Abstract:A series of novel C-4′′-substituted azithromycins
was synthesized and evaluated for in vitro antibacterial
activity against a panel of representative erythromycin-susceptible
and macrolide-lincosamide-streptogramin (MLS) resistant pathogens.
In summary, azithromycin and quinolone substructures merged in a mutually
SAR-compatible design gave rise to a new class of antimicrobials with
an improved spectrum and potency over azithromycin. Prototypical analogues 7f and 8f display an improved potency versus
azithromy… Show more
“…Antibacterial activities of the hybrids were tested on S. aureus , Streptococcus pneumoniae , and S. pyogenes. Most of the conjugates were poorly active; however, compound 56c exhibited the highest antibacterial activity against tested strains [ 138 ]. …”
This review is aimed to provide extensive survey of quinolones and fluoroquinolones for a variety of applications ranging from metal complexes and nanoparticle development to hybrid conjugates with therapeutic uses. The review covers the literature from the past 10 years with emphasis placed on new applications and mechanisms of pharmacological action of quinolone derivatives. The following are considered: metal complexes, nanoparticles and nanodrugs, polymers, proteins and peptides, NO donors and analogs, anionic compounds, siderophores, phosphonates, and prodrugs with enhanced lipophilicity, phototherapeutics, fluorescent compounds, triazoles, hybrid drugs, bis-quinolones, and other modifications. This review provides a comprehensive resource, summarizing a broad range of important quinolone applications with great utility as a resource concerning both chemical modifications and also novel hybrid bifunctional therapeutic agents.Graphical abstract
“…Antibacterial activities of the hybrids were tested on S. aureus , Streptococcus pneumoniae , and S. pyogenes. Most of the conjugates were poorly active; however, compound 56c exhibited the highest antibacterial activity against tested strains [ 138 ]. …”
This review is aimed to provide extensive survey of quinolones and fluoroquinolones for a variety of applications ranging from metal complexes and nanoparticle development to hybrid conjugates with therapeutic uses. The review covers the literature from the past 10 years with emphasis placed on new applications and mechanisms of pharmacological action of quinolone derivatives. The following are considered: metal complexes, nanoparticles and nanodrugs, polymers, proteins and peptides, NO donors and analogs, anionic compounds, siderophores, phosphonates, and prodrugs with enhanced lipophilicity, phototherapeutics, fluorescent compounds, triazoles, hybrid drugs, bis-quinolones, and other modifications. This review provides a comprehensive resource, summarizing a broad range of important quinolone applications with great utility as a resource concerning both chemical modifications and also novel hybrid bifunctional therapeutic agents.Graphical abstract
“…Several macrolide‐quinolone hybrids tethered with ester‐amino , ester‐alkynyl , ether‐amino , ester‐alkyl , and ether‐alkyl through C‐6 position of quinolone motif were assessed for their antibacterial potency against both Gram‐positive and Gram‐negative bacteria. The SAR indicated that the antibacterial activity against Gram‐positive pathogens was more potent than against Gram‐negative pathogens generally; the linkers between macrolide moiety and quinolone motif played an important role for the antibacterial activity, especially against Gram‐positive organisms; in general, alkyl‐tethered quinolone hybrids were more active than other linkers against Gram‐negative bacteria as evidenced by ester‐alkyl linked 12 and ether‐alkyl linked 13 .…”
Gram‐negative pathogens represent a significant global health threat, while the emergency and widespread of drug resistance make the situation even worse. As “privileged building blocks,” 4‐quinolones including fluoroquinolones are mainstays of chemotherapy against various bacterial infections. However, as other antibiotics, the resistance of Gram‐negative bacteria to 4‐quinolones develops rapidly and spreads widely throughout the world. To overcome the resistance and improve the potency, a number of 4‐quinolone derivatives were designed, synthesized, and screened for their in vitro and in vivo activities against representative Gram‐negative pathogens. This review aims to summarize the recent advances made towards the discovery of 4‐quinolone derivatives as anti‐Gram‐negative agents as well as their structure–activity relationship. The enriched structure–activity relationship paves the way to the further rational development of 4‐quinolones with excellent potency against both drug‐susceptible and drug‐resistant Gram‐negative pathogens.
“…s dva dušika u veznom lancu, 19 dok su se kasnije pokazali bolji s jednim ili više kisika. 20,21,22,23 S kolegama iz Verone smo objavili još neke zaostale rezultate.…”
Section: Razdoblje 1996 -2003 Godine Prijelaz Na Bazična Istraživanunclassified
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