6250-76-6Relevant academic research and scientific papers
CARBAPENEM ANTIBACTERIALS WITH GRAM-NEGATIVE ACTIVITY AND PROCESSES FOR THEIR PREPARATION
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Page/Page column 75, (2008/06/13)
The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administ
2-Substituted Penems with Amino Acid-Related Side Chains: Synthesis and Antibacterial Activity of a New Series of β-Lactam Antibiotics
Altamura, Maria,Perrotta, Enzo,Sbraci, Piero,Pestellini, Vittorio,Arcamone, Federico,et al.
, p. 4244 - 4256 (2007/10/03)
A new series of 6-(hydroxyethyl)penems 2-substituted with amino acid-related side chains was synthesized.The nature of the amino acyl derivative proved to be crucial both from a synthetic point of view, as β-lactam ring opening can compete with C-2 nucleophilic substitution, and for antibacterial activity.Primary amino acid amides emerged as the most suitable side chains for enhancing permeability through a Gram-negative outer membrane.In vitro activity of the new 2-penems 3a-u was influenced by the nature and position of the amide moiety, the ring size for cyclic amides, and the configuration of the amino acid.Compounds bearing amides derived from small N-methyl amino acids (such as 3a) or from cyclic amino acids (such as prolinamide 3p and 4-hydroxyprolinamide 3r) showed broad spectrum in vitro activity against both Gram-positive and Gram-negative microorganisms.
Aqueous Solutions Containing Amino Acids and Peptides. Part 19: The Enthalpic Coefficients for the Interactions of N-Acetylsarcosinamide with 2-(N-acetylamino)acyl Amides at 25 deg C
Blackburn, G. M.,Lilley, T. H.,Milburn, P. J.
, p. 789 - 804 (2007/10/02)
Enthalpies of dilution both of solutions of N-acetylsarcosinamide and of ternary solutions equimolal in N-acetylsarcosinamide and N-acetylglycinamide, N-acetyl-L-alaninamide, N-acetyl-L-valinamide or N-acetyl-L-leucinamide have been determined by a microc
