Waisser K, Holý P, Bures O, Kunes J, Kaustová J
Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Králové.
Ceska Slov Farm. 2003 Jan;52(1):42-7.
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.
在寻找新型抗结核药物的过程中，本文作者制备了一组3-(4-乙氧基硫代羰基苯基)-2H-苯并恶嗪-2,4(3H)-二硫酮和3-(4-乙氧基硫代羰基苯基)-4-硫代-2H-苯并恶嗪-2,4(3H)-酮的衍生物。取代基的修饰是在苯并恶嗪环上进行的。该研究基于本文作者之前的假设，即氧代基团被硫代氧代基团取代与抗分枝杆菌活性的增加有关。通过对结核分枝杆菌、堪萨斯分枝杆菌和鸟分枝杆菌的活性来评估所制备的物质。然而，得出的结论是，在3-(4-乙氧基硫代羰基苯基)-4-硫代-2H-苯并恶嗪-2,4(3H)-酮和3-(4-乙氧基硫代羰基苯基)-2H-苯并恶嗪-2,4(3H)-二硫酮衍生物组中，抗分枝杆菌活性没有出现预期的增加。
