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Biomedical subjects

A C Barnes

Publications and source records attributed to A C Barnes.

At least 19 recordsLinked to original sources

In vitro susceptibility of the fish pathogen Aeromonas salmonicida to flumequine.

The activity of the fluoroquinolone flumequine was investigated against the fish pathogen Aeromonas salmonicida and was compared with that of oxolinic acid. Flumequine was more active than oxolinic acid in terms of its MIC against oxolinic acid-resistant isolates of A. salmonicida and was as active as oxolinic acid against susceptible isolates. In contrast to oxolinic acid, flumequine was bactericidal, with only 1% of the bacteria surviving 6 h of exposure to the drug at concentrations slightly above the MIC. Mutation to resistance to flumequine was found to occur at a lower frequency than that to oxolinic acid. Hence, in vitro, flumequine appears to possess some advantages over oxolinic acid against this fish pathogen.

Aeromonas

Cross resistance between oxytetracycline and oxolinic acid in Aeromonas salmonicida associated with alterations in outer membrane proteins.

Oxytetracycline resistant mutants of Aeromonas salmonicida isolated from mutation frequency experiments showed decreased susceptibility to oxolinic acid. Outer membrane preparations of these resistant mutant strains revealed a major protein, with a molecular mass of approximately 37 kDa, which was not present in significant quantities in the parent strain.

Aeromonas

In vitro activities of 4-quinolones against the fish pathogen Aeromonas salmonicida.

The activities of five fluorinated 4-quinolones, namely, sarafloxacin, enrofloxacin, PD127391, PD117596, and CI934, against the fish pathogen Aeromonas salmonicida were investigated and compared with that of oxolinic acid. The results indicated that with the exception of CI934, these drugs are more active than oxolinic acid in terms of MIC. No inoculum effect was observed, but the drugs were less active at 10 degrees C than at 22 degrees C. The presence of 3% of NaCl caused an increase in drug activity. Resistance to the drugs appeared to be fairly stable, with only a small decrease in activity after 10 successive passages of the test strains on drug-free tryptone soya agar.

Aeromonas

Synthesis and oral antiallergic activity of carboxylic acids derived from imidazo[2,1-c][1,4]benzoxazines, imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles.

4H-Imidazo[2,1-c][1,4]benzoxazine-2-carboxylic acid (3) was found to possess potent activity in the IgE-induced rat passive cutaneous anaphylaxis model which may be predictive of clinical antiallergic activity. Compared to disodium cromoglycate (DSCG, 1), 3 was less active following iv administration but unlike DSCG showed very significant oral activity. To explore the structural requirements for this activity, a range of tricyclic compounds was prepared and their activities were measured. Individual 2-carboxylic acids derived from imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles showed iv activities up to 10(3) times as potent as DSCG and many of them showed significant oral activity. From these, imidazo[1,2-a]quinoxaline-2-carboxylic acid 114 has been chosen for further development.

Animals

Pharmacologically active sulfoximides: 5-hexyl-7-)S-methylsulfonimidoly) xanthone-2-carboxylic acid, a potent antiallergic agent.

The antiallergic activity of some xanthone derivatives containing a sulfoximide substitutent has been investigated. While 2-(S-methylsulfonimidoyl)xanthone itself was found to be inactive, a series of 7-(S-methylsulfonimidoly)-xanthone-2-carboxylic acids showed good levels of activity in the passive cutaneous anaphylaxis screen. N-Substituted sulfoximide derivatives were, without exception, less active than the corresponding unsubstituted compounds. The activity of the 7-(S-methylsulfonimidoyl)xanthone-2-carboxylic acids could be enhanced by the introduction of an alkyl or alkoxy substituent at C-5. As a result of these studies, 5-hexyl-7(S-methylsulfonimidoyl)xanthone-2-carboxylic acid has been selected for further investigation as an antipasthmatic agent.

Animals