Dimetridazole

Dimetridazole（CAS 号 551-92-8）是硝基咪唑类广谱抗菌抗原生动物兽药，核心生物活性为抑制厌氧菌及原生动物（如阴道毛滴虫、阿米巴原虫）生长，还可通过靶向细菌群体感应（QS）系统（LasR、RhlR、PqsR 受体）及破坏细胞膜完整性、下调脂肪酸合成基因（fabA、fabD、fabG、cfa）发挥 antivirulence 作用，且能与头孢他啶（CAS号72558-82-8，货号： B3539）、多粘菌素 B （Polymyxin B，货号：C3090）等抗生素协同增强对多重耐药菌的抑制效果；无明确 IC50/EC50 数据，MIC 具有菌株特异性，对多重耐药大肠杆菌 NX400 的 MIC 为 256 μg/mL，与头孢他啶联用时（16 μg/mL DMZ + 64 μg/mL 头孢他啶）FICI=0.188，呈显著协同；常用应用浓度：体外抗菌测试 256 μg/mL（肉汤稀释法），铜绿假单胞菌 QS 抑制及毒力因子（绿脓素、生物膜）抑制为 50-200 μM，电化学检测浓度范围 0.1 nM-100 μM；动物实验中，Galleria mellonella 感染模型通过注射给药，小鼠急性肺感染模型采用 200 μM 鼻腔给药（每 12 小时一次）；临床作为兽药用于猪、家禽、蜜蜂的厌氧菌及原生动物感染，无明确人体治疗浓度，且多国禁止作为饲料添加剂，动物食品中残留需不可检出，其有效抗菌浓度需结合联用抗生素调整，协同场景下可显著降低抗生素使用浓度。

参考文献：

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[4] Wei X, Wang W, Arbab S, Wang Q, Bai Y, Zhang J. Dimetridazole potentiates cefotaxime against multidrug-resistant E. coli via membrane disruption and fatty acid composition. Sci Rep. 2025 Jul 1;15(1):21171. doi: 10.1038/s41598-025-07751-7. PMID: 40594620; PMCID: PMC12219633.