Effect of Assay Medium on the Antibacterial Activity of Certain Penicillins and Cephalosporins

Pursiano, T. A.; Misiek, M.; Leitner, F.; Price, K. E.

doi:10.1128/aac.3.1.33

Cited by 32 publications

(19 citation statements)

References 9 publications

(6 reference statements)

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“…We carried out the screening experiments for the antibacterial activity [15,16] of β-lactams (±)-10-15 as well as the reference compounds cephalothin (16) [2] and penicillin G (17) [17]. The experiments were performed in vitro against different strains of four pathogenic microorganisms.…”

Section: Biological Activitymentioning

confidence: 99%

Design, Synthesis, and Antibacterial Activity of Novel Carbacephems

Moosavi‐Movahedi¹,

Yen²,

Chamani³

et al. 2006

LDDD

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Syntheses of (±)-cis-3-hydroxycarbonyl-7-(phenylacetamido)carbacephem (10 ), (±)-cis-3-methoxycarbonyl-7-(phenylacetamido)carbacephem (11 ), (±)-cis-2-chloro-3-hydroxycarbonyl-7-(phenylacetamido)carbacephem (14 ), and (±)-cis-2-chloro-3-methoxycarbonyl-7-(phenylacetamido)carbacephem (15 ) were accomplished. These four heretofore undescribed compounds 10 , 11 , 14 , and 15 showed notable activity against Staphylococcus aureus FDA 209P, Escherichia coli ATCC 39188, Pseudomonas aeruginosa 1101-75, Klebsiella pneumoniae NCTC 418 as well as the β-lactamase producing organisms E. coli A9675, P. aeruginosa 18S-H and methicillin-resistant organism S. aureus 95. The electronic activation of lactam moieties of 11 and 15 enhanced remarkably their antibacterial activity relative to those of the 10 and 14 . The chlorine atom in 14 and 15 , acting as an effective leaving group, also resulted in an increment in the biological activity in comparison with those of the parent carbacephemes 10 and 11 . The mode of action related to 14 and 15 can be explained by a non-classical [1,4]-elimination process.

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Section: Biological Activitymentioning

confidence: 99%

Design, Synthesis, and Antibacterial Activity of Novel Carbacephems

Moosavi‐Movahedi¹,

Yen²,

Chamani³

et al. 2006

LDDD

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“…Our data agree with the latter study. The reason for the difference in results is probably related to the marked effect of culture media on BL-P1654 (17,21). The weakly basic BL-P1654 has up to a 40-fold reduction in activity on MHA as compared to nutrient broth.…”

Section: Resultsmentioning

confidence: 99%

“…Carbenicillin, which is acidic, does not show this variation. MHA is a more reliable indicator of the relative in vivo potency of BL-P1654 and carbenicillin than nutrient agar (17). The …”

Section: Resultsmentioning

confidence: 99%

Activity of Three Aminoglycosides and Two Penicillins Against Four Species of Gram-Negative Bacilli

Weinstein

Young

Hewitt

1975

Antimicrob Agents Chemother

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Three aminoglycoside antibiotics and two penicillins were compared for their in vitro activity against 60 isolates of Serratia, Pseudomonas, Proteus mirabilis , and indole-positive Proteus sp. Testing was done by the agar dilution method using Mueller-Hinton broth solidified with 1.5% agar. The activity of amikacin, aminodeoxybutirosin, and gentamicin against Proteus and Pseudomonas , as related to their peak blood levels, showed no significant differences. Amikacin was the most active against Serratia marcescens . Results using Mueller-Hinton media in broth dilution tests correlated with the agar dilution method except for Pseudomonas aeruginosa . The minimal inhibitory concentration for aminoglycosides in agar was considerably greater than the minimal inhibitory concentration in Mueller-Hinton broth, and the disparity was related to the higher divalent cation concentration of agar. BL-P1654 and carbenicillin were similar except that carbenicillin was much more active against indole-positive Proteus sp. Additionally, the ratio of bactericidal to bacteriostatic concentrations of BL-P1654 was considerably greater than for carbenicillin.

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“…Biological activity: We carried out the screening experiments for antimicrobial activities [10,11] of b-lactams (AE)-13 ± (AE)-16, a mixture of (AE)-13 and (AE)-15 (1:1 w/w), as well as the reference compounds ampicillin (25), amoxicillin (26), penicillin G (27), and clavulanic acid (28). The experiments were performed in vitro against different strains of five pathogenic microorganisms up to 128 mg mL…”

Section: Discussionmentioning

confidence: 99%

Concept of Counterattack Reagents: Intramolecular Counterattack Strategy in the Synthesis of Biologically Active Isopenams

et al. 1999

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A novel strategy was developed for the synthesis of isopenams in high yields. The strategy involves use of the intramolecular counterattack process in the conversions of (AE)-5 3(AE)-11, (AE)-6 3(AE)-12, and (AE)-19 3(AE)-11. Catalytic hydrogenation of (AE)-11 afforded isopenam (AE)-13, which possessed notable antimicrobial activities. Oxidation of (AE)-13 with KMnO 4 gave sulfone (AE)-15, which functioned as a potent inhibitor of various bacterial blactamases. Sulfone (AE)-15 exerted a great synergistic effect on antimicrobial agent (AE)-13. Results from the CVFF calculations of the C-2 b-epimer of isopenam 13 (i.e., 23) and the corresponding sulfone derivative 24 indicate the existence of a severe electronic repulsion between the b-lactam carbonyl and the C-2 carboxyl groups. Steric interaction also exists between the C-6 amide side chain and the C-2 carboxylic acid moiety in 23 and 24. These interactions, however, do not exist in the corresponding a-epimers 13 and 15.

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Effect of Assay Medium on the Antibacterial Activity of Certain Penicillins and Cephalosporins

Cited by 32 publications

References 9 publications

Design, Synthesis, and Antibacterial Activity of Novel Carbacephems

Design, Synthesis, and Antibacterial Activity of Novel Carbacephems

Activity of Three Aminoglycosides and Two Penicillins Against Four Species of Gram-Negative Bacilli

Concept of Counterattack Reagents: Intramolecular Counterattack Strategy in the Synthesis of Biologically Active Isopenams

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