Antibacterials

Antibacterials, Medicinal chemistry, Research

Antimicrobial resistance (AMR) is a growing global health threat, responsible for 700,000 deaths each year, a number projected to rise to 10 million by 2050. To address this challenge, collaborative efforts between academia and industry, supported by public and private funding, are driving early-stage antibiotic discovery.
Our group contributes to the development of new antibacterial agents as well as adjuvant molecules such as serine and metallo β-lactamase inhibitors to boost the effectiveness of existing antibiotics and tackle the growing challenge of antimicrobial resistance.

Publications

49. Synthesis and Evaluation of Novel 5-O-(4-C-Aminoalkyl-β-D-ribofuranosyl) Apramycin Derivatives for the Inhibition of Gram-Negative Pathogens Carrying the Aminoglycoside Phosphotransferase(3′)-Ia Resistance Determinant

Lubriks, D.; Haldimann, K.; Kiliç, F.; Hartmann, M.; Böttger, E. C.; Hobbie, S. N.; Suna, E.; Crich, D. Helv. Chim. Acta 2023, e202300138
DOI: 10.1002/hlca.202300138.

44. Optimized Synthesis of Indole Carboxylate Metallo-β-Lactamase Inhibitor EBL-3183

Baran, A.; Kuzmins, J.; Kuznecovs, J.; Farley, A., J., M.; Panduwawala, T.; Parkova, A.; Donets, P., A.; Brem, J.; Suna, E.; Schofield, C., J.; Shubin, K. Org. Process Res. Dev. 2023, 27, 692–706. DOI:10.1021/acs.oprd.3c00002

41. Synthesis, Antibacterial and Antiribosomal Activity of the 3C-Aminoalkyl Modification in the Ribofuranosyl Ring of Apralogs (5-O-Ribofuranosyl Apramycins)

Lubriks, D.; Haldimann, K.; Hobbie, S. N.; Vasella A.; Suna E.; Crich D.; Antibiotics 2023, 12, 25–39. DOI: 10.3390/antibiotics12010025

38. Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors

Brem, J.; Panduwawala, T.; Hansen, J. U.; Hewitt, J.; Liepins, E.; Donets, P.; Espina, L.; Farley, A. J. M.; Shubin, K; Campillos, G. G.; Kiuru, P.; Shishodia, S.; Krahn, D.; Leśniak, R. K.; Schmidt (Adrian), J.; Calvopiña, K.; Turrientes, M. C.; Kavanagh, M. E.; Lubriks, D.; Hinchliffe, P.; Langley, G. W.; Aboklaish, A. F.; Eneroth, A.; Backlund, M.; Baran, A. G.; Nielsen, E. I.; Speake, M.; Kuka, J.; Robinson, J.; Grinberga, S.; Robinson, L.; McDonough, M. A.; Rydzik, A. M.; Leissing, T. M.; Jimenez-Castellanos, J. C.; Avison, M. B; Pinto, S. S.; Pannifer, A. D.; Martjuga, M.; Widlake, E.; Priede, M.; Navratilova, I. H.; Gniadkowski, M.; Belfrage, A. K.; Brandt, P.; Yli-Kauhaluoma, j.; Bacque, E.; Page, M. G. P.; Björkling, F.; Tyrrell, J. M.; Spencer, J.; Lang, P. A.; Baranczewski, P.; Cantón, R.; McElroy, S. P.; Jones, P. S.; Baquero, F.; Suna, E.; Morrison, A.; Walsh, T. R.; Schofield, C. J. Nat. Chem 2022, 14, 15-24.

DOI: 10.1038/s41557-021-00831-x

35. Synthesis and Antibacterial Activity of Propylamycin Derivatives Functionalized at the 5′′- and Other Positions with a View to Overcoming Resistance Due to Aminoglycoside Modifying Enzymes

Lubriks, D.; Zogota, R.; Sarpe, V., A.; Matsushita, T.; Sati, G., C.; Haldimann, K.; Gysin, M.; Böttger, E., C.; Vasella, A.; Suna, E.; Hobbie, S., N.; Crich, D. ACS Infect. Dis. 2021, 7, 2413–2424.

DOI: 10.1021/acsinfecdis.1c00158

31. Structure-activity relationship studies on the inhibition of the bacterial translation of novel Odilorhabdins analogues

Loza, E.; Sarciaux, M.; Ikaunieks, M.; Katkevics, M.; Kukosha, T.; Trufilkina, N.; Ryabova, V.; Shubin, K.; Pantel, L.; Serri, M.; Huseby, D. L.; Cao, S.; Yadav, K.; Hjort, K.; Hughes, D.; Gualtieri, M.; Suna, E.; Racine, E. Bioorg. Med. Chem. 2020, 28, 115469.

DOI: 10.1016/j.bmc.2020.115469

24. Mechanistic aspects of maltotriose-conjugate translocation to the Gram-negative bacteria cytoplasm

Dumont, E.; Vergalli, J.; Pajovic, J.; Bhamidimarri, S. P.; Morante, K.; Wang, J.; Lubriks, D.; Suna, E.; Stavenger, R. A.; Winterhalter, M.; Refregiers, M.; Pages, J. M. Life Science Alliance 2019, 2, e201800242.

DOI: 10.26508/lsa.201800242