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硝基噻唑衍生物的抗菌活性。

Antibacterial activities of nitrothiazole derivatives.

作者信息

Hof H, Zak O, Schweizer E, Denzler A

出版信息

J Antimicrob Chemother. 1984 Jul;14(1):31-9. doi: 10.1093/jac/14.1.31.

Abstract

A new group of chemical agents with pronounced antibacterial activities is presented. Different nitrothiazole derivatives, but not all, exhibit antibacterial activities similar to that of niridazole (AmbilharR), a nitrothiazolyl-imidazolidinone. Certain aerobic bacteria are moderately susceptible to these agents. The efficacy of these agents is almost comparable to that of ampicillin and tetracyline. It is much better than the efficacy of nitrofuran derivatives, the nitroimidazole derivatives being inactive. The mode of action of the nitrothiazole derivatives is bactericidal. Against anaerobic bacteria the nitrothiazole derivatives are unique, since the extremely low MIC's are not approached by any other of the nitro-compounds nor by any other of the common antibiotics tested, such as clindamycin, ampicillin and tetracycline. It is suggested that the nitrogroup of the nitrothiazole ring moiety represents the chemical structure responsible for their excellent antibacterial activities.

摘要

本文介绍了一类具有显著抗菌活性的新型化学药剂。不同的硝基噻唑衍生物,但并非全部,都表现出与硝噻唑咪唑烷酮(硝咪唑,AmbilharR)相似的抗菌活性。某些需氧菌对这些药剂中度敏感。这些药剂的疗效几乎与氨苄青霉素和四环素相当。它比硝基呋喃衍生物的疗效好得多,而硝基咪唑衍生物则无活性。硝基噻唑衍生物的作用方式是杀菌的。对于厌氧菌,硝基噻唑衍生物是独特的,因为其他任何硝基化合物以及所测试的任何其他常用抗生素(如克林霉素、氨苄青霉素和四环素)都无法达到其极低的最低抑菌浓度(MIC)。有人认为,硝基噻唑环部分的硝基代表了赋予其优异抗菌活性的化学结构。

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