哒嗪氮氧化物。III. 基于三环茚并[2,1-c]哒嗪和苯并[f]噌啉体系的氮氧化物衍生物的合成及“体外”抗菌性能
Pyridazine N-oxides. III. Synthesis and "in vitro" antimicrobial properties of N-oxide derivatives based on tricyclic indeno[2,1-c]pyridazine and benzo[f]cinnoline systems.
作者信息
Gavini E, Juliano C, Mulè A, Pirisino G, Murineddu G, Pinna G A
机构信息
Dipartimento di Scienze del Farmaco, Università di Sassari, Italy.
出版信息
Arch Pharm (Weinheim). 2000 Oct;333(10):341-6. doi: 10.1002/1521-4184(200010)333:10<341::aid-ardp341>3.0.co;2-u.
A number of 9H-indeno[2,1-c]pyridazine N-oxides (3a-c) and benzo[f]cinnoline N-oxides (4,5a-c) have been synthesized and tested for antimicrobial activity. All new products were inactive against Gram negative bacteria and fungi. In contrast, among the compounds synthesized, 3b, 4b and 5b showed a moderate activity against Gram positive Staphylococcus aureus and Staphylococcus epidermidis. Of the present series, the 9-nitro-benzo[f]cinnoline N-oxide 5b possessed the highest activity especially against Trichomonas vaginalis (MIC = 3.9 micrograms/ml).
已合成了多种9H-茚并[2,1-c]哒嗪N-氧化物（3a - c）和苯并[f]噌啉N-氧化物（4,5a - c），并对其抗菌活性进行了测试。所有新产品对革兰氏阴性菌和真菌均无活性。相比之下，在合成的化合物中，3b、4b和5b对革兰氏阳性金黄色葡萄球菌和表皮葡萄球菌表现出中等活性。在本系列中，9-硝基-苯并[f]噌啉N-氧化物5b具有最高活性，尤其对阴道毛滴虫（最低抑菌浓度 = 3.9微克/毫升）。
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