Supplementary Materials

Supplementary Material for:

Aminomethyl spectinomycins as therapeutics for drug-resistant respiratory tract and sexually transmitted bacterial infections

David F. Bruhn, Samanthi L. Waidyarachchi, Dora B. Madhura, Dimitri Shcherbakov, Zhong Zheng, Jiuyu Liu, Yasser M. Abdelrahman, Aman P. Singh, Stefan Duscha, Chetan Rathi, Robin B. Lee, Robert J. Belland, Bernd Meibohm, Jason W. Rosch, Erik C. Böttger, Richard E. Lee*

*Corresponding author. E-mail: richard.lee{at}

Published 20 May 2015, Sci. Transl. Med. 7, 288ra75 (2015)
DOI: 10.1126/scitranslmed.3010572

This PDF file includes:

  • Method S1. Chemical syntheses.
  • Method S2. Chemical stability studies.
  • Scheme S1. Synthesis of R-3′-aminomethyl-3′-hydroxy spectinomycins.
  • Scheme S2. Synthesis of N-benzyl aminomethyl spectinomycin S-isomer controls.
  • Fig. S1. Multiple sequence alignment of RpsE (protein S5).
  • Fig. S2. In silico analysis of the spectinomycin binding pocket in amSPC-resistant mutants.
  • Fig. S3. Computation analysis of the amSPC mutant binding site.
  • Fig. S4. Susceptibility of L. pneumophila to spectinomycin and amSPCs.
  • Fig. S5. Susceptibility of C. trachomatis to spectinomycin and amSPCs.
  • Fig. S6. Chemical stability of spectinomycin and compound 1.
  • Fig. S7. Efficacy in a mouse model of S. pneumoniae TIGR4 infection.
  • Fig. S8. Efficacy trial comparing matched doses of compound 1 and ampicillin.
  • Table S1. Activity against aerobic Gram-negative pathogens and M. tuberculosis.
  • Table S2. Testing against mammalian ribosomes.
  • Table S3. Lead profiling of compound 1.
  • Table S4. Sensitivity of amSPC-resistant clones to various classes of antibiotics.
  • Table S5. Antibacterial spectrum of activity for previously reported spectinomycins.
  • Table S6. Chemical stability of spectinomycin and compound 1.

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