New Groups of Potential Antituberculotics: 3-(4-Ethoxythiocarbonylphenyl)-2H-benzoxazin-
2,4(3H)-dithiones and 3-(4-Ethoxythiocarbonylphenyl)-4-thioxy-2H-benzoxazin-
-2,4(3H)-ones
WAISSER K., HOLÝ P., BUREŠ O., KUNEŠ J., KAUSTOVÁ J.1
Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Králové, 1Krajská hygienická stanice, Ostrava |
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Summary:
In connection with the search for new antituberculotics, the present authors prepared a group of
derivatives of 3-(4-ethoxythiocarbonylphenyl)-2H-benzoxazin-2,4(3H)-dithione and 3-(4-ethoxythiocarbonylphenyl)-
4-thioxy-2H-benzoxazin-2,4(3H)-one. The modifications of substituents were carried
out on the benzoxazine ring. The study was based on the present authors’ previous assumption
that the substitution of the oxo group for the thioxo group was connected with an increase in
antimycobacterial activity. The prepared substances were evaluated by the activity against Mycobacterium
tuberculosis, Mycobacterium kansasii, and Mycobacterium avium. However, it was concluded
that there was no assumed increase in antimycobacterial activity in the groups of
3-(4-ethoxythiocarbonylphenyl)-4-thioxy-2H-benzoxazin-2,4(3H)-one and 3-(4-ethoxythiocarbonylphenyl)-
2H-benzoxazin-2,4(3H)-dithione derivatives.
Key words:
benzoxazin – mycobacterium – tuberculostatics – thiones
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