Spectinomycin is an aminocyclitol based antibiotic discovered in 1961 and used to treat N. gonorrhoeae infections until it was discontinued in the 1980s due to increasing bacterial resistance. It has a broad but weak spectrum activity and favorable pharmacokinetic properties make it a valuable scaffold for designing new therapeutics. Over the past 20 years, there has been a rise in non-tubercular mycobacterium (NTM) infections, with Mycobacterium abscessus (M. abscessus) becoming a clinical concern for immunosuppressed or compromised patients. These infections are difficult to treat due to M. abscessus having high intrinsic resistance to antibiotics. Using structure guided design and molecular modeling we designed and synthesized a novel series of aminomethyl spectinomycins (AmSPCs) with substantial activity against M. abscessus. The structure activity relationship of this series will be discussed in detail, as well as the synthesis of the compounds.

Spectinomycin to the rescue: Novel aminomethyl spectinomycin scaffold effective against M. abscessus infections

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.