Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal
Patent
1975-04-07
1976-12-28
Gotts, Lewis
Chemistry of carbon compounds
Miscellaneous organic carbon compounds
C-metal
424177, C07C10352, A61K 3700
Patent
active
040001229
ABSTRACT:
.alpha.-Hydrazinocarboxamide and .alpha.-(.alpha.'-acylhydrazino)-carboxamide derivatives of formula I ##STR1## in which R.sup.1 and R.sup.2 each are lower alkyl or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are joined form a piperidino or morpholino radical; R.sup.3 is hydrogen, lower alkanoyl, benzoyl, p-nitrobenzoyl, p-aminobenzoyl, p-chlorobenzoyl, isocyanoacetyl, or protected amino acyl radicals, for example, N-formylglycyl or ##STR2## (N-carbobenzoxyglycylglycyl); R.sup.4 is lower alkyl, CHR.sup.7 COOR.sup.8 or CH.sub.2 CH.sub.2 COOR.sup.8 wherein R.sup.7 is hydrogen or phenyl and R.sup.8 is hydrogen or lower alkyl; R.sup.5 is hydrogen or lower alkyl; or R.sup.4 and R.sup.5 together with the carbon atom to which they are joined form a cyclohexylidene radical; and R.sup.6 is a cyclohexyl or CHR.sup.9 COY wherein R.sup.9 is hydrogen or benzyl and Y is hydroxyl, lower alkoxy or amine, with the provisos that when Y is hydroxyl then R.sup.8 is hydrogen, that when Y is lower alkoxy than R.sup.8 is lower alkyl and that when Y is amino R.sup.4 is lower alkyl, are disclosed herein along with the related .alpha.-hydrazino-carboxamide and .alpha.-(.alpha.'-acylhydrazino)carboxamide compounds of formula III ##STR3## in which R.sup.1, R.sup.2, R.sup.3 , R.sup.5 and R.sup.7 are as defind above and Y is lower alkoxy. These compounds possess antibacterial activity. Methods for their preparation and use are disclosed also.
REFERENCES:
patent: 3888840 (1975-06-01), Failli et al.
I. Ugi, "Newer Methods of Preparative Organic Chemistry", vol. IV, W. Foerst, ed., Academic Press, N.Y. (1968), p. 30.
Gokel et al., "Isonitrile Chemistry", I. Ugi, ed., Academic Press, N.Y. (1971), pp. 159-61.
Failli Amedeo
Gotz Manfred K.
Immer Hans U.
Nelson Verner R.
American Home Products Corporation
Gotts Lewis
Suyat Reginald J.
Venetianer Stephen
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