Patent classifications
C07C225/30
REVERSIBLY REDUCIBLE MATERIALS AND USE THEREOF
Provided herein are a reversibly reducible material and a method of forming a reversibly reducible material. The reversibly reducible material includes the molecular formula:
##STR00001##
wherein each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from the group consisting of hydrogen, oxygen, alkyl, cycloalkyl, O-alkyl, amine, quaternary ammonium, and sulfonate; R.sup.5 is selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, and amine; X is selected from the group consisting of hydrogen, branched or un-branched alkyl chain having 1-8 atoms containing 0-3 oxygen or nitrogen atoms, and substituted or unsubstituted aryl; and Z is selected from the group consisting of branched or un-branched alkyl chain having 1-8 atoms containing 0-3 oxygen or nitrogen atoms, and substituted or unsubstituted aryl. The method of forming a reversibly reducible material comprising reacting a quinone with an amine in an ethereal solvent. Also provided herein is a negolyte.
REVERSIBLY REDUCIBLE MATERIALS AND USE THEREOF
Provided herein are a reversibly reducible material and a method of forming a reversibly reducible material. The reversibly reducible material includes the molecular formula:
##STR00001##
wherein each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from the group consisting of hydrogen, oxygen, alkyl, cycloalkyl, O-alkyl, amine, quaternary ammonium, and sulfonate; R.sup.5 is selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, and amine; X is selected from the group consisting of hydrogen, branched or un-branched alkyl chain having 1-8 atoms containing 0-3 oxygen or nitrogen atoms, and substituted or unsubstituted aryl; and Z is selected from the group consisting of branched or un-branched alkyl chain having 1-8 atoms containing 0-3 oxygen or nitrogen atoms, and substituted or unsubstituted aryl. The method of forming a reversibly reducible material comprising reacting a quinone with an amine in an ethereal solvent. Also provided herein is a negolyte.
SMALL MOLECULE INHIBITORS OF USP1 DEUBIQUITINATING ENZYME ACTIVITY
Provided are small molecule inhibitors of ubiquitin specific protease 1 (USP1) activity and methods for their use in treating and characterizing cancers. The small molecule USP1 inhibitors of the invention are particularly useful in the treatment of cancers that are resistant to DNA cross-linking agents.
Compounds and methods for the treatment of parasitic infections
Cryptosporidium parvum is a highly prevalent zoonotic and anthroponotic protozoan parasite that causes a diarrheal syndrome in children and neonatal livestock, culminating in growth retardation and mortalities. Disclosed herein are inhibitors against the enzymatic activity of recombinant CpLDH protein that were identified. The inhibitors were tested for anti-Cryptosporidium effect using in vitro infection assays of HCT-8 cells monolayers. Compounds NSC158011 and NSC10447 were identified to inhibit the proliferation of intracellular C. parvum in vitro, with IC50 values of 14.88 and 72.65 M, respectively. At doses tolerable in mice, both NSC158011 and NSC10447 significantly reduced the shedding of C. parvum oocysts in infected immunocompromised mice's feces and prevented intestinal villous atrophy as well as mucosal erosion due to C. parvum. These findings have unveiled anti-Cryptosporidium drug candidates that can be explored further for the development of therapeutic agents against C. parvum infections.
Compounds and methods for the treatment of parasitic infections
Cryptosporidium parvum is a highly prevalent zoonotic and anthroponotic protozoan parasite that causes a diarrheal syndrome in children and neonatal livestock, culminating in growth retardation and mortalities. Disclosed herein are inhibitors against the enzymatic activity of recombinant CpLDH protein that were identified. The inhibitors were tested for anti-Cryptosporidium effect using in vitro infection assays of HCT-8 cells monolayers. Compounds NSC158011 and NSC10447 were identified to inhibit the proliferation of intracellular C. parvum in vitro, with IC50 values of 14.88 and 72.65 M, respectively. At doses tolerable in mice, both NSC158011 and NSC10447 significantly reduced the shedding of C. parvum oocysts in infected immunocompromised mice's feces and prevented intestinal villous atrophy as well as mucosal erosion due to C. parvum. These findings have unveiled anti-Cryptosporidium drug candidates that can be explored further for the development of therapeutic agents against C. parvum infections.
NAPHTHALENE-TYPE COMPOUND AND PREPARATION METHOD THEREFORE AND USE THEREFORE
A naphthalene-type compound, preparation method therefore and use therefore are provided. The naphthalene-type compound has a molecular structure substituted with polyhydroxyl, polybenzylamine, and quaternary ammonium or multiple quaternary ammonium functional groups, and compared with a raw material, the naphthalene-type compound has greatly improved water solubility in an acidic aqueous solution. An electrochemical reaction has low raw material costs and a high reaction yield, is carried out under a normal temperature and pressure condition without adding additional catalysts, and is carried out under air conditions without inert gas protection.
NAPHTHALENE-TYPE COMPOUND AND PREPARATION METHOD THEREFORE AND USE THEREFORE
A naphthalene-type compound, preparation method therefore and use therefore are provided. The naphthalene-type compound has a molecular structure substituted with polyhydroxyl, polybenzylamine, and quaternary ammonium or multiple quaternary ammonium functional groups, and compared with a raw material, the naphthalene-type compound has greatly improved water solubility in an acidic aqueous solution. An electrochemical reaction has low raw material costs and a high reaction yield, is carried out under a normal temperature and pressure condition without adding additional catalysts, and is carried out under air conditions without inert gas protection.
COMPOUNDS AND METHODS FOR THE TREATMENT OF PARASITIC INFECTIONS
Cryptosporidium parvum is a highly prevalent zoonotic and anthroponotic protozoan parasite that causes a diarrheal syndrome in children and neonatal livestock, culminating in growth retardation and mortalities. Disclosed herein are inhibitors against the enzymatic activity of recombinant CpLDH protein that were identified. The inhibitors were tested for anti-Cryptosporidium effect using in vitro infection assays of HCT-8 cells monolayers. Compounds NSC158011 and NSC10447 were identified to inhibit the proliferation of intracellular C. parvum in vitro, with IC.sub.50 values of 14.88 and 72.65 M, respectively. At doses tolerable in mice, both NSC158011 and NSC10447 significantly reduced the shedding of C. parvum oocysts in infected immunocompromised mice's feces and prevented intestinal villous atrophy as well as mucosal erosion due to C. parvum. These findings have unveiled anti-Cryptosporidium drug candidates that can be explored further for the development of therapeutic agents against C. parvum infections.
COMPOUNDS AND METHODS FOR THE TREATMENT OF PARASITIC INFECTIONS
Cryptosporidium parvum is a highly prevalent zoonotic and anthroponotic protozoan parasite that causes a diarrheal syndrome in children and neonatal livestock, culminating in growth retardation and mortalities. Disclosed herein are inhibitors against the enzymatic activity of recombinant CpLDH protein that were identified. The inhibitors were tested for anti-Cryptosporidium effect using in vitro infection assays of HCT-8 cells monolayers. Compounds NSC158011 and NSC10447 were identified to inhibit the proliferation of intracellular C. parvum in vitro, with IC.sub.50 values of 14.88 and 72.65 M, respectively. At doses tolerable in mice, both NSC158011 and NSC10447 significantly reduced the shedding of C. parvum oocysts in infected immunocompromised mice's feces and prevented intestinal villous atrophy as well as mucosal erosion due to C. parvum. These findings have unveiled anti-Cryptosporidium drug candidates that can be explored further for the development of therapeutic agents against C. parvum infections.