Abstract: The invention relates to methods for treating COVID-19 by targeting the inflammasome/caspase1/pyroptosis axis as a key inflammatory pathway. In particular, the invention relates to treating a patient infected with SARS-CoV-2 with an effective amount of one or more compounds that directly or indirectly inhibit one or more pathways of the inflammasome/caspase1/pyroptosis axis.

Abstract: The invention relates to methods for treating COVID-19 by targeting the inflammasome/caspase1/pyroptosis axis as a key inflammatory pathway. In particular, the invention relates to treating a patient infected with SARS-CoV-2 with an effective amount of one or more compounds that directly or indirectly inhibit one or more pathways of the inflammasome/caspase1/pyroptosis axis.

Abstract: The invention relates to methods for treating COVID-19 by targeting the inflammasome/caspase1/pyroptosis axis as a key inflammatory pathway. In particular, the invention relates to treating a patient infected with SARS-CoV-2 with an effective amount of one or more compounds that directly or indirectly inhibit one or more pathways of the inflammasome/caspase1/pyroptosis axis.

Abstract: The current study established that treatment of diabetes using compound 1(2,4-dinitroanilino-benzoic acid), an anthranilic acid derivative, by restoring the functional activities of the pancreas via its insulinotropic action.

Abstract: The present invention relates to anti-thymidine phosphorylase compounds. These compounds are derivatives of 4-hydroxybenzohydarzide or generally Schiff bases of hydrazones. The invention evaluates a series of Schiff bases of hydrazones against thymidine phosphorylase, and identified significant inhibitors of thymidine phosphorylase enzyme during in vitro studies.

Abstract: One embodiment of the invention relates to treating diseases associated with increased urease enzyme activity comprising administering an effective amount of a compound selected from a group consisting of 28 thiazoles Schiff bases. Kinetic studies were performed on ten (10) of the most active compounds.

Abstract: Two thiourea derivatives N-(3-chlorophenyl)-N?-(3,4-difluorophenyl)thiourea and N-(3-chlorophenyl)-N-(3-methoxyphenyl)-thiourea are reported as treatment of multidrug resistance infections from Staphylococcus aureus.

Abstract: The invention relates to methods of inhibiting the protein glycation process and the associated formation of Advanced Glycation End products (AGEs) in hyperglycemia by administering 6-Nitrobenzimidazole derivatives. These derivatives were found to be effective not merely against the formation of AGE, but they can inhibit the action of AGEs at post-receptor levels.

Abstract: One embodiment of the invention relates to treating diseases associated with increased urease enzyme activity comprising administering an effective amount of a compound selected from a group consisting of 28 thiazoles Schiff bases. Kinetic studies were performed on ten (10) of the most active compounds.

Abstract: Two thiourea derivatives N-(3-chlorophenyl)-N?-(3,4-difluorophenyl) thiourea and N-(3-chlorophenyl)-N-(3-methoxyphenyl)-thiourea are reported as treatment of multidrug resistance infections from Staphylococcus aureus.

Abstract: HslVU is the proteasome-related system composed of HslV peptidase and HslU chaperone. It is involved in intracellular proteolysis. The presence of HslVU homologs in pathogenic microbes and its absence in human makes it an antimicrobial drug target. The functional HslVU complex forms when HslV dodecamer is flanked at both ends by HslU hexamers. In the HslVU complex, intercalation of C-termini residues of HslU subunits into the clefts between adjacent HslV subunits results in allosteric activation of HslV. We identified small molecules capable of activating HslV peptidase in the absence of its natural activator HslU. Quinazoline and chromone derivatives were suggested by ligand docking to bind at the HslU C-termini intercalation pockets in the HslV. This was confirmed by HslV activation assays with these compounds that gave ED50 in sub-micromolar range. The results showed that small, extracellular non-peptidic molecules can activate the HslV peptidase which in turn would initiate intracellular proteolysis.

Abstract: ?-Chymotrypsin inhibitors of thiourea class are reported that could be potent inhibitors of proteases, elastases, proteasomes, NS3 and NS4 serine protease of hepatitis C virus, dengue virus, etc. Compounds 1-22, which are belong to thiourea class, showed good inhibition. Their kinetics study and cytotoxicity profiles showed all type of inhibition except uncompetitive-type inhibition and no cytotoxicity except few compounds. Competitive type of inhibitors could inhibit other ?-chymotrypsin-like serine proteases, which are therapeutics target.

Abstract: This invention provides a series of new oxindole derivatives 1-21, evaluated for their antiglycation potential by using in vitro BSA-MG glycation model. These derivatives showed a varying degree of antiglycation activity with IC50 values ranging between 150-856 ?M. Compound 14 (IC50=150.4±2.5 ?M) was found to be the most potent among all derivatives, even better than the standard inhibitor i.e. rutin (IC50=294.5±1.50 followed by compounds 13 and 8 with IC50 value of 194.40±2.5 and 211.41±4.1 ?M, respectively.

Abstract: The invention feature series of benzothiazole derivatives as potent immunosuppressive and antiinflammatory agents. Eight compounds 2, 4, 5, 8, 9, 10, 12, and 18 showed potent inhibitory activity on PHA-activated T-cell proliferation. Compounds 2, 4, 8, and 18 were found to have a potent inhibitory activity with IC50 values ranging <1.0-2.9 ?g/mL against IL-2. Studies on innate immune response revealed that compounds 2, 8, 9, and 10 have significant suppressive effect on ROS production with an IC50 values 1.9, <1, 3.7 and 1.1 ?g/mL, respectively. The LPS-induced nitrites in J774 macrophages cell line was inhibited by 4, 8, 9, and 18 at a concentration of 25 ?g/mL (56-91%). In addition compounds 5, 8, 12, and 18 showed potent suppression on interleukin 4 (IL-4), particularly 9 (IC50<1 ?g/mL). No cytotoxicity was found except for compound 9 and 18 (11.4 and 10.4 ?g/mL IC50), respectively.

Abstract: HslVU is the proteasome-related system composed of HslV peptidase and HslU chaperone. It is involved in intracellular proteolysis. The presence of HslVU homologs in pathogenic microbes and its absence in human makes it an antimicrobial drug target. The functional HslVU complex forms when HslV dodecamer is flanked at both ends by HslU hexamers. In the HslVU complex, intercalation of C-termini residues of HslU subunits into the clefts between adjacent HslV subunits results in allosteric activation of HslV. We identified small molecules capable of activating HslV peptidase in the absence of its natural activator HslU. Quinazoline and chromone derivatives were suggested by ligand docking to bind at the HslU C-termini intercalation pockets in the HslV. This was confirmed by HslV activation assays with these compounds that gave ED50 in sub-micromolar range. The results showed that small, extracellular non-peptidic molecules can activate the HslV peptidase which in turn would initiate intracellular proteolysis.

Abstract: Surprising antiviral activity of 3-amino-2-(4-nitrophenyl)-4-(3H)-quinazolinone (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.

Abstract: Surprising antiviral activity of 3-amino-2-(4-nitrophenyl)-4-(3H)-quinazolinone (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.

Abstract: Surprising antiviral activity of 7-Nitro-2-(3-nitro phenyl)-4H-3,1-benzoxazin-4-one (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.

Abstract: Surprising antiviral activity of 7-Nitro-2-(3-nitro phenyl)-4H-3,1-benzoxazin-4-one (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.