- Relationships between the chemical structure of antimycobacterial substances and their activity against atypical strains. Part 14: 3-Aryl-6,8-dihalogeno-2H-1,3-benzoxazine-2,4(3H)-diones)
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A set of eight derivatives of 6,8-dichloro-3-phenyl-2H-benzoxazine-2,4(3H)-dione and nine derivatives of 6,8-dibromo-3-phenyl-2H-1,3-benzoxazine-2,4(3H)-dione, substituted on the phenyl ring, was prepared by the reaction of the corresponding salicylanilides with ethyl chloroformate. The compounds were evaluated in vitro for antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii, and Mycobacterium avium. Their activity increases with increasing hydrophobicity and electron-withdrawing ability of the substituents on the phenyl ring.
- Waisser, Karel,Hladuvkova, Jana,Gregor, Jiri,Rada, Tomas,Kubicova, Lenka,Klimesova, Vera,Kaustova, Jarmila
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- Dihydro benzoxazinones and benzoxazinediones' derivatives : thesis and study as bactericides and fungicides
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A series of 3,4 dihydro 2 H 1,3 benzoxazine 2,4 diones and 3,4 dihydro 2 H 1,3 benzoxazine 4 ones were synthesized from several salicylamides and salicylanilides. Their antibacterial and antifungal activities in vitro were studied on Staphylococcus aureus 209 P A.T.C.C. (6538 P), Pseudomonas aeruginosa I.P. C.C.E.B. 481, Escherichia coli K 12 C600 (λ-) and Candida albicans. Always negative on colibacillus, activity on Staphylococcus aureus seems to be conditioned by presence of halogeno or nitro substituents: one of the compounds is notably active. Transformation into the heterocyclic derivative generally lowers or cancels action on Candida albicans; conversely, it frequently provokes action on Bacillus pyocyaneus on which some monoketonic derivatives were quite effective.
- Devaux,Renaudie,Boineau,et al.
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