69982-57-6Relevant academic research and scientific papers
Synthesis and Bioactivities of New Membrane-Active Agents with Aromatic Linker: High Selectivity and Broad-Spectrum Antibacterial Activity
Chu, Wenchao,Yang, Yi,Cai, Jianfeng,Kong, Hongtao,Bai, Mengmeng,Fu, Xiangjing,Qin, Shangshang,Zhang, En
, p. 1535 - 1545 (2019)
The worldwide emergence of microbial resistance to antibiotics constitutes an important and growing public health threat, and novel antibiotics are urgently needed. In this report, a series of symmetrical membrane-active agents linked by an aromatic nucle
Host-guest inclusion for enhancing anticancer activity of pemetrexed against lung carcinoma and decreasing cytotoxicity to normal cells
Chen, Junyi,Zhang, Yahan,Zhang, Yadan,Zhao, Liang,Chen, Longming,Chai, Yao,Meng, Zhao,Jia, Xueshun,Meng, Qingbin,Li, Chunju
, p. 3034 - 3038 (2021)
Advanced chemotherapy strategies are in urgent demand for improving anticancer efficacy. Herein, a water-soluble pillar[6]arene (WP6A) was used to load chemotherapeutic agent pemetrexed (PMX) by forming direct host-guest inclusion, which is beneficial for
Phosphonium pillar[5]arenes as a new class of efficient biofilm inhibitors: Importance of charge cooperativity and the pillar platform
Joseph, Roymon,Kaizerman, Dana,Herzog, Ido M.,Hadar, Maya,Feldman, Mark,Fridman, Micha,Cohen, Yoram
, p. 10656 - 10659 (2016)
Biofilm formation, which frequently occurs in microbial infections and often reduces the efficacy of antibiotics, also perturbs many industrial and domestic processes. We found that a new class of water soluble pillar[5]arenes bearing phosphonium moieties
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).
CLASS OF BIFUNCTIONAL COMPOUNDS WITH QUATERNARY AMMONIUM SALT STRUCTURE
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Paragraph 0305, (2019/11/11)
The invention provides a class of compounds represented by formula (I), having bifunctional active quaternary ammonium salt structure of a β2-adrenoreceptor agonist and an M receptor antagonist, a pharmaceutically acceptable salt, solvate, and optical isomer thereof. A pharmaceutical composition comprising such a compound with quaternary ammonium salt structure, a method for preparing such a compound with quaternary ammonium salt structure and an intermediate thereof, and uses thereof in treating pulmonary disorders are also provided. The compounds of the invention have high selectivity to the M receptor subtype, and have less adverse reaction and lower toxic and side effects in the treatment of pulmonary diseases such as COPD and asthma.
Aromatic phenol quaternary ammonium salt antibacterial peptide simulant with antibacterial activity and preparation method thereof
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Paragraph 0064; 0065, (2018/10/19)
The invention belongs to the technical field of medicine chemistry, and discloses an aromatic phenol antibacterial peptide simulant with anti-drug resistance activity and no obvious toxicity and a preparation method thereof. The target product is obtained
Amide aromatic phenol antibacterial peptide analogue with antibacterial activity and preparation method thereof
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Paragraph 0076, (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.
TRIAZOLIUM AND IMIDAZOLIUM SALTS AND USES THEREOF
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Page/Page column 32, (2011/10/31)
The present disclosure relates to certain new and known triazolium and/or imidazolium salts and to their therapeutic use, for example in methods of treating or preventing an infection by a Plasmodium or Babesia parasite in a subject in need thereof. The triazolium and imidazolium salts are compounds of the Formula (I) or (II): wherein R1-R4, R1′-R3′, R8-R11, X, X′, X″, Y, Y′ and Y″ are as defined in the disclosure.
The anti-malarial activity of bivalent imidazolium salts
Vlahakis, Jason Z.,Mitu, Simona,Roman, Gheorghe,Rodriguez, E. Patricia,Crandall, Ian E.,Szarek, Walter A.
experimental part, p. 6525 - 6542 (2011/12/02)
A series of compounds containing bivalent imidazolium rings and one triazolium analog were synthesized and evaluated for their ability to inhibit the replication of Plasmodium falciparum cultures. The activity and selectivity of the compounds for P. falciparum cultures were found to depend on the presence of electron-deficient rings that were spaced an appropriate distance apart. The activity of the compounds was not critically dependent on the nature of the linker between the electron-deficient rings, an observation that suggests that the rings were responsible for the primary interaction with the molecular target of the compounds in the parasite. The bivalent imidazolium and triazolium compounds disrupted the process whereby merozoites gain entry into erythrocytes, however, they did not appear to prevent merozoites from forming. The compounds were also found to be active in a murine Plasmodium berghei infection, a result consistent with the compounds specifically interacting with a parasite component that is required for replication and is conserved between two Plasmodium species.
Synthesis of some novel tetraimidazolium salts derived from diphenyl- and dimethylglycolurils
Rahimizadeh, Mohammad,Seresht, Esmaeel Rezaei,Golari, Neda,Bakavoli, Mehdi
experimental part, p. 639 - 645 (2009/07/25)
Several new tetrabromo compounds based on diphenyl- and dimethylglycolurils were synthesized. Sequential treatment of these compounds with imidazole, methyl iodide, and sodium tetrafluoroborate gave their corresponding tetra imidazolium salts. Some of the
