Hof H, Eisenbarth B, Denzler A, Zak O, Schweizer E
J Antimicrob Chemother. 1985 Aug;16(2):205-10. doi: 10.1093/jac/16.2.205.
The antibacterial activities of niridazole (AmbilharR) and 12 other newly synthesized nitrothiazole derivatives were examined. Most of these compounds were active in vitro against Salmonella typhimurium (MICs 1-4 mg/l) and Bacteroides fragilis (MICs 0.015-0.03 mg/l). A therapeutic effect as determined by a reduction of bacterial counts per spleen of mice infected with Salm. typhimurium could only be achieved with those agents which displayed a similar side chain as niridazole, i.e. an imidazolidinone ring. Other nitrothiazole derivatives with a cleaved imidazolidinone ring as the side chain, although active in vitro, could not exert a reduction of bacterial counts in vivo. Similar results were obtained in mice infected with Bact. fragilis. Whereas niridazole and another nitrothiazole derivative with an imidazolidinone ring in the side chain were able to reduce the bacterial counts in a subcutaneous abscess, the derivative with a laminar side chain was inactive in vivo, although highly active in vitro.
对硝唑咪（安比哈R）和其他12种新合成的硝基噻唑衍生物的抗菌活性进行了检测。这些化合物大多在体外对鼠伤寒沙门氏菌（最低抑菌浓度为1 - 4毫克/升）和脆弱拟杆菌（最低抑菌浓度为0.015 - 0.03毫克/升）具有活性。对于感染鼠伤寒沙门氏菌的小鼠，只有那些具有与硝唑咪相似侧链（即咪唑烷酮环）的药物才能通过减少脾脏细菌计数来确定其治疗效果。其他以断裂的咪唑烷酮环为侧链的硝基噻唑衍生物，尽管在体外有活性，但在体内不能减少细菌计数。在感染脆弱拟杆菌的小鼠中也得到了类似的结果。硝唑咪和另一种侧链带有咪唑烷酮环的硝基噻唑衍生物能够减少皮下脓肿中的细菌计数，而带有层状侧链的衍生物尽管在体外活性很高，但在体内无活性。
