24239-07-4Relevant academic research and scientific papers
Water-soluble two-photon absorption benzoxazole-based pyridinium salts with the planar cationic parts: crystal structures and bio-imaging
Liu, Dan,Wang, Haiyan,Li, Hong,Zhang, Huihui,Liu, Qingsong,Wang, Zepeng,Gan, Xiaoping,Wu, Jieying,Tian, Yupeng,Zhou, Hongping
, p. 378 - 384 (2017)
Six new benzoxazole-based compounds 1–6 of the donor-bridge-accepter (D-π-A) type with different anions were obtained by methylation and anion exchange reaction. The single crystals of 1, 3 and 6 were obtained by slow evaporation of acetonitrile and determined by X-ray crystallography. Ellipsoidal structures of the three compounds showed that the cationic parts all maintained good planarity, which was beneficial for two-photon absorption (2PA) properties and accorded with the results of two-photon excited fluorescence tests. Biological imaging experiments showed water-soluble six compounds had excellent penetrability in living cells and could located in cytoplasm in one- and two-photon cell imaging. Biological imaging result of compound 6 was more excellent than other compounds, which indicated synergy of anions and cations played a very important role in cell imaging.
Synthesis and anticholinesterase activity of new substituted benzo[d]oxazole-based derivatives
Pouramiri, Behjat,Moghimi, Setareh,Mahdavi, Mohammad,Nadri, Hamid,Moradi, Alireza,Tavakolinejad-Kermani, Esmat,Firoozpour, Loghman,Asadipour, Ali,Foroumadi, Alireza
, p. 783 - 789 (2017)
A series of novel benzo[d]oxazole derivatives (6a–n) have been synthesized and biologically evaluated as potential inhibitors of acetylcholinesterases (AChE) and butyrylcholinesterase (BChE). The chemical structures of all final compounds were confirmed by spectroscopic methods. In vitro studies showed that most of the synthesized compounds are potent acetylcholinesterase and butyrylcholinesterase inhibitors. Among them, compounds 6a and 6j strongly inhibited AChE and BChE activities with IC50 values of 1.03–1.35 and 6.6–8.1?μm, respectively. Docking studies also provided the binding modes of action and identified hydrophobic pi forces as the main interaction.
Two-photon fluorescent material benzoxazole-based pyridinium salt as well as preparation method and application thereof
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Paragraph 0045; 0046, (2018/03/01)
The invention discloses a two-photon fluorescent material benzoxazole-based pyridinium salt as well as a preparation method and application thereof. The two-photon fluorescent material benzoxazole-based pyridinium salt is a water-soluble two-photon induced fluorescent material, is low in toxicity, has good membrane penetration performance, can enter cells, and can be used for the two-photon fluorescent confocal microscopic imaging. A structural formula of the two-photon fluorescent material benzoxazole-based pyridinium salt is as follows: (shown in the description).
Synthesis, biological evaluation and molecular docking of 2-phenyl-benzo[d]oxazole-7-carboxamide derivatives as potential Staphylococcus aureus Sortase A inhibitors
Zhang, Yong,Bao, Jian,Deng, Xin-Xian,He, Wan,Fan, Jia-Jun,Jiang, Fa-Qin,Fu, Lei
supporting information, p. 4081 - 4085 (2016/08/01)
A series of novel 2-phenyl-benzo[d]oxazole-7-carboxamide derivatives were designed, synthesized and evaluated for their in vitro inhibitory activities against Staphylococcus aureus Sortase A with known Sortase A inhibitor pHMB as positive compound (IC50?=?130?μM). Most compounds exhibited excellent inhibitory activity (IC50?=?19.8–184.2?μM). Structure–activity relationship studies demonstrated that substitution at 7-position and 2-position of benzoxazole had great influence on the activities. Specifically, the substituent at 7-position is indispensable for inhibitory activity. The molecular docking studies revealed the i-butyl amide group went towards the β6/β7 loop-β8 substructure of the protein and the benzoxazole core lied in a hydrophobic pocket composed of Ala118, Val166, Val168, Val169 and Ile182, shaping the whole molecule into a L-shape mode to be recognized by Sortase A.
AMINO BI- AND TRI-CARBOCYCLIC AKLANE BIS-ARYL SQUALENE SYNTHASE INHIBITORS
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, (2008/06/13)
This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
ALIPHATIC AMINO BIS-ARYL SQUALENE SYNTHASE INHIBITORS
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, (2008/06/13)
This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
MULTICYCLIC TERTIARY AMINE POLYAROMATIC SQUALENE SYNTHASE INHIBITORS
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, (2008/06/13)
This invention relates to polycyclic compounds containing two mono- and/or bicyclic rings and a basic tertiary amino group capable of forming an ammonium ion at biological pH and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention. The compounds of this invention are described by the formula where Ar I is phenylene or naphthylene, Ar II is phenyl or naphthyl and A is 1-azabicyclo[2.2.2]octan-3-yl
Side chain polymers exhibiting nonlinear optical response
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, (2008/06/13)
This invention provides novel side chain polymers which exhibit nonlinear optical response, and which have utility as a transparent optical component in all-optical and electrooptical light switch and light modulator devices. An invention side chain polymer is illustrated by the following structure: STR1
Bichromophoric benzotriazole-benzoxazole ultraviolet stabilizers and their use in organic compositions
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, (2008/06/13)
The invention relates to bichromophoric benzotriazole-benzoxazole compounds which have been found to be effective ultraviolet stabilizers. The invention also relates to ultraviolet degradable organic compositions containing a stabilizing amount of the bic
