Discovery and hit-to-lead optimization of benzothiazole scaffold-based DNA gyrase inhibitors with potent activity against Acinetobacter baumannii and Pseudomonas aeruginosa

Autor: Andrej Emanuel Cotman, Martina Durcik, Davide Benedetto Tiz, Federica Fulgheri, Daniela Secci, Maša Sterle, Štefan Možina, Žiga Skok, Nace Zidar, Anamarija Zega, Janez Ilaš, Lucija Peterlin Mašič, Tihomir Tomašič, Diarmaid Hughes, Douglas L. Huseby, Sha Cao, Linnéa Garoff, Talía Berruga Fernández, Paraskevi Giachou, Lisa Crone, Ivailo Simoff, Richard Svensson, Bryndis Birnir, Sergiy V. Korol, Zhe Jin, Francisca Vicente, Maria C. Ramos, Mercedes de la Cruz, Björn Glinghammar, Lena Lenhammar, Sara R. Henderson, Julia E. A. Mundy, Anthony Maxwell, Clare E. M. Stevenson, David M. Lawson, Guido V. Janssen, Geert Jan Sterk, Danijel Kikelj

Publikováno v: Journal of medicinal chemistry, vol. 66, no. 2, 2023.
Journal of medicinal chemistry, str. 1380-1425 : Ilustr., Vol. 66, no. 2, 2023
COBISS-ID: 512806681
Journal of medicinal chemistry, 66(2), 1380-1425. American Chemical Society
Cotman, A E, Durcik, M, Benedetto Tiz, D, Fulgheri, F, Secci, D, Sterle, M, Možina, Š, Skok, Ž, Zidar, N, Zega, A, Ilaš, J, Peterlin Mašič, L, Tomašič, T, Hughes, D, Huseby, D L, Cao, S, Garoff, L, Berruga Fernández, T, Giachou, P, Crone, L, Simoff, I, Svensson, R, Birnir, B, Korol, S V, Jin, Z, Vicente, F, Ramos, M C, De La Cruz, M, Glinghammar, B, Lenhammar, L, Henderson, S R, Mundy, J E A, Maxwell, A, Stevenson, C E M, Lawson, D M, Janssen, G V, Sterk, G J & Kikelj, D 2023, ' Discovery and Hit-to-Lead Optimization of Benzothiazole Scaffold-Based DNA Gyrase Inhibitors with Potent Activity against Acinetobacter baumannii and Pseudomonas aeruginosa ', Journal of medicinal chemistry, vol. 66, no. 2, pp. 1380-1425 . https://doi.org/10.1021/acs.jmedchem.2c01597

We have developed compounds with a promising activity against Acinetobacter baumannii and Pseudomonas aeruginosa, which are both on the WHO priority list of antibiotic-resistant bacteria. Starting from DNA gyrase inhibitor 1, we identified compound 2

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https://repozitorij.uni-lj.si/Dokument.php?id=166579&dn=

Določanje termodinamske topnosti in permeabilnostnega koeficienta zaviralcev bakterijskih giraz B in topoizomeraz IV

Autor: Lipovnik, Lana

Nizka topnost je eden izmed najpogostejših vzrokov za prekinitev razvoja učinkovine, zato je topnost treba spremljati že v začetnih fazah razvoja zdravila. Slaba topnost pomeni slabšo absorpcijo spojine, kar se kaže v slabšem učinku zdravila.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od______3505::3ff0ef652030c7d266db820e336a2e11
https://repozitorij.uni-lj.si/IzpisGradiva.php?id=146379

Solubilizacija slabo topne učinkovine s samo-mikroemulgirajočimi sistemi vgrajenimi v trdne farmacevtske oblike

Autor: Čerpnjak, Katja

Topnost zdravilne učinkovine (ZU) je eden izmed najbolj pomembnih parametrov, s katerim zagotavljamo terapevtsko koncentracijo ZU v sistemskem krvnem obtoku. Ker pa je kar 40 – 70 % na novo odkritih ZU slabo vodotopnih, je razvoj učinkovitih pero

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https://repozitorij.uni-lj.si/Dokument.php?id=165645&dn=

Proof-of-concept for a miniaturized shake-flask biopharmaceutical solubility determination by sonic mixing

Autor: Veseli, Ardita, Kristl, Albin, Žakelj, Simon

Publikováno v: Pharmazie, vol. 75, no. 12, pp. 626-631, 2020.
Pharmazie, str. 626-631 : Graf. prikazi, tabele, Vol. 75, no. 12, 2020
COBISS-ID: 1720079

The solvent volume must be very small to obtain biopharmaceutically relevant drug solubility data with low consumption of the solid sample which is often in low supply during early drug development. However, the adequate and repeatable mixing of a sm

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https://repozitorij.uni-lj.si/IzpisGradiva.php?id=141963

Uporaba infrardeče spektroskopske semi-kvantitativne metode za določitev ocene topnosti luteolina v vodi, nepolarnih in polarnih topilih

Autor: Rajhard, Saša

V zadnjih letih so flavonoidi zaradi svojih številnih učinkov na zdravje človeka postali pogosto raziskovana tema v znanosti. Topnost flavonoidov ima velik pomen v farmacevtski, prehranski in kemijski industriji, zato je določitev ustreznih topil

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https://repozitorij.uni-lj.si/Dokument.php?id=160473&dn=