| Description | Tinidazole (CP12574)a is a 5-nitroimidazole derivative with the antiprotozoal property. Although the mechanism of action has not been fully elucidated, it has been suggested that tinidazole is metabolized and yields nitrite anions and metronidazole. Metronidazole's nitro group, in turn, is reduced via the parasite ferredoxin, thereby generating a series of free nitro radicals including nitro anions. Toxicity is achieved via depletion of sulfhydryl groups and DNA strand breaks with multiple hits having an additive effect and ultimately leading to cell death. |
| In vivo | Tinidazole对多种细菌均有抗菌作用,如：广泛的临床明显厌氧细菌（Bacteroides fragilis, Clostridium difficile等）,致病性原生动物（Tricbomonas vaginalis, Entamoeba bistolytica, Giardia duodenalis等）和微需氧的幽门螺杆菌。 Tinidazole对10种Prevotella bivia,11种Bacteroides fragilis和40种Clostridium difficile临床分离株有活性,Tinidazole和甲硝唑的平均MIC分别是： C. difficile,0.31 μg/mL和0.28 μg/mL;B. fragilis,0.5 μg/mL和0.71 μg/mL; P. bivia,2.33 μg/mL与1.52 μg/mL。在敏感细菌细胞和原生动物中,Tinidazole被还原为细胞毒性中间体,与DNA共价结合,导致细胞不可逆损伤。在低MLC时Tinidazole可杀死甲硝唑敏感株,但只对12甲硝唑耐药株中的4株有效。 Tinidazole对104 种T. vaginalis分离株均有抑制,平均MLC为1014.9 μM。Tinidazole影响滋养体对Giardia duodenalis的形态,可行性和依从性。 |
| Synonyms | 替硝唑, CP12574 |
| molecular weight | 247.27 |
| Molecular formula | C8H13N3O4S |
| CAS | 19387-91-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (242.65 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Narcisi EM, et al. Antimicrob Agents Chemother, 1996, 40(5), 1121-1125. 2. Fung HB, et al. Clin Ther, 2005, 27(12), 1859-1884. 3. Crowell AL, et al. Antimicrob Agents Chemother, 1996, 40(5), 1121-1125. 4. Meloni BP, et al. Trans R Soc Trop Med Hyg, 1990, 84(3), 375-379. |