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Conjugates of monocyclic β-lactams and siderophore mimetics : a patent evaluation (WO2023023393)Krajnc, Alen, Farmacija, 1994 ; Gobec, Stanislav, 1970-Introduction: β-Lactams, which include monobactams, remain the most important class of antibiotics worldwide. Aztreonam, the only monobactam in clinical use, has remarkable activity against many ... Gram-negative bacteria, but limited activity against some of the most problematic multidrug-resistant (MDR) pathogens, such as MDR Pseudomonas aeruginosa and Acinetobacter baumannii co-expressing extended-spectrum- and metallo-β-lactamases, which can inactivate aztreonam by hydrolysis. Areas covered: Structurally novel siderophore-conjugated aztreonam derivatives with improved antibacterial properties against several high-priority pathogens are claimed. This invention reports that sidechain extension of aztreonam is tolerated; the coupling of its aminothiazoloxime carboxylic acid part with a siderophore mimetic significantly improved the antibacterial activity against several problematic strains, including MDR A. baumannii isolates with carbapenemase/cephalosporinase activity. Expert Opinion: Finding new strategies to tackle bacterial resistance to β-lactam antibiotics is critical. Considering that β lactams are validated and safe drugs, this research may stimulate the field to develop new ideas in the arena of antimicrobial drug discovery, particularly with respect to siderophore mimetics.Vir: Expert opinion on therapeutic patents. - ISSN 1354-3776 (Vol. 33, iss. 7-8, 2023, str. 471-476)Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasleLeto - 2023Jezik - angleškiCOBISS.SI-ID - 171047171
Avtor
Krajnc, Alen, Farmacija, 1994 |
Gobec, Stanislav, 1970-
Teme
Bakterijska rezistenca |
Farmacevtska kemija |
antimicrobial resistance |
conjugates |
aztreonam |
anticoagulant |
β-lactams |
monocyclic β-lactams |
siderophores |
protimikrobna odpornost |
aztreonam |
konjugati |
β-laktami |
monociklični β-laktami |
siderofori
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Avtor | Krajnc, Alen, Farmacija, 1994 ; Gobec, Stanislav, 1970- |
Naslov | Conjugates of monocyclic β-lactams and siderophore mimetics : a patent evaluation (WO2023023393) |
Datum objave | 2023-11-06 |
COBISS.SI-ID | 171047171 |
Verzija objave v repozitoriju | Založnikova različica |
Licenca objave v repozitoriju | Creative Commons Priznanje avtorstva 4.0 Mednarodna |
Embargo | Takojšnja javna objava |
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vir: Expert opinion on therapeutic patents. - ISSN 1354-3776 (Vol. 33, iss. 7-8, 2023, str. 471-476)
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Krajnc, Alen, Farmacija, 1994 | 55572 |
Gobec, Stanislav, 1970- | 15284 |
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