Synthesis and biological activity of 4″-O-acyl derivatives of 14- and 15-membered macrolides linked to ω-quinolone-carboxylic unit

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

“…Lengthening of the linker by incorporating two oxygen atoms and a nitrogen atom, compound 29, gave an improved antimicrobial activity and oral bioavailability (10.7%) in comparison to other tested non-ester compounds. These results are in line with previously reported PK data for azithromycin derivatives of the same linker length [29]. Compound 29 is characterized by a low CLs (13% LBF), a large Vd (10.7 L/kg) and long t 1/2 (9.1 h).…”

Od vitamina do antibiotika – sjećanja jednog kemičara II. dio

“…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.…”

Design, Synthesis, Antibacterial Evaluation and Docking Study of Novel 2‐Hydroxy‐3‐(nitroimidazolyl)‐propyl‐derived Quinolone

“…Moreover, increasing bulk at C-7 position is tolerated (12). Thus, much effort has been made on the structural modification of C-7 position in quinolones by incorporating several bioactive moieties including macrolides (13,14), oxazolidinones (15), triazoles (16), 5-(nitroaryl)-1,3,4-thiadiazoles (17,18) and sulfonamides (19,20). This led to obtaining quinolone hybrids as a new class of antimicrobial agents (21).…”