| abstract |
The present invention pertains to synthetic analogues of microcin B17 component units, methods of making and using these analogues, including, for example, as inhibitors of DNA gyrase. More particularly, the present invention pertains to compounds of the Formula (1) wherein: W is independently: -H or a peptide group; Z is independently: -OH or a peptide group; wherein each peptide group, if present, is: an amino acid group and comprises exactly one amino acid, or: a poly(amino acid) group and comprises two or more amino acids; RN3 is independently: -H, C1-6alkyl, C2-6alkenyl, C3-6cycloalkyl, or C3-6cycloalkenyl, C6-14carboaryl, C5-14heteroaryl, C6-14carboaryl-C1-6alkyl, C5-14heteroaryl-C1-6alkyl, and is optionally substituted; the circle represents a mono-heterocycle or a bis-heterocycle, wherein the heterocycle, or each of the two heterocycles, is a five membered ring having at least a first ring heteroatom that is N, and optionally a second ring heteroatom that is selected from N, O, and S; and the heterocycle, or each of the two heterocycles, is optionally substituted with one or more substituents; and pharmaceutically acceptable salts, amides, esters, solvates, and hydrates thereof. The present invention also pertains to uses of such compounds, for example, to inhibit DNA Gyrase activity in a cell and in methods of therapy, for example, to treat a disease or condition that is ameliorated by the inhibition of DNA Gyrase, such as a bacterial infection, cancer, etc.; as a herbicide; as a microbicide; as a bactericide; etc. |