5335-05-7Relevant articles and documents
Evaluation of the antibacterial efficacy of diesters of azelaic acid
Charnock, Colin,Brudeli, Bjarne,Klaveness, Jo
, p. 589 - 596 (2004)
A number of diesters of the topical dermatosis treatment azelaic (nonanedioic) acid were prepared and tested for antibacterial effect. Two esters, bis-[(hexanoyloxy)methyl] nonanedioate and especially bis-[(butanoyloxy)methyl] nonanedioate showed promising activity against acne related bacteria in vitro. No activity of azelaic acid was detected in Mueller Hinton II agar at pH 7.3 when using the agar diffusion method, whereas both esters gave zones of growth inhibition. At pH 5.6, activity of azelaic acid was detected. At this pH, the zones of inhibition and MIC values obtained with azelaic acid were smaller than those of bis-[(butanoyloxy)methyl] nonanedioate for all test organisms. A preparation for topical use containing 20% (w/w) bis-[(butanoyloxy)methyl] nonanedioate, and the commercially available Skinoren (20% (w/w) azelaic acid), were compared for antibacterial effect against cutaneous bacteria using contact plate analyses of the skin. Though Skinoren was usually most effective, the differences were not statistically significant. Furthermore, bacteria surviving contact with the topical preparations were invariably more sensitive to the ester than to azelaic acid upon subculturing onto agar (pH 5.6) containing either preparation at 0.2-0.7mg/ml. This might indicate that other factors, such as the composition of the cream base, mitigate the antibacterial activity of the ester. It is proposed that the pharmacological and microbiological properties of bis-[(butanoyloxy)methyl] nonanedioate are worthy of further study based on an extended screening of acne sufferers.
Amoxicillin derivative as well as preparation method and application thereof
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Paragraph 0020; 0049-0050, (2020/08/02)
The invention provides an amoxicillin derivative with a structure shown as a formula I or a pharmaceutically and/or veterinary acceptable solvate of the amoxicillin derivative, wherein R is a hydrogenatom, an alkyl group, an amino group, a hydroxyl group, an amidino group, a guanidino group, a nitro group, a sulfonyl group or a group containing one of the alkyl group, the amino group, the hydroxyl group, the amidino group, the guanidino group, the nitro group and the sulfonyl group. According to the invention, two different lead compounds are connected together through a covalent bond to generate a synergistic effect, an addition effect or new pharmacological activity in vivo; benzoic acid is spliced to an amoxicillin side chain to generate a new amoxicillin-benzoic acid derivative, and the obtained new compound can broaden the antibacterial spectrum, has good antibacterial activity on gram-positive bacteria and gram-negative bacteria, and is effective for drug-resistant bacteria.
SULFONAMIDE DERIVATIVE AND MEDICINAL USE THEREOF
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Paragraph 1522-1523, (2015/02/25)
Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent α4 integrin-inhibitory action.
