Glyco-optimization of aminoglycosides: new aminoglycosides as novel anti-infective agents |
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| Authors: | Yao Sulan Sgarbi Paulo W M Marby Kenneth A Rabuka David O'Hare Sean M Cheng Mayling L Bairi Mrunali Hu Changyong Hwang San-Bao Hwang Chan-Kou Ichikawa Yoshi Sears Pamela Sucheck Steven J |
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| Affiliation: | Department of Chemistry, Optimer Pharmaceuticals, Inc., 10110 Sorrento Valley Road, Suite C, San Diego, CA 92121, USA. ssucheck@optimerpharma.com |
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| Abstract: | Glyco-optimization (OPopS) of aminoglycosides has been performed by replacing the existing sugar moiety with a variety of sugar derivatives. Glycosylation of the 6-position of nebramine provided a library of novel 4,6-linked aminoglycosides (AMGs). Among them, compounds 8b,g,i,l, and 8u with 2"-amino, 2",3"-diamino, 2",4"-diamino, 3",4"-diamino, 3"-amino groups, respectively, showed significant antimicrobial activity against Gram-(+) and -(-) bacteria. Several were particularly potent against Pseudomonus aeruginosa with MICs in the 1-2 microg/mL range. |
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