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
Nové skupiny potenciálních antituberkulotik: 3-(4-ethoxythiokarbonylfenyl)-2H-benzoxazin-2,4(3H)-dithiony a 3-(4-ethoxythiokarbonylfenyl)-4-thioxy-2H-benzoxazin-2,4(3H)--ony
V souvislosti s pátráním po nových antituberkulotikách jsme připravili skupinu derivátů 3-(4-ethoxythiokarbonylfenyl)-2H-benzoxazin-2,4(3H)-dithionu a 3-(4-ethoxythiokarbonylfenyl)-4-thioxy-2H-benzoxazin-2(3H)-onu. Obměny substituentů byly prováděny na benzoxazinovém kruhu. Studievycházela z našich předchozích předpokladů, že záměna oxo skupiny za thioxo skupinu je spojenas růstem antimykobakteriální aktivity. Připravené sloučeniny byly hodnoceny aktivitou vůči Mycobacteriumtuberculosis,Mycobacterium kansasii aMycobacterium avium. Došli jsme však k poznatku,že ve skupinách derivátů 3-(4-ethoxythiokarbonylfenyl)-4-thioxy-2H-benzoxazin-2(3H)-onua 3-(4-ethoxythiokarbonylfenyl)-2H-benzoxazin-2,4(3H)-dithionu nedochází k předpokládanémuzvýšení antimykobakteriální aktivity.
Klíčová slova:
benzoxazin – mycobacterium – tuberkulostatika – thiony
Authors:
K. Waisser; P. Holý; O. Bureš; J. Kuneš; J. Kaustová 1
Authors‘ workplace:
Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Králové, 1Krajská hygienická stanice, Ostrava
Published in:
Čes. slov. Farm., 2003; , 42-47
Category:
Overview
In connection with the search for new antituberculotics, the present authors prepared a group ofderivatives 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 carriedout on the benzoxazine ring. The study was based on the present authors’ previous assumptionthat the substitution of the oxo group for the thioxo group was connected with an increase inantimycobacterial activity. The prepared substances were evaluated by the activity against Mycobacteriumtuberculosis, Mycobacterium kansasii, and Mycobacterium avium. However, it was concludedthat there was no assumed increase in antimycobacterial activity in the groups of3-(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
Labels
Pharmacy Clinical pharmacologyArticle was published in
Czech and Slovak Pharmacy
2003 Issue 1
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