Chemical Property of Benznidazole
Chemical Property:
- Melting Point:189-192 °C
- Refractive Index:1.643
- PKA:14?+-.0.46(Predicted)
- PSA：92.74000
- Density:1.35 g/cm3
- LogP:2.02180
- Storage Temp.:Sealed in dry,Room Temperature
- Solubility.:methanol: soluble50mg/mL, clear, colorless to yellow
- Water Solubility.:0.4g/L(temperature not stated)
- XLogP3:0.9
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:4
- Rotatable Bond Count:4
- Exact Mass:260.09094026
- Heavy Atom Count:19
- Complexity:325
- Purity/Quality:
-
99%, *data from raw suppliers
Benznidazole *data from reagent suppliers
Safty Information:
- Pictogram(s):
Xi
- Hazard Codes:Xi
- Statements:
36/37/38
- Safety Statements:
26-36
- MSDS Files:
-
SDS file from LookChem
Total 1 MSDS from other Authors
Useful:
- Drug Classes:Antiinfective Agents
- Canonical SMILES:C1=CC=C(C=C1)CNC(=O)CN2C=CN=C2[N+](=O)[O-]
- Recent ClinicalTrials:A Phase 1 Study of the Safety and Tolerability of ICM20 in Adults
- Recent EU Clinical Trials:Phase II trial for assessing different benznidazol regimens in the treatment of Chagas disease in adult patients on chronic phase . BERINECE project
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Description
Benznidazole is the second of the drugs approved for treatment of Chagas' disease. Like
nifurtimox, it is effective against the circulating form of Trypanosoma cruzi during the acute phase
of the disease, but also like nifurtimox, it is ineffective during the chronic stage of the disease. Benznidazole is an orally bioavailable antiprotozoal agent. It is a 2-nitroimidazole prodrug that becomes active when the nitro group is reduced within the parasite. It inhibits the growth of the parasites T. cruzi, T. vaginalis, G. lamblia, and E. histolytica (IC50s = 8.1, 18.62, 22.58, and 4.27 μM, respectively). It also inhibits clonogenic growth of human C33A cervical and KNS42 glioblastoma cancer cells under hypoxic, but not normoxic, conditions when used at a concentration of 100 μM. Benznidazole (100 mg/kg per day) decreases T. cruzi blood parasitemia to below detectable levels in a mouse model of chronic stable Chagas disease. Formulations containing benznidazole have been used in the treatment of Chagas disease caused by T. cruzi.
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Uses
N-Benzyl-2-nitro-1H-imidazole-1-acetamide (Benznidazole) may be used as reference drug for the extraction of guaianolide from the aerial parts of Tanacetum parthenium and to evaluate its in vitro antiprotozoal activity. Benznidazole (BNZ) is traditionally used to treat Chagas disease caused by Trypanosoma cruzi. The drugs used for the treatment of this disease, Nifurtimox and Benznidazole, are toxic and present sever
e side effects.
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Clinical Use
N-Benzyl-2-nitroimidazole-1-acetamide (Radanil, Rochagan)is a nitroimidazole derivative that is used for the treatment ofChagas disease. It is not available in the United States but isused extensively in South America. The effectiveness of benznidazoleis similar to that of nifurtimox. Therapy forAmerican trypanosomiasis with oral benznidazole requiresseveral weeks and is frequently accompanied by adverse effectssuch as peripheral neuropathy, bone marrow depression,and allergic-type reactions. Benznidazole is used in treatment of South American trypanosomiasis (Chagas disease).
