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Your search keyword '"Ropponen, Henni‐Karoliina"' showing total 10 results
Start Over Author "Ropponen, Henni‐Karoliina"
10 results on '"Ropponen, Henni‐Karoliina"'

1. High-throughput screening of small-molecules libraries identified antibacterials against clinically relevant multidrug-resistant A. baumannii and K. pneumoniae

Author

Blasco, Benjamin, Jang, Soojin, Terauchi, Hiroki, Kobayashi, Naoki, Suzuki, Shuichi, Akao, Yuichiro, Ochida, Atsuko, Morishita, Nao, Takagi, Terufumi, Nagamiya, Hiroyuki, Suzuki, Yamato, Watanabe, Toshiaki, Lee, Hyunjung, Lee, Sol, Shum, David, Cho, Ahreum, Koh, Dahae, Park, Soonju, Lee, Honggun, Kim, Kideok, Ropponen, Henni-Karoliina, Augusto da Costa, Renata Maria, Dunn, Steven, Ghosh, Sunil, Sjö, Peter, and Piddock, Laura J.V.

Published
2024
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6. Mastering the Gram-negative bacterial barrier - Chemical approaches to increase bacterial bioavailability of antibiotics

Author

Ropponen, Henni-Karoliina, Richter, Robert, Hirsch, Anna K H, Lehr, Claus Michael, and HIPS, Helmholtz-Institut für Pharmazeutische Forschung Saarland, Universitätscampus E8.1 66123 Saarbrücken, Germany.

Subjects
Antibiotic drug design & discovery, Accumulation rules, Drug delivery, In silico &in vitro assays, Medicinal chemistry, Antimicrobial resistance, Permeability
Abstract

To win the battle against resistant, pathogenic bacteria, novel classes of anti-infectives and targets are urgently needed. Bacterial uptake, distribution, metabolic and efflux pathways of antibiotics in Gram-negative bacteria determine what we here refer to as bacterial bioavailability. Understanding these mechanisms from a chemical perspective is essential for anti-infective activity and hence, drug discovery as well as drug delivery. A systematic and critical discussion of in bacterio, in vitro and in silico assays reveals that a sufficiently accurate holistic approach is still missing. We expect new findings based on Gram-negative bacterial bioavailability to guide future anti-infective research.

Published
2021

10. Assessment of the rules related to gaining activity against Gram-negative bacteriaElectronic supplementary information (ESI) available: Synthetic protocols and biological data. See DOI: 10.1039/d0md00409j

Author

Ropponen, Henni-Karoliina, Diamanti, Eleonora, Siemens, Alexandra, Illarionov, Boris, Haupenthal, Jörg, Fischer, Markus, Rottmann, Matthias, Witschel, Matthias, and Hirsch, Anna K. H.

Abstract

In the search for new antibacterial compounds, we repositioned an antimalarial compound class by derivatising it based on the so-called “eNTRy” rules for enhanced accumulation into Gram-negative bacteria. We designed, synthesised and evaluated a small library of amino acid modified compounds together with the respective Boc-protected analogues, leading to no substantial improvement in antibacterial activity against Escherichia coliwild-type K12, whereas more distinct activity differences were observed in E. colimutant strains ΔtolC, D22, ΔacrBand BL21(DE3)omp8. A comparison of the activity results of the E. colimutants with respect to the known rules related to enhanced activity against Gram-negative bacteria revealed that applicability of the rules is not always ensured. Out of the four amino acids used in this study, glycine derivatives showed highest antibacterial activity, although still suffering from efflux issues.

Published
2021
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