title: Preparation and in vitro anti-staphylococcal activity of novel 11-deoxy-11-hydroxyiminorifamycins.
abstract: We report herein the preparation and anti-staphylococcal activity of a series of novel 11-deoxy-11-hydroxyiminorifamycins. Many of the compounds synthesized exhibit potent activity against wild-type Staphylococcus aureus with MICs equivalent to, or better than, rifamycin reference agents. In addition, some of the compounds retain potent activity against an intermediate rifamycin-resistant strain of Staphylococcus aureus. For instance, compound 5k exhibits an MIC of 0.12 microg/mL against an intermediate rifamycin-resistant strain, while the rifamycin reference agents, rifampin and rifalazil, exhibit MICs of 16 microg/mL and 2 microg/mL, respectively, against the same strain.
authors.affiliation: Department of Medicinal Chemistry, Cumbre Pharmaceuticals Inc., 1502 Viceroy Drive, Dallas, TX 75235, USA.
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.forename: Zhenkun
authors.initials: Z
authors.lastname: Ma
authors.forename: Katrina
authors.initials: K
authors.lastname: Chapo
authors.forename: Dalai
authors.initials: D
authors.lastname: Yan
authors.forename: A Simon
authors.initials: AS
authors.lastname: Lynch
authors.forename: Charles Z
authors.initials: CZ
authors.lastname: Ding
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006900:Hydroxylation; D007097:Imines / Q000737:chemistry*; D015394:Molecular Structure; D010100:Oxygen / Q000737:chemistry*; D012294:Rifamycins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship