Structure-activity relationships of bivalent aminoglycosides and evaluation of their microbiological activities |
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| Authors: | Liang Chang-Hsing Romero Alex Rabuka David Sgarbi Paulo W M Marby Kenneth A Duffield Jonathan Yao Sulan Cheng Mayling L Ichikawa Yoshi Sears Pamela Hu Changyong Hwang San-Bao Shue Youe-Kong Sucheck Steven J |
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| Affiliation: | Department of Chemistry, Optimer Pharmaceuticals, Inc., 10110 Sorrento Valley Rd., Suite C, San Diego, CA 92121, USA. |
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| Abstract: | A library of 4,5- and 4,6-linked bivalent aminoglycoside (AMG) antibiotics consisting of neamine and nebramine pharmacophores have been synthesized. We probed the effect of the linker on antibiotic activity with a series of selected synthetic analogues with varied length and substituents. A number of compounds demonstrated in vitro activity against several bacterial strains and showed activity against drug resistant strains of Pseudomonas aeruginosa. Among the compounds prepared, analogues 12a-d were novel 4,6-linked AMGs containing the nebramine pharmacophore. In addition the lead compound OPT-11 possessed an ED(50) of
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