158495-65-9Relevant academic research and scientific papers
Synthesis and antimicrobial activity of novel 3- [(aminopyrimidiniumyl)thio]methyl cephalosporins
Kim,Lim,Yeo,Bang,Kim,Kim,Woo -,Yang,Oh,Nahm
, p. 3828 - 3833 (2007/10/02)
A series of novel cephalosporin compounds which have 3- [(aminopyrimidiniumyl)thio]methyl substituents was synthesized. They show high antimicrobial activity against various bacterial species including Pseudomonas aeruginosa. Structure-activity relationships with various thiopyrimidines, thiopyrimidiniums, bicyclic thiotriazolopyrimidiniums, and bicyclic thioimidazolopyrimidiniums as 3'-substituents were also studied; cephalosporins with quarternized pyrimidinium moieties have better antimicrobial activities than neuteral pyrimidine cephalosporins, and stabilization of the positive charge on the pyrimidinium moieties is essential for better activity. According to semiempirical PM3 calculations, amino and alkylthio substituents on the pyrimidinium rings play a major role in charge stabilization and delocalization.
Novel cephalosporin compounds and processes for the preparation thereof
-
, (2008/06/13)
The present invention relates to novel cephalosporin compounds, pharmaceutically acceptable non-toxic salts, physiologically hydrolyzable esters, hydrates and solvates and isomers thereof which possess potent and broad antibacterial activities. The compounds of the present invention have a (1,5,6-substituted-4-aminopyrimidinium-2-yl)thiomethyl group in 3-position of the cephem nucleus and is specifically represented by the following formula(I): ψψψ
