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Antitrypanosomal agent 1

Names

[ CAS No. ]:
75144-12-6

[ Name ]:
Antitrypanosomal agent 1

[Synonym ]:
1-(3,4-Dichlorophenyl)-3-dimethylamino-1-propanone HCl
AmbscPOD_38/0850
1-(3,4-dichlorophenyl)-3-dimethylamino-1-propanone hydrochloride

Biological Activity

[Description]:

Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor with an IC50 of 3.3 μM. Antitrypanosomal agent 1 inhibits glutathione reductase (GR) (IC50=64.8 μM) and T. brucei (EC50=1 μM). Antitrypanosomal agent 1 has anti-trypanosomal activity[1].

[Related Catalog]:

Research Areas >> Infection

[Target]

IC50: 3.3 μM (trypanothione reductase) and 64.8 μM (glutathione reductase)[1] EC50: 1 μM (T. brucei)[1]


[In Vitro]

Antitrypanosomal agent 1 (compound 8a) has an selectivity for TR (GR IC50/TR IC50) of 20[1].

[References]

[1]. Martyn DC, et al. High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1280-3.

Chemical & Physical Properties

[ Density]:
1.22g/cm3

[ Boiling Point ]:
341.9ºC at 760 mmHg

[ Molecular Formula ]:
C11H14Cl3NO

[ Molecular Weight ]:
282.59400

[ Flash Point ]:
160.6ºC

[ Exact Mass ]:
281.01400

[ PSA ]:
20.31000

[ LogP ]:
3.92980

[ Index of Refraction ]:
1.544

[ Storage condition ]:
2-8℃

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Related Compounds