In one aspect, the disclosure relates to a for -helix mimetics that can replicate the -helices found at protein protein interaction (PPI) interfaces and can selectively discriminate cognate proteins in PPIs. In one aspect, the scaffolds have Formula I

##STR00001## wherein each of X.sub.1-X.sub.8 is individually selected from H, OR.sub.1, NR.sub.1R.sub.2, SR.sub.1, or PR.sub.1R.sub.2; wherein each of Y.sub.1-Y.sub.2 is individually selected from H, CO.sub.2R.sub.1, C(O)NR.sub.1R.sub.2, C(O)R.sub.1, OR.sub.1, NR.sub.1R.sub.2, SR.sub.1, or PR.sub.1R.sub.2; and wherein each of R.sub.1 and R.sub.2 is individually selected from H, or optionally substituted linear or branched C1-C20 alkyl, C3-C20 aryl, linear or branched C2-C20 alkenyl, linear or branched C2-C20 alkynyl, or C3-C20 arylalkyl.

Also disclosed are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating cancer using the compounds.

A compound with broad-spectrum antibacterial activity and its antibacterial composition are provided. The compound with broad-spectrum antibacterial activity has formula (I), which are antibacterial drug source compounds with a broad antibacterial spectrum, good antibacterial activity, suitable in vivo pharmacokinetics, and significant in vivo therapeutic effects. Preferred compound BAB159 has good antibacterial activity against Staphylococcus, Clostridium perfringens, Enterococcus, Bacillus, Streptococcus, Haemophilus, Candida krusei, Aspergillus niger, and Trichophyton, which is comparable or better than the listed drugs. The combination of preferred compound BAB159 and polymyxin E exhibits significantly enhanced synergistic antibacterial activity, especially against multidrug-resistant strains.

A compound with broad-spectrum antibacterial activity and its antibacterial composition are provided. The compound with broad-spectrum antibacterial activity has formula (I), which are antibacterial drug source compounds with a broad antibacterial spectrum, good antibacterial activity, suitable in vivo pharmacokinetics, and significant in vivo therapeutic effects. Preferred compound BAB159 has good antibacterial activity against Staphylococcus, Clostridium perfringens, Enterococcus, Bacillus, Streptococcus, Haemophilus, Candida krusei, Aspergillus niger, and Trichophyton, which is comparable or better than the listed drugs. The combination of preferred compound BAB159 and polymyxin E exhibits significantly enhanced synergistic antibacterial activity, especially against multidrug-resistant strains.

The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g., neurosurgery, endovascular clot removal, spinal tap, aneurysm repair, or deep brain stimulation, as well as retinal edema), as well as hyponatremia and excess fluid retention, and diseases such as epilepsy, retinal ischemia and other diseases of the eye associated with abnormalities in intraocular pressure and/or tissue hydration, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines, as well as to novel assays for identifying aquaporin inhibitors.

The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g., neurosurgery, endovascular clot removal, spinal tap, aneurysm repair, or deep brain stimulation, as well as retinal edema), as well as hyponatremia and excess fluid retention, and diseases such as epilepsy, retinal ischemia and other diseases of the eye associated with abnormalities in intraocular pressure and/or tissue hydration, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines, as well as to novel assays for identifying aquaporin inhibitors.

The disclosure provides for resorcinol-based compounds, pharmaceutical compositions made therefrom, and methods of treatment thereof for various disorders, including neoplastic disorders.

The disclosure provides for resorcinol-based compounds, pharmaceutical compositions made therefrom, and methods of treatment thereof for various disorders, including neoplastic disorders.