Design, Synthesis, and Structure - Activity Relationship Studies of Dual Inhibitors of Soluble Epoxide Hydrolase and 5-Lipoxygenase

Autor: Hiesinger, K., Kramer, J.S., Beyer, S., Eckes, T., Brunst, S., Flauaus, C., Wittmann, S.K., Weizel, L., Kaiser, A., Kretschmer, S.B.M., George, S., Angioni, C., Heering, J., Geisslinger, G., Schubert-Zsilavecz, M., Schmidtko, A., Pogoryelov, D., Pfeilschifter, J., Hofmann, B., Steinhilber, D., Schwalm, S., Proschak, E.

Inhibition of multiple enzymes of the arachidonic acid cascade leads to synergistic anti-inflammatory effects. Merging of 5-lipoxygenase (5-LOX) and soluble epoxide hydrolase (sEH) pharmacophores led to the discovery of a dual 5-LOX/sEH inhibitor, wh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od_______610::c07111b1bc9589c2536a41f7ea81da3d
https://publica.fraunhofer.de/handle/publica/265846

Challenges in the Development of a Thiol-Based Broad-Spectrum Inhibitor for Metallo-v-Lactamases

Autor: Büttner, D., Kramer, J.S., Klingler, F.-M., Wittmann, S.K., Hartmann, M.R., Kurz, C.G., Kohnhäuser, D., Weizel, L., Brüggerhoff, A., Frank, D., Steinhilber, D., Wichelhaus, T.A., Pogoryelov, D., Proschak, E.

Pathogens, expressing metallo-v-lactamases (MBLs), become resistant against most v-lactam antibiotics. Besides the dragging search for new antibiotics, development of MBL inhibitors would be an alternative weapon against resistant bacterial pathogens

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od_______610::082c8363792d2ac000fc8951c7708895
https://publica.fraunhofer.de/handle/publica/257327

Approachable Synthetic Methodologies for Second-Generation β -Lactamase Inhibitors: A Review.

Autor: Fatima, Noor¹ (AUTHOR) noorfatima09263@gmail.com, Khalid, Shehla¹ (AUTHOR) shehlakhalid47@gmail.com, Rasool, Nasir¹ (AUTHOR) bushrachemgcuf@gmail.com, Imran, Muhammad² (AUTHOR) imranchemist@gmail.com, Parveen, Bushra¹ (AUTHOR) aqsa6373@gmail.com, Kanwal, Aqsa¹ (AUTHOR), Irimie, Marius³ (AUTHOR) marius.irimie@unitbv.ro, Ciurea, Codrut Ioan³ (AUTHOR) codrut.ciurea@unitbv.ro

Publikováno v: Pharmaceuticals (14248247). Sep2024, Vol. 17 Issue 9, p1108. 62p.

Structure-Based Optimization of 1,2,4-Triazole-3-Thione Derivatives: Improving Inhibition of NDM-/VIM-Type Metallo-β-Lactamases and Synergistic Activity on Resistant Bacteria.

Autor: Bersani, Matteo¹ (AUTHOR) matteo.bersani@unito.it, Failla, Mariacristina¹ (AUTHOR) mariacristina.failla@unito.it, Vascon, Filippo² (AUTHOR) filippo.vascon@unipd.it, Gianquinto, Eleonora¹ (AUTHOR) eleonora.gianquinto@unito.it, Bertarini, Laura³ (AUTHOR) laura.bertarini@unimore.it, Baroni, Massimo⁴ (AUTHOR) massimo@moldiscovery.com, Cruciani, Gabriele⁵ (AUTHOR) gabriele.cruciani@unipg.it, Verdirosa, Federica⁶ (AUTHOR) federica.verdirosa95@gmail.com, Sannio, Filomena⁶ (AUTHOR) filomena.sannio@unisi.it, Docquier, Jean-Denis^6,7 (AUTHOR) jddocquier@unisi.it, Cendron, Laura² (AUTHOR) laura.cendron@unipd.it, Spyrakis, Francesca¹ (AUTHOR) francesca.spyrakis@unito.it, Lazzarato, Loretta¹ (AUTHOR) loretta.lazzarato@unito.it, Tondi, Donatella³ (AUTHOR) loretta.lazzarato@unito.it

Publikováno v: Pharmaceuticals (14248247). Dec2023, Vol. 16 Issue 12, p1682. 22p.

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