Highly active antimycobacterial derivatives of benzoxazine

被引：40

作者：

Petrlikova, Eva ^{[1
]}

Waisser, Karel ^{[1
]}

Divisova, Hana ^{[1
]}

Husakova, Petra ^{[1
]}

Vrabcova, Petra ^{[2
]}

Kunes, Jiri ^{[1
]}

Kolar, Karel ^{[2
]}

Stolarikova, Jirina ^{[3
]}

机构：

[1] Charles Univ Prague, Dept Inorgan & Organ Chem, Fac Pharm Hradec Kralove, Hradec Kralove 50005, Czech Republic

[2] Univ Hradec Kralove, Dept Chem, Hradec Kralove 50003, Czech Republic

[3] Reg Inst Publ Hlth, Ostrava, Czech Republic

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 23期

关键词：

Benzoxazine; Thioxo group; Antimycobacterial activity; Tuberculosis; EFFICIENT SYNTHESIS; INHIBITORS; SYSTEMS;

D O I：

10.1016/j.bmc.2010.10.017

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

New 3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones and 3-(4-alkylphenyl)-2H-1,3-benzoxazine-2,4(3H)-dithiones were synthesized. The compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium avium and two strains of Mycobacterium kansasii. The antimycobacterial activity increased with the replacement of the carbonyl group by the thiocarbonyl group in the starting 3-(4-alkylphenyl)-2H-1,3-benzoxazine-2,4(3H)-diones. The most active derivatives were more active than isonicotinhydrazide (INH). Free-Wilson analysis was also carried out and the activity contribution was examined. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：8178 / 8187

页数：10

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