Design, synthesis and structure-activity relationships of novel macrolones: Hybrids of 2-fluoro 9-oxime ketolides and carbamoyl quinolones with highly improved …

CX Ma, W Lv, YX Li, BZ Fan, X Han, FS Kong… - European Journal of …, 2019 - Elsevier
Constitutively erythromycin-resistant apathogens are more difficult to address than inducibly
resistant and efflux-resistant strains. Three series of the 4th generation 2-fluoro 9-oxime …

Synthesis and Antibacterial Activity of Ketolides (6-O-Methyl-3-oxoerythromycin Derivatives):  A New Class of Antibacterials Highly Potent Against Macrolide …

C Agouridas, A Denis, JM Auger… - Journal of medicinal …, 1998 - ACS Publications
In the search for new antibiotics active against macrolide-resistant pneumococci and
Haemophilus influenzae, we synthesized a new class of 3-oxo-6-O-methylerythromycin …

Synthesis and antibacterial activity of 6-O-(heteroaryl-isoxazolyl) propynyl 2-fluoro ketolides

T Sugimoto, Y Shimazaki, A Manaka… - Bioorganic & medicinal …, 2012 - Elsevier
Macrolide antibiotics are widely prescribed for the treatment of respiratory tract infections;
however, the increasing prevalence of macrolide-resistant pathogens is a public health …

Design and synthesis of novel macrolones bridged with linkers from 11, 12-positions of macrolides

XP Liu, W Lv, F Zhao, J Ding, JR Zhang, F Xue… - Bioorganic & Medicinal …, 2022 - Elsevier
Resistance to telithromycin and off-target effects associated with the metabolic instability
present serious and challenging problems for the development of novel macrolides. Herein …

4 ″-O-(ω-Quinolylamino-alkylamino) propionyl derivatives of selected macrolides with the activity against the key erythromycin resistant respiratory pathogens

A Fajdetić, HČ Paljetak, G Lazarevski, A Hutinec… - Bioorganic & medicinal …, 2010 - Elsevier
Four macrolides—6-O-methyl-8a-aza-8a-homoerythromycin, clarithromycin, azithromycin
and azithromycin 11, 12-cyclic carbonate, have been selected for the construction of a series …

Synthesis and structure-bactericidal activity relationships of non-ketolides: 9-Oxime clarithromycin 11, 12-cyclic carbonate featured with three-to eight-atom-length …

XM Li, W Lv, SY Guo, YX Li, BZ Fan, M Cushman… - European Journal of …, 2019 - Elsevier
In general, potent non-ketolide versions of erythromycin possessed conformationally
constricted two-or three-atom-length sidechains at 3-OH. Novel 14-membered non-ketolides …

Synthesis and antibacterial evaluation of novel 4 ″-glycyl linked quinolyl-azithromycins with potent activity against macrolide-resistant pathogens

D Pavlović, S Mutak - Bioorganic & Medicinal Chemistry, 2016 - Elsevier
A new azithromycin-based series of antibacterial macrolones is reported, which features the
use of a 4 ″-ester linked glycin for tethering the quinolone side chain to the macrolide …

Conformations in solution and bound to bacterial ribosomes of ketolides, HMR 3647 (telithromycin) and RU 72366: A new class of highly potent antibacterials

N Evrard-Todeschi, J Gharbi-Benarous, C Gaillet… - Bioorganic & medicinal …, 2000 - Elsevier
The new class of antibiotics called ketolides is endowed with remarkable antibacterial
activity against macrolide-resistant strains. Further modifications of the 3 keto-macrolactone …

Design, synthesis, and antimicrobial activity of 6-O-substituted ketolides active against resistant respiratory tract pathogens

YS Or, RF Clark, S Wang, DTW Chu… - Journal of medicinal …, 2000 - ACS Publications
Design Rationale. Structural modification of existing antibiotics remains one of the most
effective approaches for overcoming bacterial resistance. 10 We focused our efforts on the …

Design, synthesis and structure-bactericidal activity relationships of novel 9-oxime ketolides and reductive epimers of acylides

JC Tian, X Han, W Lv, YX Li, H Wang, BZ Fan… - Bioorganic & Medicinal …, 2017 - Elsevier
Erythromycin was long viewed as a bacteriostatic agent. The erythromycin derivatives, 9-
oxime ketolides have a species-specific bactericidal profile. Among them, the 3′-allyl …