The title compounds, C20H17NO3S, (I), and C19H15NO2S, (II), were prepared by the reaction of benzo[b]thiophene‐2‐carbaldehyde with (3,4,5‐trimethoxyphenyl)acetonitrile and (3,4‐dimethoxyphenyl)acetonitrile, respectively, in the presence of methanolic potassium hydroxide. In (I), the C=C bond linking the benzo[b]thiophene and the 3,4,5‐trimethoxyphenyl units has E geometry, with dihedral angles between the plane of the bridging unit and the planes of the two adjacent ring systems of 5.2 (3) and 13.1 (2)°, respectively. However, in (II), the C=C bond has Z geometry, with dihedral angles between the plane of the bridging unit and the planes of the adjacent benzo[b]thiophene and 3,4‐dimethoxyphenyl units of 4.84 (17) and 76.09 (7)°, respectively. There are no significant intermolecular hydrogen‐bonding interactions in the packing of (I) and (II). The packing is essentially stabilized via van der Waals forces. 相似文献
A series of novel 1-thiazolyl-5-coumarin-3-yl-pyrazole derivatives (4a–l) were synthesized via one-pot multicomponent reaction of 5-substituted salicylaldehydes (1a–c), 4-hydroxy-6-methyl-2H-pyran-2-one (2) and 2-hydrazinyl-4-arylthiazoles (3a–d) in acetonitrile using a catalytic amount of piperidine under reflux conditions. This multicomponent approach has advantages such as reduced reaction time and a high product yield percentage when compared with corresponding multistep approaches. All the synthesized compounds were evaluated for their cytotoxic activity against Hep G2 (hepatocellular liver carcinoma) and MCF-7 (breast cancer) cell lines and compared with the standard drug Doxorubicin. Among all the compounds, compounds 4d against Hep G2, 4k against MCF-7 and 4e against both Hep G2 & MCF-7 showed excellent cytotoxic activity. 相似文献
Control over supramolecular assemblies of donor and acceptor arrays in nanoscale dimension that facilitate efficient energy transfer resulting in tunable emission is an outstanding challenge. In pursuit of this goal, we have designed a supramolecular donor-acceptor organogel with tunable emission from green to red through controlled energy transfer by simply varying the acceptor concentration. Temperature-dependent UV/vis absorption, XRD, and AFM studies of the coassembly of 1 (donor) and 2 (acceptor) revealed the intercalation of 2 within the self-assembly of 1. Upon excitation of the decane gels of 1 with 0-2 mol % of 2, quenching of the emission of the former at 509 nm with the formation of the monomer emission of the latter at 555 nm is observed. Upon further addition of 2 (2-20 mol %), the emission was continuously red-shifted to 610 nm, which corresponds to the aggregate emission of 2. Consequently, a 98% quenching of the donor emission was observed at 509 nm. Fluorescence microscopic studies provided visual evidence for the color tuning of the FRET emission. Thus efficient trapping of excitons by "isolated" or "aggregated" acceptors through a subtle control of the self-assembly and the photophysical properties of the donor-acceptor building blocks allowed a continuous shifting of the emission color anywhere between green and red (lambdamax, 509-610 nm) in a supramolecular light harvesting system. 相似文献
α-Amylase and α-Glucosidase are important therapeutic targets for type II diabetes. The present focus of our study is to elucidate the hypoglycemic activity of novel compounds through in vitro and in silico studies. Here, we synthesized the nitro acridines (3a–3c), amino acridines (4a–4c), and nitro phenylquinoline (3d) and amino phenylquinoline (4d) using a multi-step reaction protocol in good yields. All the above derivatives were screened for molecular docking, α-Amylase and α-Glucosidase inhibitory activities utilizing acarbose as standard drug. In silico studies were performed to explore the binding ability of compounds with the active site of α-Amylase and α-Glucosidase enzymes. The in vitro antihyperglycemic report of 3c exhibits the maximum inhibitory activity with IC50 values of 200.61?±?9.71 μmol/mL and 197.76?±?8.22 μmol/mL against α-Amylase and α-Glucosidase, respectively. Similarly, the compound 3a exhibits IC50 values of 243.78?±?13.25 μmol/mL and 296.57?±?10.66 μmol/mL, and 4c exhibits IC50 values of 304.28?±?3.51 μmol/mL and 278.86?±?3.24 μmol/mL with a significant p?<?0.05 in both enzyme inhibitions. In addition, the presence of diverse functional moieties in synthesized compounds may provide a strong inhibitory action against the abovementioned enzymes compared with standard acarbose inhibition (IC50, 58.74?±?3.68 μmol/mL and 49.39?±?4.94 μmol/mL). Also, the docking studies provided an excellent support for our in vitro studies. The outcome of these studies recommends that the tested compounds might be treated as potential inhibitors for the starch hydrolyzing enzymes in type II diabetes.
(Z)‐3‐(1H‐Indol‐3‐yl)‐2‐(3‐thienyl)acrylonitrile, C15H10N2S, (I), and (Z)‐3‐[1‐(4‐tert‐butylbenzyl)‐1H‐indol‐3‐yl]‐2‐(3‐thienyl)acrylonitrile, C26H24N2S, (II), were prepared by base‐catalyzed reactions of the corresponding indole‐3‐carboxaldehyde with thiophene‐3‐acetonitrile. 1H/13C NMR spectral data and X‐ray crystal structures of compounds (I) and (II) are presented. The olefinic bond connecting the indole and thiophene moieties has Z geometry in both cases, and the molecules crystallize in space groups P21/c and C2/c for (I) and (II), respectively. Slight thienyl ring‐flip disorder (ca 5.6%) was observed and modeled for (I). 相似文献
Fullerenes are soccer ball-shaped molecules composed of carbon atoms, and, when derivatized with functional groups, they become soluble and can act as photosensitizers. Antimicrobial photodynamic therapy combines a nontoxic photosensitizer with harmless visible light to generate reactive oxygen species that kill microbial cells. We have compared the antimicrobial activity of six functionalized C(60) compounds with one, two, or three hydrophilic or cationic groups in combination with white light against gram-positive bacteria, gram-negative bacteria, and fungi. After a 10 min incubation, the bis- and tris-cationic fullerenes were highly active in killing all tested microbes (4-6 logs) under conditions in which mammalian cells were comparatively unharmed. These compounds performed significantly better than a widely used antimicrobial photosensitizer, toluidine blue O. The high selectivity and efficacy exhibited by these photosensitizers encourage further testing for antimicrobial applications. 相似文献