isolated and synthesized de novo. From within the positive clone, a single open reading frame that shares extensive sequence similarity with members of the 4-hydroxyphenylpyruvate family of enzymes was found to be necessary and sufficient to confer the production of at least one of the subject compounds on E. coli.

Abstract: The invention relates to the human protein FRAP, and in particular to the FKBP12-rapamycin binding domain thereof and to the ternary complex formed by the FRB domain, rapamycin and FKBP12. A new crystalline composition comprising the ternary complex, coordinates defining its three dimensional structure in atomic detail, and uses thereof are disclosed.

Abstract: Novel thioimidazoles are 5-carboxyaldehyde-1-methyl-4-(phenylmethyl)thioimidazole and 5-(.alpha.-aminoacetyl)-1-methyl-4-(phenylmethyl)thioimidazole acid addition salt. The latter is prepared from the former by steps comprising Grignard addition to form 5-(1-hydroxyethyl)-1-methyl-4-(phenylmethyl)thioimidazole, oxidizing the hydroxy compound to form the corresponding ketone, brominating under acidic conditions to form the bromoacetyl derivative, converting the bromo in the bromoacetyl derivative to N,N-diformylamino and then hydrolyzing. The latter thioimidazole is an intermediate for forming 5-methylimidazo[4,5-e]-1,2-thiazin-4(5H)-one, that is neamphine, and for forming 3-chloro-(5-methylimidazo) [4,5-e]-1,2-thiazin-4(5H)-one, that is 3-chloroneamphine.