39170-09-7Relevant academic research and scientific papers
Carbazole-Terpyridine Donor-Acceptor Dyads with Rigid π-Conjugated Bridges
Matteucci, Elia,Baschieri, Andrea,Sambri, Letizia,Monti, Filippo,Pavoni, Eleonora,Bandini, Elisa,Armaroli, Nicola
, p. 1353 - 1365 (2019/07/18)
A series of molecules in which 9H-carbazole (electron donor, D) and 2,2′:6′,2′′-terpyridine (electron acceptor, A) are connected through rigid π-conjugated bridges (D-π-A systems) have been synthesized and their photophysical properties examined in detail, with the support of DFT calculations. The bridges are made of different sequences of ethynylene, phenylene, and anthracene groups. The synthetic strategies involve condensation of 2-acetylpyridine with the aromatic aldehyde moiety on different functionalized π-conjugated bridges and couplings with carbazole derivatives. The system incorporating anthracene in the bridge shows the typical absorption and emission fingerprints of this polycyclic hydrocarbon. The other systems have HOMOs and LUMOs centred, respectively, over the carbazole and the bridge and exhibit solvatochromic charge-transfer (CT) luminescence with high photoluminescence yield up to 70 %, except when an ethynylene unit is directly attached to the carbazole ring, due to a trans-bent non-emissive π–σ* excited state.
Discovery of (5-Phenylfuran-2-yl)Methanamine derivatives as new human sirtuin 2 Inhibitors
Wang, Lijiao,Li, Chao,Chen, Wei,Song, Chen,Zhang, Xing,Yang, Fan,Wang, Chen,Zhang, Yuanyuan,Qian, Shan,Wang, Zhouyu,Yang, Lingling
, (2019/08/07)
Human sirtuin 2 (SIRT2), a member of the sirtuin family, has been considered as a promising drug target in cancer, neurodegenerative diseases, type II diabetes, and bacterial infections. Thus, SIRT2 inhibitors have been involved in effective treatment strategies for related diseases. Using previously established fluorescence-based assays for SIRT2 activity tests, the authors screened their in-house database and identified a compound, 4-(5-((3-(quinolin-5-yl)ureido)methyl) furan-2-yl)benzoic acid (20), which displayed 63 ± 5% and 35 ± 3% inhibition against SIRT2 at 100 μM and 10 μM, respectively. The structure-activity relationship (SAR) analyses of a series of synthesized (5-phenylfuran-2-yl)methanamine derivatives led to the identification of a potent compound 25 with an IC50 value of 2.47 μM, which is more potent than AGK2 (IC50 = 17.75 μM). Meanwhile, 25 likely possesses better water solubility (cLogP = 1.63 and cLogS = ?3.63). Finally, the molecular docking analyses indicated that 25 fitted well with the induced hydrophobic pocket of SIRT2.
Synthesis of arylfurfural oximes and their biological evaluation
Aslam, Samina,Khakwani, Samia,Jnazeer, Areesha,Shahi, Mehrzadi Jnoureen,Yaqoob, Asma,Shafiq, Hamna,Manazer, Rafia,Nasim, Faizul Hassan,Khan, Misbahul Ain
, p. 1210 - 1214 (2016/04/10)
Various oximes of arylfurfural were prepared and characterized through elemental analysis and spectroscopic techniques (FTIR, 1H NMR, 13C NMR and Mass). Synthesized compounds were tested for their antioxidant, tyrosinase and chemotrypson activities.
5-Phenyl-2-furamidines: A new chemical class of potential antidepressants
Pong,Pelosi Jr.,Wessels,Yu,Burns,White,Anthony Jr.,Ellis,Wright,White Jr.
, p. 1411 - 1416 (2007/10/02)
A series of 5-phenyl-2-furamidines has been synthesized and evaluated for antidepressant activities. Substitution in the phenyl ring with a nitro (4) or an amino (12) group in the ortho-position resulted in an increase in antidepressant activity. Both 4 and 12 antagonized tetrabenazine-induced ptosis in rodents and inhibited norepinephrine (noradrenaline) uptake into crude synaptosomes of whole mouse brain at doses or concentrations comparable to those of the tricyclic antidepressants. However, these compounds did not possess the anticholinergic and antihistaminic activities common to tricyclic antidepressants. In addition, they lacked monoamine oxidase inhibitory activity. The 5-phenyl-2-furamidines represent a new chemical class of antidepressants and may be useful for depressive patients who cannot tolerate the compromising side effects of the tricyclic antidepressants and monoamine oxidase inhibitors.
