title: Synthetic dihydropacidamycin antibiotics: a modified spectrum of activity for the pacidamycin class.
abstract: Dihydropacidamycins having an antibacterial spectrum modified from that of the natural product pacidamycins and mureidomycins have been synthesized. Synthetic dihydropacidamycins with noteworthy antibacterial activity against wild-type and resistant Escherichia coli have been identified (MIC=4-8 microg/mL). Some dihydropacidamycins are shown to have activity against multi-resistant clinical strains of Mycobacterium tuberculosis. Compounds of this class are inhibitors of the cell wall biosynthetic enzyme, MraY.
authors.affiliation: Essential Therapeutics, Inc. (formerly Microcide Pharmaceuticals, Inc.), 850 Maude Avenue, Mountain View, CA 94043, USA. dboojamra@gilead.com
authors.forename: Constantine G
authors.initials: CG
authors.lastname: Boojamra
authors.forename: Rémy C
authors.initials: RC
authors.lastname: Lemoine
authors.forename: Johanne
authors.initials: J
authors.lastname: Blais
authors.forename: Nicole G
authors.initials: NG
authors.lastname: Vernier
authors.forename: Karin A
authors.initials: KA
authors.lastname: Stein
authors.forename: Angela
authors.initials: A
authors.lastname: Magon
authors.forename: Suzanne
authors.initials: S
authors.lastname: Chamberland
authors.forename: Scott J
authors.initials: SJ
authors.lastname: Hecker
authors.forename: Ving J
authors.initials: VJ
authors.lastname: Lee
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D006088:Gram-Negative Aerobic Bacteria / Q000187:drug effects / Q000254:growth & development; D006801:Humans; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D011741:Pyrimidine Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D010455:Peptides; D011741:Pyrimidine Nucleosides; C432124:dihydropacidamycin D