10436-25-6Relevant articles and documents
Covalent inhibition of bacterial quorum sensing
Amara, Neri,Mashiach, Roi,Amar, Dotan,Krief, Pnina,Spieser, Stephane A. H.,Bottomley, Matthew J.,Aharoni, Amir,Meijler, Michael M.
, p. 10610 - 10619 (2009)
Chemical coordination of gene expression among bacteria as a function of population density is regulated by a mechanism known as 'quorum sensing' (QS). QS in Pseudomonas aeruginosa, an opportunistic pathogen that causes disease in immunocompromised patients, is mediated by binding of the transcriptional activator, LasR, to its ligand, 3-oxo-C12-HSL, leading to population-wide secretion of virulence factors and biofilm formation. We have targeted QS in P. aeruginosa with a set of electrophilic probes designed to covalently bind Cys79 in the LasR binding pocket, leading to specific inhibition of QS-regulated gene expression and concomitant reduction of virulence factor secretion and biofilm formation. This first example of covalent modification of a QS receptor provides a new tool to study molecular mechanisms of bacterial group behavior and could lead to new strategies for targeting bacterial virulence.
Reversible photo-responsive vesicle based on the complexation between an azobenzene containing molecule and α-cyclodextrin
Liu, Jianjia,Yan, Liang,Wang, Jie,Li, Tao,Zhao, Hanqing,Li, Li,Lincoln, Stephen F.,Prud'homme, Robert K.,Guo, Xuhong
, p. 32846 - 32852 (2015)
An amphiphilic molecule (Azo-Cl) was successfully synthesized and found to be able to construct reversible spherical vesicles in water. The assembled vesicles disappeared on the addition of equimolar α-cyclodextrin (α-CD) and reformed with UV irradiation
Polyanion inhibitors of human immunodeficiency virus and other viruses. 5. Telomerized anionic surfactants derived from amino acids
Leydet, Alain,Barragan, Véronique,Boyer, Bernard,Montéro, Jean Louis,Roque, Jean Pierre,Witvrouw, Myriam,Este, José,Snoeck, Robert,Andrei, Graciela,De Clercq, Erick
, p. 342 - 349 (1997)
ω-Acryloyl anionic surfactants, whose polar heads are derived from amino acids, have been telomerized to prepare polyanions of a predetermined molecular weight. The main goal of this study was to verify whether the antiviral activity is influenced by the degree of polymerization of the polyanions. The oligomeric polyanions were evaluated for their activity against human immunodeficiency virus (HIV-1 or HIV-2) and various other RNA and DNA viruses. With regard to their anti-HIV activity, a minimum number of anionic groups was necessary to achieve an inhibitory effect. Moreover, to be active the overall conformation of the polyanion must be such that the anionic groups are located on the external site of the molecule. With some of the polyanions, a 50% inhibition concentration (IC50) as low as 1 μg/mL, or even 0.1 μg/mL, was noted against HIV-1 in CEM-4 and MT-4 cells, respectively. The most potent polyanions also proved active against human cytomegalovirus and herpex simplex virus at concentrations of 5-10 and 20-40 μg/mL, respectively. No activity was observed against any of the other viruses tested (i.e., vesicular stomatitis, Sindbis, Semliki forest, parainfluenza, Junin, Tacaribe, Coxsackie, polio, reo, and vaccinia). No toxicity for the host cells was observed at concentrations up to 200 μg/mL.
The Synthesis of a Glucosyldiglyceride for Constructing pH-Sensitive Liposomes
Alshoaibi,Andryushina,Morozova,Serebrennikova
, p. 293 - 295 (2003)
A glucosyldiglyceride containing residues of 11-aminoundecanoic acid was synthesized for constructing pH-sensitive liposomes.
A Lewis acid-mediated protocol for the protection of aryl amines as their Boc-derivatives
Bartoli, Giuseppe,Bosco, Marcella,Locatelli, Manuela,Marcantoni, Enrico,Massaccesi, Massimo,Melchiorre, Paolo,Sambri, Letizia
, p. 1794 - 1798 (2004)
A new protocol of protection of poorly reactive aryl amines and functionalized amines with Boc2O in the presence of Zn(ClO 4)2·6H2O as the catalyst is reported. The catalytic action of Zn(ClO4)2·6H2O is specific for the activation of the pyrocarbonates, thus acid sensitive functionalities and stereochemical configurations of the starting materials remain unaltered in the protection process.
Helicity- and Molecular-Weight-Driven Self-Sorting and Assembly of Helical Polymers towards Two-Dimensional Smectic Architectures and Selectively Adhesive Gels
Li, Yan-Xiang,Xu, Lei,Kang, Shu-Ming,Zhou, Li,Liu, Na,Wu, Zong-Quan
, p. 7174 - 7179 (2021)
Self-sorting plays a crucial role in living systems such as the selective assembly of DNA and specific folding of proteins. However, the self-sorting of artificial helical polymers such as biomacromolecules has rarely been achieved. In this work, single-h
Discovery, synthesis of novel fusidic acid derivatives possessed amino-terminal groups at the 3-hydroxyl position with anticancer activity
Ni, Jingxuan,Guo, Mengqi,Cao, Yucheng,Lei, Lei,Liu, Kangli,Wang, Binghua,Lu, Fangfang,Zhai, Rong,Gao, Xiangwei,Yan, Chunhong,Wang, Hongbo,Bi, Yi
, p. 122 - 131 (2019)
A series of novel fusidic acid (FA) derivatives were synthesized and screened for their in vitro cytotoxicity against the Hela, U87, KBV and MKN45 cancer cell lines. Selected FA derivatives with anti-tumor activity were firstly identified including compound 4, which exhibited good anti-proliferative activity with IC50 values in the range of 1.26–3.57 μM. Further research revealed that compound 4 induced Hela cells to undergo apoptosis by increasing the ratio of the cells in the Sub-G0/G1 phase via decreasing the neo-synthesized proteins in a dose-dependent manner from 1 to 10 μM. Compound 4 also showed good in vivo anti-tumor activity against the xenograft tumor of Hela cells and had no apparent toxicity. This study highlights the advantage of introducing the medium-length amino-terminal groups at the 3-OH position of FA to enhance its anti-tumor activity and suggests that compound 4 provides a starting point for designing more potent derivatives in the future.
Synthesis and antibacterial evaluation of novel 3-substituted ocotillol-type derivatives as leads
Bi, Yi,Liu, Xian-Xuan,Zhang, Heng-Yuan,Yang, Xiao,Liu, Ze-Yun,Lu, Jing,Lewis, Peter John,Wang, Chong-Zhi,Xu, Jin-Yi,Meng, Qing-Guo,Ma, Cong,Yuan, Chun-Su
, (2017)
Due to the rapidly growing bacterial antibiotic-resistance and the scarcity of novel agents in development, bacterial infection is still a global problem. Therefore, new types of antibacterial agents, which are effective both alone and in combination with traditional antibiotics, are urgently needed. In this paper, a series of antibacterial ocotillol-type C-24 epimers modified from natural 20(S)-protopanaxadiol were synthesized and evaluated for their antibacterial activity. According to the screening results of Gram-positive bacteria (B. subtilis 168 and MRSA USA300) and Gram-negative bacteria (P. aer PAO1 and A. baum ATCC19606) in vitro, the derivatives exhibited good antibacterial activity, particularly against Gram-positive bacteria with an minimum inhibitory concentrations (MIC) value of 2-16 μg/mL. The subsequent synergistic antibacterial assay showed that derivatives 5c and 6c enhanced the susceptibility of B. subtilis 168 and MRSA USA300 to chloramphenicol (CHL) and kanamycin (KAN) (FICI 0.5). Our data showed that ocotillol-type derivatives with long-chain amino acid substituents at C-3 were good leads against antibiotic-resistant pathogens MRSA USA300, which could improve the ability of KAN and CHL to exhibit antibacterial activity at much lower concentrations with reduced toxicity.
Lipase sensing by naphthalene diimide based fluorescent organic nanoparticles: a solvent induced manifestation of self-assembly
Chakraborty, Debayan,Sarkar, Deblina,Ghosh, Anup Kumar,Das, Prasanta Kumar
, p. 2170 - 2180 (2021/03/14)
The precise control of supramolecular self-assembly is gaining utmost interest for the demanding applications of manifested nano-architecture across the scientific domain. This study delineates the morphological transformation of naphthalene diimide (NDI) derived amphiphiles with varying water content in dimethyl sulfoxide (DMSO) and the selective sensing of lipase using its aggregation-induced emission (AIE) properties. To this end, NDI-based, benzyl alcohol protected alkyl chain (C1, C5, and C10) linked amphiphilic molecules (NDI-1,2,3) were synthesized. Among the synthesized amphiphiles, benzyl ester linked C5 tailored naphthalene diimide (NDI-2) exhibited AIE with an emission maximum at 490 nm in a DMSO-water binary solvent system fromfw= 30% and above water content. The fibrous morphology ofNDI-2atfw= 30% got gradually transformed to spherical aggregated particles along with steady increment in the emission intensity upon increasing the amount of water in DMSO. Atfw= 99% water in DMSO, complete transformation to fluorescent organic nanoparticles (FONPs) was observed. Microscopic and spectroscopic techniques demonstrated the solvent driven morphological transformation and the AIE property ofNDI-2. Moreover, this AIE ofNDI-2FONPs was employed in the selective turn-off sensing of lipase against many other enzymes including esterase, through hydrolysis of a benzyl ester linkage with a limit of detection 10.0 ± 0.8 μg L?1. TheNDI-2FONP also exhibited its lipase sensing efficiencyin vitrousing a human serum sample.
ORGANIC COMPOSITIONS TO TREAT APOC3-RELATED DISEASES
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Paragraph 00708, (2016/02/26)
The present disclosure relates to compositions and methods for treating APOC3-related diseases such as: hypertriglyceridemia (e.g., Type V Hypertriglyceridemia), abnormal lipid metabolism, abnormal cholesterol metabolism, atherosclerosis, hyperlipidemia, diabetes, including Type 2 diabetes, obesity, cardiovascular disease, and coronary artery disease, among other disorders relating to abnormal metabolism or otherwise, using a therapeutically effective amount of a RNAi agent to APOC3.
