In vitro activity of carumonam (RO 17-2301) and twelve other antimicrobials against clinical isolates ofPseudomonas aeruginosa

Abstract

Minimal inhibitory concentrations of the monobactam carumonam (RO 17-2301) and twelve other antimicrobials were determined using agar dilution against 140 recent non-replicate clinical isolates of Pseudomonas aeruginosa. The most active drugs were ciprofloxacin, amikacin, imipenem and ceftazidime, inhibiting 96, 91, 90 and 86 percent of the strains, respectively, at or below the susceptibility threshold. The monobactams carumonam and aztreonam were active against 78 and 65 percent of the strains, respectively. Tobramycin inhibited 68 percent of the strains, and gentamicin and netilmicin 50 and 21 percent, respectively. Analysis of correlation coefficients revealed a low correlation between imipenem and the other beta-lactams and a remarkably good correlation between the beta-lactams (excepting imipenem) and the aminoglycosides.

Antibacterial and β‐Lactamase Inhibitory Activity of Monocyclic β‐Lactams

“…The structure-activity relationships of aztreonam 5 are presented in Figure 3. 48 As the discovery, development, 9,53,55 as well as the general activity against multiple bacterial species, pharmacokinetics and clinical and pharmacological aspects have been described extensively in the past; [46][47][48][56][57][58][59][60][61][62][63] this review will not go into further detail on the properties of aztreonam 5. Also the β-lactamase stability has been described repeatedly.…”

Enantioselective hydrolysis of 3,4-disubstituted β-lactams. An efficient enzymatic method for the preparation of a key Taxol side-chain intermediate

“…A large number of recent published articles and reviews have stressed the biological and chemical importance of ␤-lactams and ␤-amino acids [1]. Molecules containing a 2-azetidinone ring may possess antibacterial activity, e.g., carumonam is a ␤-lactamaseresistant monobactam antibiotic [2], while others containing a cis 3,4-disubstituted ␤-lactam ring may display PPAR ␣/␥ agonist [3], vasopressin VIa agonist [4] or anticancer [5,6] activity. ␤-Amino acids and some of their derivatives are widely used in combinatorial, peptide, organic and medicinal chemistry [7][8][9].…”

Preparation of pharmaceutically important enantiomer components through lipase catalysed acylation and hydrolysis

“…Carumonam is a β-lactamase-resistant monobactam antibiotic, 17 while others containing a cis-3,4-disubstituted β-lactam ring may display PPAR α/γ agonist, 18 vasopressin VIa agonist 19 or anticancer activity. 20,21 The enantiomers of 2-azabicyclo[2.2.1]hept-5-en-3-one are building blocks of pharmaceutically important molecules exhibiting antiviral or antibacterial activity.…”