Antimycobacterial activity of 1-deaza-7,8-dihydropteridine derivatives against Mycobacterium tuberculosis and Mycobacterium avium complex in vitro.

Antimycobacterial activity of 1-deaza-7,8-dihydropteridine derivatives against Mycobacterium tuberculosis and Mycobacterium avium complex in vitro.
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DOI:
10.1093/jac/47.4.451
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发表时间:
2001-04
期刊:
The Journal of antimicrobial chemotherapy
影响因子:
--
通讯作者:
W. J. Suling;J. Maddry
W. J. Suling;J. Maddry
中科院分区:
其他
文献类型:
--
作者:
W. J. Suling;J. Maddry

文献摘要

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筛选了25种1-脱氮-7,8-二氢蝶啶衍生物对结核分枝杆菌菌株H37 Ra和三种鸟分枝杆菌临床分离株(血清型1、4或6)的抗分枝杆菌活性。用比色微量稀释肉汤测定法测定抗菌活性。17种化合物在>1.28至<或=12.8 mg/L范围内对一种或多种试验菌株的生长具有抑制作用。2位氨基氮上存在烷氧羰基并不是活性所必需的。活性取决于6-苯基环上基团取代的类型和位置,在某些情况下,取决于7-烷基的存在。
Twenty-five 1-deaza-7,8-dihydropteridine derivatives were screened for antimycobacterial activity against Mycobacterium tuberculosis strain H37Ra and three Mycobacterium avium clinical isolates (serovar 1, 4 or 6). Antibacterial activity was determined with a colorimetric microdilution broth assay. Seventeen of the compounds inhibited growth in the range >1.28 to <or=12.8 mg/L against one or more of the test strains. The presence of an alkoxycarbonyl group on the amino nitrogen at position 2 was not required for activity. Activity was dependent upon the type and location of group substitutions on the 6-phenyl ring and, in some cases, the presence of a 7-alkyl group.