1251931-75-5

Upstream product

• 697762-43-9 ethyl 3-(dimethylamino)-2-[(2-fluoro-5-iodophenyl)carbonyl]-2-propenoate 
• 75-04-7 ethylamine 
• 124700-41-0 2-fluoro-5-iodobenzoic acid 
• 924-99-2 ethyl 3-(dimethylamino)acrylate 
• 186584-73-6 2-fluoro-5-iodobenzoyl chloride 

Downstream Products

• 869310-65-6 1-ethyl-4-oxo-6-[3-({2-[(phenylmethyl)oxy]ethyl}oxy)-1-propyn-1-yl]-1,4-dihydro-3-quinolinecarboxylic acid 
• 1251931-78-8 1-ethyl-4-oxo-6-[3-({2-[(phenylmethyl)oxy]ethyl}oxy)propyl]-1,4-dihydro-3-quinolinecarboxylic acid 
• 1251931-77-7 C₁₅H₁₇NO₃ 

Relevant academic research and scientific papers

Macrolide and carbostyril heterocomplex and preparation method thereof

The invention provides a macrolide and carbostyril heterocomplex. The macrolide and carbostyril heterocomplex is characterized by comprising compounds shown in the formula I and the formula II, or thecompounds shown in the formula I and the formula II and

Erythromycin derivative and preparing method thereof

The invention provides an erythromycin derivative. The erythromycin derivative is characterized by comprising a compound in a general formula I or comprising pharmaceutically-acceptable salt formed with the compound in the general formula I and inorganic

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

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 erythromycin ketolides were synthesized and evaluated. Incorporation of substituted heteroaryl groups (a - m), in contrast to previously reported the unsubstituted heteroaryl groups, proved to the beneficial for enhancement of the activities of the 9-propgargyl ketolide 8 series and the 9-allyl ketolide 14 series. But these aryl groups (a - m) cannot supply the resulting compounds 8 and 14, unlike corresponding the 6-allyl ketolide 20 series, with activity against constitutively resistant Streptococcus pneumoniae. However, hybrids of macrolides and quinolones (8, 14 and 20, Ar = n - t) exhibited not only high activities against susceptible, inducibly erm-mediated resistant, and efflux-mediated resistant strains, but also significantly improved potencies against constitutively resistant Streptococcus pneumoniae and Streptococcus pyogenes. The capacity was highlighted by introduction of newly designed carbamoyl quinolones (q, r, s and t) rather than commonly seen carboxy quinolones (o and p) as the pharmacophores. Structure-activity relationships and molecular modelling indicated that 8r, 14r and 20q may have different binding sites compared to current erythromycins. Moreover, 8r, 14r and 20q have 2.5–3.6 times prolonged half-life and 2.3- to 2.6-fold longer mean residence time in vivo over telithromycin. These findings pave the way for rational design of novel non-telithromycin macrolides that target new binding sites within bacterial ribosomes.

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

The synthesis and antimicrobial activity of a new class of macrolide antibiotics which consist of a macrolide scaffold and a quinolone unit covalently connected by an appropriate linker are described. Optimization of several synthetic steps and structural

Initial Scale-Up and Process Improvements for the Preparation of a Lead Antibacterial Macrolone Compound

Macrolones are a novel class of potent antimicrobial agents that consist of a macrolide scaffold to which a quinolone unit is tethered by various linkers to the 4 -O-position of the cladinose sugar. In this paper is described a modified 13-step route to a