5463-16-1Relevant articles and documents
Low-toxicity amphiphilic molecules linked by an aromatic nucleus show broad-spectrum antibacterial activity and low drug resistance
Chu, Wenchao,Yang, Yi,Qin, Shangshang,Cai, Jianfeng,Bai, Mengmeng,Kong, Hongtao,Zhang, En
supporting information, p. 4307 - 4310 (2019/04/17)
Amphiphilic molecules linked by an aromatic nucleus were developed that showed high selectivity toward bacteria over mammalian cells, and low drug resistance. A promising compound 4g exhibited strong bactericidal activity against a panel of sensitive and resistant bacteria, low toxicity, the ability to reduce cell viability in biofilms, stability in mammalian fluids, rapid killing of pathogens, and high in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA).
Amide aromatic phenol antibacterial peptide analogue with antibacterial activity and preparation method thereof
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Paragraph 0085; 0086; 0092, (2018/12/03)
The invention belongs to the technical field of pharmaceutical chemistry, and discloses an amide aromatic phenol antibacterial peptide analogue with drug-resistance bacteria resistant activity and without obvious toxicity and a preparation method thereof. The target product is obtained by 3-4 reaction steps, and the main structure of the product is shown as follows. In-vitro antibacterial activityexperiments prove that most of the series of compounds have excellent activity on Gram-positive staphylococcus aureus and enterococcus faecalis, Gram-negative Escherichia coli and stenotrophomonas maltophilia, and the compounds have excellent broad spectrum antibacterial activity; moreover, in-vitro red cell hemolytic data is low in toxicity and has excellent selectivity. One part of the compounds also have excellent antibacterial activity on 'superbacteria' comprising drug-resistant methicillin staphylococcus aureus (MRSA), clinical strains producing enzymes NDM-1 and KPC-2 and the like. Therefore, the series of compounds are expected to serve as novel antibacterial candidate drugs.
Cyclic diamine compounds and medicine containing the same
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, (2008/06/13)
The present invention offers novel cyclic diamine compounds and a pharmaceutical composition containing the same. The present invention relates to a compound represented by the formula (I) or salt(s) or solvate(s) thereof. (In the formula, is an optionally substituted divalent residue of benzene, pyridine, cyclohexane or naphthalene or is a vinylene group where Ar is an optionally substituted aryl group;X is —NH—, oxygen atom or sulfur atom;Y is —NR1—, oxygen atom, sulfur atom, sulfoxide or sulfone;Z is a single bond or —NR2—;R1 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group;R2 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group;l is an integer of from 0 to 15;m is an integer of 2 or 3; andn is an integer of from 0 to 3). The compound of the present invention is useful as a pharmaceutical composition, particuarly as an inhibitor of acyl coenzyme A cholesterol acyltransferase (ACAT).
Novel cyclic diamine compounds and medicine containing the same
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, (2008/06/13)
The present invention offers novel cyclic diamine compounds and a pharmaceutical composition containing the same. The present invention relates to a compound represented by the formula (I) or salt(s) or solvate(s) thereof. (In the formula, is an optionally substituted divalent residue of benzene, pyridine, cyclohexane or naphthalene or is a vinylene group where Ar is an optionally substituted aryl group; X is —NH—, oxygen atom or sulfur atom; Y is —NR1—, oxygen atom, sulfur atom, sulfoxide or sulfone; Z is a single bond or —NR2—; R1 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group; R2 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group; l is an integer of from 0 to 15; m is an integer of 2 or 3; and n is an integer of from 0 to 3). The compound of the present invention is useful as a pharmaceutical composition, particuarly as an inhibitor of acyl coenzyme A cholesterol acyltransferase (ACAT).
NOVEL CYCLIC DIAMINE COMPOUNDS AND MEDICINE CONTAINING THE SAME
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, (2008/06/13)
The present invention offers novel cyclic diamine compounds and a pharmaceutical composition containing the same. The present invention relates to a compound represented by the formula (I) or salt(s) or solvate(s) thereof. (In the formula, is an optionally substituted divalent residue of benzene, pyridine, cyclohexane or naphthalene or is a vinylene group whereAr is an optionally substituted aryl group;X is -NH-, oxygen atom or sulfur atom;Y is -NR1-, oxygen atom, sulfur atom, sulfoxide or sulfone;Z is a single bond or -NR2-;R1 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group;R2 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group;l is an integer of from 0 to 15;m is an integer of 2 or 3; andn is an integer of from 0 to 3).The compound of the present invention is useful as a pharmaceutical composition, particuarly as an inhibitor of acyl coenzyme A cholesterol acyltransferase (ACAT).