The oriented development of antituberculotics (Part II):: Halogenated 3-(4-alkylphenyl)-1,3-benzoxazine-2,4-(3H)-diones

被引:13
作者
Waisser, Karel
Matyk, Josef
Divisova, Hana
Husakova, Petra
Kunes, Jiri
Klimesova, Vera
Palat, Karel
Kaustova, Jarmila
机构
[1] Charles Univ Prague, Fac Pharm Hradec Kralove, Dept Inorgan & Organ Chem, CZ-50005 Hradec Kralove, Czech Republic
[2] Reg Inst Publ Hlth, Dept Diagnost Mycobacteria, Ostrava, Czech Republic
关键词
antimycobacterial activity; antituberculotic activity; benzoxazine; tuloerculostatics;
D O I
10.1002/ardp.200600002
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Based on our previous studies, 21 new halogenated 3-(4-allcylphenyl)-1,3-benzoxazine-2,4-(3H)-diones were synthesized by the reaction of salicylanilides and methyl-chloroformate. All compounds were screened in vitro against three different strains of mycobacterium, and Free-Wilson method was used to establish structure-activity relationships. 6-Bromo-3-(4-butylphenyl)-1,3-benzoxazine-2,4-(3H)-dione 3b proved to be the most active compound of the series.
引用
收藏
页码:264 / 267
页数:4
相关论文
共 13 条
  • [1] A note on the antitubercular activities of 1-aryl-5-benzylsulfanyltetrazoles
    Adamec, J
    Waisser, K
    Kunes, J
    Kaustová, J
    [J]. ARCHIV DER PHARMAZIE, 2005, 338 (08) : 385 - 389
  • [2] Matyk Josef, 2005, Farmaco (Lausanne), V60, P399, DOI 10.1016/j.farmac.2005.02.002
  • [3] Schachtner JE, 1999, PHARMAZIE, V54, P335
  • [4] A new pharmacophore of potential antimycobacterial activity: The disulfide group in the ring of alicyclic compounds
    Stachel, HD
    Odlerova, Z
    Waisser, K
    [J]. COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS, 1997, 62 (03) : 510 - 515
  • [5] New antimycobacterial 2,3-dihydro-1-alkylindole-2-thiones
    Waisser, K
    Heinisch, L
    Slosárek, M
    Janota, J
    [J]. FOLIA MICROBIOLOGICA, 2006, 51 (01) : 25 - 26
  • [6] QSAR study of antimycobacterial activity of quaternary ammonium salts of piperidinylethyl esters of alkoxysubstituted phenylcarbamic acids
    Waisser, K
    Dolezal, R
    Palát, K
    Cizmárik, J
    Kaustová, J
    [J]. FOLIA MICROBIOLOGICA, 2006, 51 (01) : 21 - 24
  • [7] New antimycobacterial S-alkyllsothiosemicarbazones
    Waisser, K
    Heinisch, L
    Slosárek, M
    Janota, J
    [J]. FOLIA MICROBIOLOGICA, 2005, 50 (06) : 479 - 481
  • [8] 1-Aryl-5-benzylsulfanyltetrazoles, a new group of antimycobacterial compounds against potentially pathogenic strains
    Waisser, K
    Adamec, J
    Dolezal, R
    Kaustová, J
    [J]. FOLIA MICROBIOLOGICA, 2005, 50 (03) : 195 - 197
  • [9] Waisser K, 2003, PHARMAZIE, V58, P83
  • [10] WAISSER K, 2003, FOLIA PHARM U CAROL, V29, P17