Genz 669178

Names

[ Name ]:
Genz 669178

[Synonym ]:
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-

Biological Activity

[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

Chemical & Physical Properties

[ 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

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.