A note to the biological activity of benzoxazine derivatives containing the thioxo group.
New 3-benzyl-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones and 3-benzyl-2H-1,3-benzoxazine-2,4(3H)-dithiones were synthesized. The compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium. The replacement of the carbonyl group by the thiocarbonyl group increased the antimycobacterial activity. The most active derivatives were more active than isonicotinhydrazide (INH). The cytotoxicity and the antiproliferative activity were studied as well.
Waisser
Karel
K
Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Heyrovský-Str. 1203, 50005 Hradec Králové, Czech Republic. waisser@faf.cuni.cz
Petrlíková
Eva
E
Perina
Milan
M
Klimesová
Vera
V
Kunes
Jirí
J
Palát
Karel
K
Kaustová
Jarmila
J
Dahse
Hans-Martin
HM
Möllmann
Ute
U
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D048588:Benzoxazines / Q000737:chemistry* / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects
D000900:Anti-Bacterial Agents; D048588:Benzoxazines