132496-71-0

Upstream product

• 108098-45-9 2,5-dichloro-3,4-dihydroxybenzoic acid 
• 824-94-2 p-methoxybenzyl chloride 
• 2746-25-0 p-Methoxybenzyl bromide 

Downstream Products

• 132496-72-1 2,5-Dichloro-3,4-di-p-methoxybenzyloxybenzylalcohol 
• 1225208-51-4 C₃₀H₃₃Cl₂N₇O₁₀S₂ 
• 1225208-52-5 2,5-dichloro-3,4-bis((4-methoxybenzyl)oxy)-N-(2-(pyrrolidin-1-yl)ethyl)benzamide 

Relevant academic research and scientific papers

Cefiderocol (S-649266), A new siderophore cephalosporin exhibiting potent activities against Pseudomonas aeruginosa and other gram-negative pathogens including multi-drug resistant bacteria: Structure activity relationship

The structure-activity relationship (SAR) for a novel series of catechol conjugated siderophore cephalosporins is described with their in vitro activities against multi-drug resistant Gram-negative pathogens including Pseudomonas aeruginosa, Acinetobacter baumannii, Stenotrophomonas maltophilia and Enterobacteriaceae. Cefiderocol (3) was one of the best molecules which displayed well-balanced and potent activities against multi-drug resistant Gram-negative pathogens including carbapenem resistant bacteria among the prepared compounds with the modified C-7 side chain and the modified C-3 side chain. Cefiderocol (3) is a highly promising parenteral cephalosporin for the treatment of multi-drug resistant Gram-negative infection.

CEPHALOSPORIN HAVING CATECHOL GROUP

The present invention provides Cephem compounds which have a wide antimicrobial spectrum and have potent antimicrobial activity against beta-lactamase producing Gram negative bacteria as follows: A compound of the formula: wherein, X is N, CH or C-Cl; T is S or the like; A and G are lower alkylene or the like; B is a single bond or the like; D is a single bond, -NR7-, -CO-, -CO-NR7-, -NR7-CO-, -NR7-CO-NR7-, or the like; E is optionally substituted lower alkylene; F is a single bond or optionally substituted phenylene; R3, R4, R5 and R6 each is independently hydrogen, halogene, nitrile, or the like; or an ester, a compound protected at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.

Piperaziniocephalosporins

Antibacterial hydroxyarylpiperazinocephalosporins of the formula: STR1 wherein R1 is amino or acylamino; R2 is H or methoxy; R3 is alkyl; R4 is --(P--C--Q)n --, where P and Q each are H, alkyl or OH, or P and Q combine to form oxo, and n is 0 or 4; R5 is substituted or unsubstituted hydroxyaryl; R6 has a negative charge and is COO, or an anion in combination with an optionally protected carboxy; and X is O, S or S→O; an antibacterial preparation containing the same; a method for killing bacteria and preventing or treating bacterial infection by using the same; and syntheses of the cephalosporins are provided.

Cephalosporin compounds and their use

A cephalosporin compound of the formula (I): wherein X and Y may be the same or different and are a hydrogen or halogen atom; Z is a hydrogen or halogen atom, -CH=CH2, -CH=CH-CH3, -OR1, -SR2 or -CH2W in which R1 and R2 are a lower alkyl group and W is a hydrogen atom or a nucleophilic residue, its pharmaceutically acceptable salt, a process for preparing the same and their antibacterial composition.