1254834-91-7
1254834-91-7 structure
- Name: Genz 669178
- Chemical Name: 5-(4-Cyano-2-methyl-1H-benzimidazol-1-yl)-N-cyclopropyl-2-thiophenecarboxamide
- CAS Number: 1254834-91-7
- Molecular Formula: C17H14N4OS
- Molecular Weight: 322.384
- Create Date: 2020-01-11 19:41:50
- Modify Date: 2023-01-14 21:44:13
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A potent PfDHODH inhibitor that exhibits low nanomolar in vitro potency against DHODH from P falciparum, P vivax, and P berghei; demonstrates in vitro potency against the 3D7 and Dd2 strains of P. falciparum, good tolerability and oral exposure in the mouse, and ED(50) values in the 4-day murine P. berghei efficacy model of 13-21 mg/kg/day with oral twice-daily dosing.
| Name | 5-(4-Cyano-2-methyl-1H-benzimidazol-1-yl)-N-cyclopropyl-2-thiophenecarboxamide |
|---|---|
| Synonyms |
5-(4-Cyano-2-methyl-1H-benzimidazol-1-yl)-N-cyclopropyl-2-thiophenecarboxamide
5-(4-Cyano-2-Methyl-1h-Benzimidazol-1-Yl)-N-Cyclopropylthiophene-2-Carboxamide 2-Thiophenecarboxamide, 5-(4-cyano-2-methyl-1H-benzimidazol-1-yl)-N-cyclopropyl- |
| Description | A potent PfDHODH inhibitor that exhibits low nanomolar in vitro potency against DHODH from P falciparum, P vivax, and P berghei; demonstrates in vitro potency against the 3D7 and Dd2 strains of P. falciparum, good tolerability and oral exposure in the mouse, and ED(50) values in the 4-day murine P. berghei efficacy model of 13-21 mg/kg/day with oral twice-daily dosing. |
|---|---|
| References | References 1. Lukens AK, e tal. Proc Natl Acad Sci U S A. 2014 Jan 14;111(2):799-804. 2. Booker ML, et al. J Biol Chem. 2010 Oct 22;285(43):33054-64. 3. Skerlj RT, et al. ACS Med Chem Lett. 2011 Jul 11;2(9):708-13. View Related Products by Target Bacterial |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Molecular Formula | C17H14N4OS |
| Molecular Weight | 322.384 |
| Exact Mass | 322.088837 |
| LogP | 2.17 |
| Index of Refraction | 1.766 |