Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-09-08
1996-11-26
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
548192, A61K 31425
Patent
active
055786219
ABSTRACT:
The present invention relates to a new compound of formula I ##STR1## with one of the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 representing OH, whereas the remaining symbols represent H; to a pharmaceutical composition containing the said compound, and to the use of said compound as anti-parasital, anti-bacterial, anti-fungal agent.
The Prior Art
Nitrothiazole compound PH 5776 (2-(acetolyloxy)-N-(5-nitro 2-thiazolyl) benzamide) is a compound of formula II ##STR2## in which R.sub.1 =O--COCH3 R.sub.2 =R.sub.3 =R.sub.4 =R.sub.5 =H
The preparation and uses of this compound are disclosed in U.S. Pat. No. 3,950,351, as well as in publication made by Applicant.
In U.S. Pat. No. 3,950,351, the compound of formula II is prepared by reacting ##STR3## This reaction is not suitable for the preparation of pure compound of formula I ##STR4## in which one of the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent OH, whereas the remaining symbols represent H.
Moreover, contrary to what could be expected from the prior art, i.e. that the presence of an acyloxy group was necessary for rendering the compound active and efficient against bacteria, parasites, . . . , it has now been found that the compound of formula I ##STR5## with one of the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 representing OH, whereas the remaining symbols represent H; had an excellent efficiency against parasites, bacteria, fungus although it does not contain an acyloxy group.
The compound of formula I had a substantially immediate action against parasite, fungus, bacteria.
REFERENCES:
patent: 3950351 (1976-04-01), Rossignol
R. Cavier et al., "Recherches sur les d eriv es nitr es d'int er et biologique", European Journal of Medicinal Chemistry, Chimica, Therapeutica, vol. 13 No. 6 1978 Paris Fr. pp. 539-543.
M. Dymicky et al., "Inhibition of Clostridium botulinum by 5-nitrothiazoles", Antimicrobial Aents and Chemotherapy, vol. 12, No. 3, Sep. 1977, pp. 353-356.
Dymicky, AntiMicrobial Agents and ChemoTherapy, 12(3) 353 (1977).
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