111491-95-3Relevant academic research and scientific papers
Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase
Ronkin, Steven M.,Badia, Michael,Bellon, Steve,Grillot, Anne-Laure,Gross, Christian H.,Grossman, Trudy H.,Mani, Nagraj,Parsons, Jonathan D.,Stamos, Dean,Trudeau, Martin,Wei, Yunyi,Charifson, Paul S.
scheme or table, p. 2828 - 2831 (2010/08/19)
Bacterial DNA gyrase is an attractive target for the investigation of new antibacterial agents. Inhibitors of the GyrB subunit, which contains the ATP-binding site, are described in this communication. Novel, substituted 5-(1H-pyrazol-3-yl)thiazole compounds were identified as inhibitors of bacterial gyrase. Structure-guided optimization led to greater enzymatic potency and moderate antibacterial potency. Data are presented for the demonstration of selective enzyme inhibition of Escherichia coli GyrB over Staphlococcus aureus GyrB.
α-Amino Ketones - A Contribution to the Synthesis of Optically Active Derivatives of Amino Acids and Peptides
Fittkau, Siegfried,Jahreis, Guenther,Peters, Klaus,Balaspiri, Lajos
, p. 529 - 538 (2007/10/02)
The synthesis of N-Z-protected methyl ketones from amino acids via the chloromethyl ketones and dehalogenation of the latter with zinc in glacial acetic acid is described.Deprotection of the methyl ketones results in the formation of hydrohalogenides of the α-aminoalkyl methyl ketones further converted to N-acylated peptide ketones as analogs of peptide hormones or as competitively acting substrate analogs of proteolytic enzymes.Aminoacetone is conveniently prepared as well as methyl-pyrrolidyl ketone and methyl-piperidyl ketone.
