Antischistosomal and some toxicological properties of a nitrodiphenylaminoisothiocyanate (C 9333-Go/CGP 4540)

Bueding, Ernest; Batzinger, Robert P.; Petterson, G.

doi:10.1007/bf01990188

Cited by 47 publications

(14 citation statements)

References 12 publications

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“…This antischistosomal compound is not mutagenic in vitro to Ames tester strain TAtOO even in the presence of microsomal preparations, but mutagenesis occurs with the tester strain in the mouse peritoneum (69). Metabolic activity by the flora may explain this observation since mutagenic activity in mouse urine after feeding 4-isothiocyanat0-4'-nitrodiphenyla mine is markedly decreased by prior treatment with succinylsulfathiazole.…”

Section: The Further Study Of This Problemmentioning

confidence: 92%

Biochemical Pharmacology of the Intestinal Flora

Goldman¹

1978

Annu. Rev. Pharmacol. Toxicol.

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Animal and bacteriological techniques have been developed for clarifying the role of the flora in the metabolism of drugs and other exogenous compounds. In general the flora tends to catalyze reductive and hydrolytic reactions, some of which reverse the detoxification reactions normally occurring in the liver. These reactions and others have been implicated in the pharamacological or toxicological action of exogenous compounds. Only in a few instances, however, have practical consequences of these reactions been documented. The major challenge at present is to develop methods capable of further defining the implications of reactions due to the flora.

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Section: The Further Study Of This Problemmentioning

confidence: 92%

Biochemical Pharmacology of the Intestinal Flora

Goldman¹

1978

Annu. Rev. Pharmacol. Toxicol.

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“…Treatment of mice infected with Schistosoma mansoni with CS-A was at least additive to the effects of subcurative doses of amoscanate, a new potent antischistosomal drug [11,12] (Table 2). Therefore, it appears that the actions of the two compounds on the parasites are synergistic with each other.…”

Section: Methodsmentioning

confidence: 99%

Antischistosomal effects of cyclosporin A

Bueding

Hawkins

1981

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Administration of cyclosporin A, a new selective immunosuppressive agent, to mice infected with Schistosoma mansoni resulted in a significant reduction in the number of mature and immature male and, to a greater extent, female worms. With lower, subeffective, doses a reduction in hemoglobinase activity and protein content of female schistosomes is produced. Evidence available so far suggests that the antischistosomal effects of cyclosporin A are mediated through a stimulation of host mechanisms directed against the parasite.

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“…In 1976, Striebel described the use of amoscanate (4-isothiocyanato-4'-nitrodiphenylamine) against helminthic diseases. At that time its wide activity range was confirmed, as it was used against most Schistosoma species, filariae and gastrointestinal nematodes (Bueding et al, 1976). Amoscanate was tested in humans infected with S. japonicum, and the cure rates were as high as 92%.…”

Section: Chemotherapy Against Schistosomiasismentioning

confidence: 96%