Patent classifications
C07D501/26
6,7-trans cephalosporin-based probes for detecting bacteria expressing a metallo-beta-lactamase
The present invention discloses a probe useful for the selective detection of metallo-beta-lactamases, in particular carbapenemases, thereby distinguishing those species of bacteria that are carbapenem-resistant from bacterial strains that are sensitive. Cephalospori based probes that have the 6,7 R,R configuration are susceptible to cleavage by beta-lactamases but cannot distinguish between cleavage by metallo-beta-lactamases and other beta-lactamases. By modifying a side group of the cephalosporin, selectivity can be introduced allowing the probes to distinguish between various types of metallo-beta-lactamases.
6,7-trans cephalosporin-based probes for detecting bacteria expressing a metallo-beta-lactamase
The present invention discloses a probe useful for the selective detection of metallo-beta-lactamases, in particular carbapenemases, thereby distinguishing those species of bacteria that are carbapenem-resistant from bacterial strains that are sensitive. Cephalospori based probes that have the 6,7 R,R configuration are susceptible to cleavage by beta-lactamases but cannot distinguish between cleavage by metallo-beta-lactamases and other beta-lactamases. By modifying a side group of the cephalosporin, selectivity can be introduced allowing the probes to distinguish between various types of metallo-beta-lactamases.
Synthesis process of precursors of derivatives of beta-lactam nuclei and precursors and derivatives thereof
A synthesis process of precursors of derivatives of beta-lactam compounds, said beta-lactam compounds being selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, comprising the following steps: a) protection of the amine group of the beta-lactam compound, selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, through the formation of a carbamate by reaction with a dicarbonate; b) esterification of the carboxyl group in position 2 of the beta-lactam compound obtained in step a) by reaction with propargyl alcohol.
Synthesis process of precursors of derivatives of beta-lactam nuclei and precursors and derivatives thereof
A synthesis process of precursors of derivatives of beta-lactam compounds, said beta-lactam compounds being selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, comprising the following steps: a) protection of the amine group of the beta-lactam compound, selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, through the formation of a carbamate by reaction with a dicarbonate; b) esterification of the carboxyl group in position 2 of the beta-lactam compound obtained in step a) by reaction with propargyl alcohol.
SYNTHESIS PROCESS OF PRECURSORS OF DERIVATIVES OF BETA-LACTAM NUCLEI AND PRECURSORS AND DERIVATIVES THEREOF
A synthesis process of precursors of derivatives of beta-lactam compounds, said beta-lactam compounds being selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, comprising the following steps: a) protection of the amine group of the beta-lactam compound, selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, through the formation of a carbamate by reaction with a dicarbonate; b) esterification of the carboxyl group in position 2 of the beta-lactam compound obtained in step a) by reaction with propargyl alcohol.
SYNTHESIS PROCESS OF PRECURSORS OF DERIVATIVES OF BETA-LACTAM NUCLEI AND PRECURSORS AND DERIVATIVES THEREOF
A synthesis process of precursors of derivatives of beta-lactam compounds, said beta-lactam compounds being selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, comprising the following steps: a) protection of the amine group of the beta-lactam compound, selected from 6-aminopenicillanic acid and 7-aminocephalosporanic acid, preferably 6-aminopenicillanic acid, through the formation of a carbamate by reaction with a dicarbonate; b) esterification of the carboxyl group in position 2 of the beta-lactam compound obtained in step a) by reaction with propargyl alcohol.
β-lactamase substrates and methods of their use for the diagnosis of tuberculosis
-Lactamase substrates and methods for using the substrates to detect -lactamase diagnose tuberculosis.
β-lactamase substrates and methods of their use for the diagnosis of tuberculosis
-Lactamase substrates and methods for using the substrates to detect -lactamase diagnose tuberculosis.