Naphthoquinone derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ketone doai

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514895, 552298, 552299, A01N 3500, C07C 5038

Patent

active

050534327

ABSTRACT:
Novel antiprotozoal naphthoquinones having the general formula ##STR1## (wherein either R.sup.1 is hydrogen and R.sup.2 is selected from C.sub.1-6 alkoxy, aralkoxy, C.sub.1-6 alkyl-C.sub.1-6 alkoxy, phenyl substituted by one or two groups selected from halogen and C.sub.1-6 alkyl, halogen and perhalo-C.sub.1-6 alkyl; or R.sup.1 and R.sup.2 are both C.sub.1-6 alkyl or phenyl; and n is 0 or 1) and salt thereof. The compounds of formula (I) are useful for the treatment or prophylaxis of protozoal diseases including malaria, theileriosis and coccidiosis. Various processes for preparing compounds of formula (I) are described.

REFERENCES:
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patent: 3206358 (1965-09-01), Stevenson
patent: 3347742 (1967-10-01), Rogers et al.
patent: 3367830 (1968-02-01), Sarett
patent: 3682991 (1972-08-01), Tullar et al.
patent: 4031220 (1977-06-01), Richards
patent: 4195089 (1980-03-01), Richards
patent: 4485116 (1984-11-01), Hudson et al.
patent: 4485117 (1984-11-01), Hudson et al.
Fieser, et al., Journal of Medicinal Chemistry, vol. 10, No. 1, Jun. 26, 1967, Naphthoquinone Antimalarials. XXIX, 2-Hydroxy-3-(w-cyclohexylalkyl)-1,4-naphthoquinones, pp. 513-517.
Fieser, et al., vol. 70, pp. 3158-3164, Naphthoquinone Antimalarials. II. Correlation of Structure and Activity Against P. lophurae in Ducks.sup.1.

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