324035-44-1Relevant academic research and scientific papers
Activation of Cell-Penetrating Peptides with Ionpair-π Interactions and Fluorophiles
Chuard, Nicolas,Fujisawa, Kaori,Morelli, Paola,Saarbach, Jacques,Winssinger, Nicolas,Metrangolo, Pierangelo,Resnati, Giuseppe,Sakai, Naomi,Matile, Stefan
, p. 11264 - 11271 (2016)
In this report, we elaborate on two new concepts to activate arginine-rich cell-penetrating peptides (CPPs). Early on, we have argued that repulsion-driven ion-pairing interactions with anionic lipids account for their ability to move across hydrophobic c
An unanticipated discovery towards novel naphthalimide corbelled aminothiazoximes as potential anti-MRSA agents and allosteric modulators for PBP2a
Zhang, Peng-Li,Gopala, Lavanya,Zhang, Shao-Lin,Cai, Gui-Xin,Zhou, Cheng-He
supporting information, (2021/12/20)
Available therapeutic strategies are urgently needed to conquer multidrug resistance of MRSA. A visible effort was guided towards the advancement of novel antibacterial framework of naphthalimide corbelled aminothiazoximes, and desired to assert some insight on the conjunction of individual pharmacophore with distinct biological activities and unique action mechanism. Preliminary assessment displayed that dimethylenediamine derivative 13d presented a wonderful inhibition on MRSA (MIC = 0.5 μg/mL), and showed excellent membrane selectivity (HC50 > 200 μg/mL) from an electrostatic distinction of the electronegative bacterial membranes and the electroneutral mammalian membranes. Moreover, 13d could effectually relieve the development of MRSA resistance. Investigations into explaining the mechanism of anti-MRSA disclosed that 13d displayed strong lipase affinity, which facilitated its permeation into cell membrane, causing membrane depolarization, leakage of cytoplasmic contents and lactate dehydrogenase (LDH) inhibition. Meanwhile, 13d could exert interaction with DNA to hinder biological function of DNA, and disrupt the antioxidant defense system of MRSA through up-regulation of ROS subjected the strain to oxidative stress. In particular, the unanticipated mechanism for naphthalimide corbelled aminothiazoximes that 13d could suppress the expression of PBP2a by inducing allosteric modulation of PBP2a and triggering the open of the active site, was discovered for the first time. These findings of naphthalimide corbelled aminothiazoximes as a small-molecule class of anti-MRSA agents held promise in strategies for treatment of MRSA infections.
Piperazine-bridged naphthalimide aminothiazole oxime compound as well as preparation method and application thereof
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Paragraph 0036-0040, (2021/03/13)
The invention relates to piperazine bridged naphthalimide aminothiazole oxime compounds as well as a preparation method and application thereof, and belongs to the technical field of chemical synthesis. The piperazine-bridged naphthalimide aminothiazole oxime compound is shown as a general formula I, has certain inhibitory activity on one or more of gram-positive bacteria, gram-negative bacteria and fungi, and can be used for preparing antibacterial and/or antifungal drugs, so that more efficient and safe candidate drugs are provided for clinical antimicrobial treatment, and the clinical treatment problems of increasingly serious drug resistance, stubborn pathogenic microorganisms, newly appearing harmful microorganisms and the like are favorably solved. The preparation raw materials are simple, cheap and easy to obtain, the synthetic route is short, and the method has important significance in anti-infection application.
N and P active materials for organic photoelectric conversion layers in organic photodiodes
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Paragraph 0035; 0784; 0785, (2018/01/14)
The invention relates to the field of active materials for organic image sensors. The present invention relates to transparent N materials and/or to transparent P materials and their use in absorptionlayer(s), photoelectric conversion layer(s) and/or an o
Solvent dependent energy transfer of N-bridged naphthalimide- bisindolymaleimide fluorescent dyes
Li, Xiaochuan,Zhu, Kaijuan,Li, Yajuan,Kim, Hyungjoo,Son, Young-A
, p. 18 - 26 (2014/01/23)
Double build-in chromophores, naphthalimide (NIM) and bisindolymaleimide (BIM), were synthesized and characterized. Absorption and emission properties of double chromophores dye were fully investigated in various solvents. The priority of through bond ene
Synthesis and properties of dicarboximide derivatives of perylene and azaperylene
Nagao, Yukinori,Yoshida, Tatsurou,Arimitsu, Koji,Kozawa, Kozo
experimental part, p. 1197 - 1213 (2010/10/04)
The N-alkyl dicarboximide derivatives of naphthylisoquinoline and binaphthalene were prepared by the hetero coupling reaction of the corresponding N-alkyl dicarboximide derivatives of stannylnaphthalene with bromodimethyisoquinoline and bromodimethylnaphthalene, respectively. The ring closing of the N-hexyl derivatives of naphthylisoquinoline and binaphthalene produced the N-hexyldicarboximide derivatives of azaperylene and perylene having the same substituents, respectively. The absorption spectra and fluorescence spectra of the azaperylene and perylene derivatives were investigated.
Synthesis and modification of terrylenediimides as high-performance fluorescent dyes
Nolde, Fabian,Qu, Jianqiang,Kohl, Christopher,Pschirer, Neil G.,Reuther, Erik,Muellen, Klaus
, p. 3959 - 3967 (2007/10/03)
Two new synthetic approaches to terrylenediimides, highly photostable fluorescent dyes, are described. For the first time terrylenediimide has been synthesised in a straightforward procedure that makes large quantities available. The second route includes an efficient cross-coupling reaction followed by a cyclodehy-drogenation. Monofunctionalisation of the imide structure allows terrylenediimides now to be coupled with a variety of compounds, for example, by Suzuki cross-coupling, which can lead to an array of terrylenediimides with new functional groups such as hydroxy, amino, or carboxy groups needed to link up with other molecules. The functionalisation in the bay region is used to tune the properties of terrylenediimides and extend the range of applications, for example, by introducing water solubility. These tetrasubstituted terrylenediimides offer, depending on the substituents used, exciting features such as good solubility in common organic solvents, water solubility, or NIR absorption.
