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 …

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 …

Discovery of macrolide antibiotics effective against multi-drug resistant gram-negative pathogens

AG Myers, RB Clark - Accounts of chemical research, 2021 - ACS Publications
Conspectus Macrolides are among the most widely prescribed antibiotics, particularly for
bacterial lung infections, due to their favorable safety, oral bioavailability, and spectrum of …

Synthesis and activity of new macrolones: Conjugates between 6 (7)-(2′-aminoethyl)-amino-1-cyclopropyl-3-carboxylic acid (2′-hydroxyethyl) amides and 4 …

S Kapić, A Fajdetić, S Koštrun, A Čikoš… - Bioorganic & medicinal …, 2011 - Elsevier
A set of novel macrolones containing the flexible C8 basic linker and quinolone 3-(2′-
hydroxyethyl) carboxamido group has been prepared and structurally characterized by NMR …

Synthesis, activity and pharmacokinetics of novel antibacterial 15-membered ring macrolones

A Fajdetić, A Vinter, HČ Paljetak, J Padovan… - European journal of …, 2011 - Elsevier
Synthesis, antibacterial activity and pharmacokinetic properties of a novel class of macrolide
antibiotics—macrolones—derived from azithromycin, comprising oxygen atom (s) in the …

Synthesis and structure–activity relationship of a novel class of 15-membered macrolide antibiotics known as '11a-azalides'

T Sugimoto, T Tanikawa, K Suzuki… - 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 …

Desmethyl macrolides: synthesis and evaluation of 4-desmethyl telithromycin

I Glassford, M Lee, B Wagh, V Velvadapu… - ACS Medicinal …, 2014 - ACS Publications
Novel sources of antibiotics are needed to address the serious threat of bacterial resistance.
Accordingly, we have launched a structure-based drug design program featuring a …

Recent advances in the field of 16-membered macrolide antibiotics

W Cui, S Ma - Mini Reviews in Medicinal Chemistry, 2011 - ingentaconnect.com
The continuing emergence of bacterial resistance has provided an incentive for recent
intensified research on macrolide antibiotics. Belonging to the macrolide family, 16 …

Synthesis and Antibacterial Activity of a Novel Class of 15-Membered Macrolide Antibiotics,“11a-Azalides”

T Sugimoto, T Tanikawa - ACS Medicinal Chemistry Letters, 2011 - ACS Publications
An efficient method for the reconstruction of the 9-dihydroerythromycin A macrolactone
skeleton has been established. The key steps are oxidative cleavage at the 11, 12-position …

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 …