Patent GB-692060-A (GB)
Title: Improvements in or relating to the preparation of antibacterial composition of matter
IPC: A61K31/63
Filed: 1951-02-12
Abstract: Thiosemicarbazones of chalcones, of general formula <FORM:0692060/IV (b)/1> where R=aryl, substituted or not; R1=alkyl, substituted or not; R11=hydrogen or alkyl, substituted or not; are prepared by the action of thiosemicarbazide upon a chalcone.  The thiosemicarbazone of benzalacetone is prepared by adding a saturated aqueous solution of thiosemicarbazide at 90 DEG  C. to a saturated solution of benzalacetone in alcohol at 60-70 DEG  C. and heating on a steam bath.  The thiosemicarbazones of salicylalacetone, 6-hydroxy-3-methyl benzalacetone and 4-acetamino-benzalacetone are prepared by similar methods.ALSO:A composition adapted for combating microorganisms of the genus Brucella comprises at least one active hydrophil component which is capable of substantially reducing the growth of Brucella in a hydrophilic medium and at least one active lipophil component which is capable of substantially reducing the growth of Brucella in a lipoidic medium.  Specified hydrophil components are: - antibiotics e.g. aureomycin, streptomycin, chloromycetin and patulin; sulpha compounds e.g. sulphadiazine and p-phenylsulphanilamide; 1,4-hydroquinone; a -naphthoquinone; and 3-methyl a -naphthoquinone. Typical lipophil components are the chloro-, bromo-, nitro- or acyl derivatives of 1,4-hydroquinone e.g. 2-bromo-, 2-chloro-, 2,5-dibromo-, 2,5-dichloroderivatives and quinacetophenone; the thiosemicarbazones of patulin; the semicarbazones of patulin; and the thiosemicarbazones of chalcones of general formula:- <FORM:0692060/VI/1> where R=aryl, substituted or not; R1=alkyl, substituted or not; R11=hydrogen or alkyl, substituted or not. Examples are the thiosemicarbazones of benzalacetone, 6-hydroxy-3-methylbenzal acetone, salicylalacetone, 4-acetamino benzalacetone and 3-nitrobenzalacetone.  Substances promoting the growth of lactobacillus e.g. galactose, lactose, glucose or stabilised lactobacilli may be added to the compositions, especially those in the form of vaginal pencils and suppositories. Examples are given of vaginal pencils containing 1,4-hydroquinone and 2-bromo-1,4-hydroquinone; lactose, galactose, glucose or stabilised lactobacilli; polymerised ethylene oxide; as such, or with the further addition of one or more of the following: thiosemicarbazone or semicarbazone of patulin, starch, paraffin wax, glycerin and gelatin.  An ointment has a base of petroleum jelly, liquid paraffin, lanolin, emulsifier and water.  Oral preparations consist of the active components and galactose, or lactose or a phosphate buffer. Pastils may have magnesium stearate as excipient.  The compositions may be administered to both man and animals by injection, orally, rectally or vaginally. Aqueous emulsions of vegetable or mineral oils may be used for general application to stables and the like.  The thiosemicarbazone of patulin is described in Specification 679,391, [Group IV (b)].  The thiosemicarbazones of chalcones of the above formula are prepared by the action of thiosemicarbazide upon a chalcone (see Group IV (b)).