571. Amocarzine

Nomenclature

CAS number: 36590-19-9
4-Methyl-N-[4-[(4-nitrophenyl)amino]phenyl]-1-piperazinecarbothioamide; 4-nitro-4′-[(N-methylpiperazinyl)thiocarbonylamino]diphenylamine; CGP-6140.
C18H21N5O2S; mol wt 371.46.
C 58.20%, H 5.70%, N 18.85%, O 8.61%, S 8.63%.

Description and references

Orally active macrofilaricide; derivative of amoscanate, q.v. Prepn: BE 772053 (1971 to Agripat); R. Spaun et al., US 3781290 (1973 to Ciba-Geigy). Mechanism of action study: K. P. Davies et al., Exp. Parasitol. 68, 382 (1989). HPLC determn in biological fluids: S. C. Bhatia et al., J. Chromatogr. 434, 288 (1988). Pharmacokinetics: J. B. Lecaillon et al., Br. J. Clin. Pharmacol. 30, 625, 629 (1990). Clinical trial in onchocerciasis: A. A. Poltera et al., Lancet 337, 583 (1991).

Chemical structure

Properties

mp 191-196°. Sol in acetonitrile.

Therapeutic Category

Anthelmintic (Nematodes).

Keywords

Anthelmintic (Nematodes)