Böttger Erik C., Crich David (2020), Aminoglycosides: Time for the Resurrection of a Neglected Class of Antibacterials?, in ACS Infectious Diseases
, 6(2), 168-172.
Sati Girish C., Sarpe Vikram A., Furukawa Takayuki, Mondal Sujit, Mantovani Matilde, Hobbie Sven N., Vasella Andrea, Böttger Erik C., Crich David (2019), Modification at the 2′-Position of the 4,5-Series of 2-Deoxystreptamine Aminoglycoside Antibiotics To Resist Aminoglycoside Modifying Enzymes and Increase Ribosomal Target Selectivity, in ACS Infectious Diseases
, 5(10), 1718-1730.
Sonousi Amr, Shcherbakov Dimitri, Vasella Andrea, Böttger Erik C., Crich David (2019), Synthesis, ribosomal selectivity, and antibacterial activity of netilmicin 4′-derivatives, in MedChemComm
, 10(6), 946-950.
Matsushita Takahiko, Sati Girish C., Kondasinghe Nuwan, Pirrone Michael G., Kato Takayuki, Waduge Prabuddha, Kumar Harshitha Santhosh, Sanchon Adrian Cortes, Dobosz-Bartoszek Malgorzata, Shcherbakov Dimitri, Juhas Mario, Hobbie Sven N., Schrepfer Thomas, Chow Christine S., Polikanov Yury S., Schacht Jochen, Vasella Andrea, Böttger Erik C., Crich David (2019), Design, Multigram Synthesis, and in Vitro and in Vivo Evaluation of Propylamycin: A Semisynthetic 4,5-Deoxystreptamine Class Aminoglycoside for the Treatment of Drug-Resistant Enterobacteriaceae and Other Gram-Negative Pathogens, in Journal of the American Chemical Society
, 141(12), 5051-5061.
This proposal targets the further development of established proven antibacterials to expand their use for treatment of infections with (multi)-drug resistant microorganisms. Specifically, we address the problem of drug resistant infectious diseases by the synthesis and evaluation of novel mechanism-based aminoglycoside antibiotics designed to avoid common resistance determinants and to minimize the well-known side effects associated with currently available aminoglycosides.