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抗分枝杆菌物质的化学结构与其对非典型菌株活性之间的关系。第14部分：3-芳基-6,8-二卤代-2H-1,3-苯并恶嗪-2,4(3H)-二酮

Relationships between the chemical structure of antimycobacterial substances and their activity against atypical strains. Part 14: 3-Aryl-6,8-dihalogeno-2H-1,3-benzoxazine-2,4(3H)-diones.

作者信息

Waisser K, Hladuvková J, Gregor J, Rada T, Kubicová L, Klimesová V, Kaustová J

机构信息

Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Hradec Králové, Czech Republic.

出版信息

Arch Pharm (Weinheim). 1998 Jan;331(1):3-6. doi: 10.1002/(sici)1521-4184(199801)331:1<3::aid-ardp3>3.0.co;2-2.

DOI:10.1002/(sici)1521-4184(199801)331:1<3::aid-ardp3>3.0.co;2-2
PMID:9507695
Abstract

A set of eight derivatives of 6,8-dichloro-3-phenyl-2H-benzoxazine-2,4(3H)-dione and nine derivatives of 6,8-dibromo-3-phenyl-2H-1, 3-benzoxazine-2,4(3H)-dione, substituted on the phenyl ring, was prepared by the reaction of the corresponding salicylanilides with ethyl chloroformate. The compounds were evaluated in vitro for antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii, and Mycobacterium avium. Their activity increases with increasing hydrophobicity and electron-withdrawing ability of the substituents on the phenyl ring.

摘要

通过相应的水杨酰苯胺与氯甲酸乙酯反应，制备了一组在苯环上取代的8种6,8 - 二氯 - 3 - 苯基 - 2H - 苯并恶嗪 - 2,4(3H) - 二酮衍生物和9种6,8 - 二溴 - 3 - 苯基 - 2H - 1,3 - 苯并恶嗪 - 2,4(3H) - 二酮衍生物。对这些化合物进行了体外抗结核分枝杆菌、堪萨斯分枝杆菌和鸟分枝杆菌的抗分枝杆菌活性评估。它们的活性随着苯环上取代基疏水性和吸电子能力的增加而增强。

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