24239-07-4Relevant articles and documents
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.
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.
