Design, synthesis and photochromism studies of thienyl containing triarylethylene derivatives and their applications in real-time photoresponsive surfaces

2018 ◽  
Vol 6 (32) ◽  
pp. 8832-8838 ◽  
Author(s):  
Leyu Wang ◽  
Tao Yu ◽  
Zongliang Xie ◽  
Xiaojie Chen ◽  
Zhan Yang ◽  
...  
Keyword(s):  
Real Time ◽  
Photochromic Properties ◽  
Design Synthesis ◽  
Chemical Structures ◽  
Simple Chemical ◽  
Photochromic Materials

Developing new photochromic materials with simple chemical structures, striking photochromic properties, real-time morphology changeable surfaces and tunable wettability.

Hybridized Quinoline Derivatives as Anticancer Agents: Design, Synthesis, Biological Evaluation and Molecular Docking

2019 ◽  
Vol 19 (4) ◽  
pp. 439-452 ◽  
Author(s):  
Mohamed R. Selim ◽  
Medhat A. Zahran ◽  
Amany Belal ◽  
Moustafa S. Abusaif ◽  
Said A. Shedid ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Caspase 3 ◽  
Biological Evaluation ◽  
Tubulin Polymerization ◽  
Design Synthesis ◽  
Chemical Structures ◽  
M Phase ◽  
Induced Apoptosis ◽  
Derivatives Of

Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.

scholarly journals Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives

2020 ◽  
Vol 32 (3) ◽  
pp. 580-586
Author(s):  
Ranjit V. Gadhave ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Biological Evaluation ◽  
Bacterial Strains ◽  
Active Compounds ◽  
Design Synthesis ◽  
Structural Modifications ◽  
E Coli ◽  
Chemical Structures ◽  
Ft Ir ◽  
Antioxidant Agent

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

scholarly journals Synthesis, Anti-Inflammatory Activity, and In Silico Study of Novel Diclofenac and Isatin Conjugates

2018 ◽  
Vol 2018 ◽  
pp. 1-11
Author(s):  
Musab Mohamed Ibrahim ◽  
Tilal Elsaman ◽  
Mosab Yahya Al-Nour
Keyword(s):  
Virtual Screening ◽  
Condensation Reaction ◽  
Docking Study ◽  
Positive Control ◽  
Inflammatory Activity ◽  
Molecular Docking Study ◽  
Design Synthesis ◽  
Chemical Structures ◽  
Anti Inflammatory

The design, synthesis, and development of novel non-steroidal anti-inflammatory drugs (NSAIDs) with better activity and lower side effects are respectable area of research. Novel Diclofenac Schiff’s bases (M1, M2, M4, M7, and M8) were designed and synthesized, and their respective chemical structures were deduced using various spectral tools (IR, 1H NMR, 13C NMR, and MS). The compounds were synthesized via Schiff’s condensation reaction and their anti-inflammatory activity was investigated applying the Carrageenan-induced paw edema model against Diclofenac as positive control. Percentage inhibition of edema indicated that all compounds were exhibiting a comparable anti-inflammatory activity as Diclofenac. Moreover, the anti-inflammatory activity was supported via virtual screening using molecular docking study. Interestingly compound M2 showed the highest in vivo activity (61.32% inhibition) when compared to standard Diclofenac (51.36% inhibition) as well as the best binding energy score (-10.765) and the virtual screening docking score (-12.142).

Functionalization of Cellulose Paper by Coating Nano Metal-Organic Frameworks for Use as Photochromic Material

2021 ◽  
Vol 43 (1) ◽  
pp. 67-67
Author(s):  
Qiang Yang Qiang Yang ◽  
Wei Gong Wei Gong ◽  
Xiaowei Cui Xiaowei Cui ◽  
Chunsheng Zhou Chunsheng Zhou
Keyword(s):  
Functional Materials ◽  
Photochromic Properties ◽  
Coated Paper ◽  
Cellulose Paper ◽  
Chemical Structures ◽  
Coating Method ◽  
Potential Applications ◽  
Metal Organic ◽  
Light Green ◽  
Photochromic Reaction

The cellulose paper-based functional materials modified by Zn-NDI and Cu-NDI were prepared by the coating method. The chemical structures were characterized by FTIR, XRD, UV-vis and SEM, and the photochromic properties of the composite functional materials were studied. The results showed that Zn-NDI and Cu-NDI were successfully prepared and retained on the surface of copy paper, the wavelength of photochromic reaction is between 300-400 nm of MOFs materials. Optical analysis confirmed that the NDI/paper, Zn-NDI/paper and Cu-NDI/paper changed from tan to wheat, light green to olive, and dark tan to brown after 60 seconds of exposure to hernia light irradiations, the MOFs coated paper returned to its original color when it was placed in the dark for 4 hours. The above results indicated that the prepared Zn-NDI and Cu-NDI coated paper composites exhibited excellent photochromic ability and had potential applications in the field of anti-counterfeiting packaging materials.

Aldehyde-Substituted Donor–Acceptor-Type Dithienylethenes as Novel Building Blocks for Photochromic Materials

2018 ◽  
Vol 42 (10) ◽  
pp. 531-534 ◽  
Author(s):  
Yangyang Wang ◽  
Mengna Li ◽  
Yufei Song ◽  
Ming Qin ◽  
Xuehui Li ◽  
...  
Keyword(s):  
Dft Calculations ◽  
Near Infrared ◽  
Building Blocks ◽  
Formyl Group ◽  
Photochromic Properties ◽  
H Nmr ◽  
Donor Acceptor ◽  
Group Functions ◽  
Photochromic Materials ◽  
C Nmr

Two novel donor–π–acceptor-type dithienylethene derivatives, in which the triphenylamine group acts as electron donor and the formyl group functions as electron acceptor, have been developed. Their structures were confirmed by 1H NMR, 13C NMR and HRMS (ESI). Investigation of their photochromic properties indicated that they had good photochromic behaviour and excellent fatigue resistance on irradiation with UV or visible light. DFT calculations further validated these experimental results for photochromic behaviour. Moreover, these compounds can be utilised as versatile building blocks to construct novel near-infrared photochromic materials.

scholarly journals Robust microscale grasping through a multimodel design: synthesis and real time implementation

2015 ◽  
Vol 39 ◽  
pp. 12-22 ◽  
Author(s):  
Mokrane Boudaoud ◽  
Marcelo Gaudenzi De Faria ◽  
Yassine Haddab ◽  
Sinan Haliyo ◽  
Yann Le Gorrec ◽  
...  
Keyword(s):  
Real Time ◽  
Design Synthesis

Preparation and Properties of Photochromic Microspheres

2013 ◽  
Vol 785-786 ◽  
pp. 618-623
Author(s):  
Dong Ying Li ◽  
Gui Fang Wang ◽  
Guang Ling Pei
Keyword(s):  
Dispersion Medium ◽  
Room Temperature ◽  
Mixed Solution ◽  
Polystyrene Microspheres ◽  
Photochromic Properties ◽  
Adsorption Parameters ◽  
Adsorption Temperature ◽  
Photochromic Materials ◽  
Sun Light ◽  
Adsorption Quantity

Monodisperse porous polystyrene microspheres were prepared with the mixed solution of ethanol and water as dispersion medium and poly (vinylpyrrolidone) was used as dispersant. The even size of microspheres prepared at optimal process was about 1μm. Photochromic microspheres were obtained using polystyrene microspheres to absorb the photochromic materials. The effect of dispersion medium on the microspheres morphology was investigated. The adsorption parameters affecting microspheres adsorption quantity, such as the concentration of spiropyran solution and adsorption temperature, were studied in detail. Furthermore, photochromic properties of the microspheres were analyzed and PVA as coating was used to increase the fatigue resistance of photochromic microcapsules. The photochromic microspheres obtained could rapid reversibly change color under UV or sun light at room temperature and common pressure.

scholarly journals Design, Synthesis, and Antifungal Activity of New α-Aminophosphonates

2011 ◽  
Vol 2011 ◽  
pp. 1-11 ◽  
Author(s):  
Zahra Rezaei ◽  
Soghra Khabnadideh ◽  
Kamiar Zomorodian ◽  
Keyvan Pakshir ◽  
Setareh Nadali ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Active Site ◽  
Catalytic Effect ◽  
Docking Study ◽  
Microsporum Canis ◽  
Pharmacological Activities ◽  
Design Synthesis ◽  
Chemical Structures ◽  
New Compounds ◽  
Time Of Reaction

α-Aminophosphonates are bioisosteres of amino acids and have several pharmacological activities. These compounds have been synthesized by various routes from reaction between amine, aldehyde, and phosphite compounds. In order to synthesize α-aminophosphonates, catalytic effect of CuCl2 was compared with FeCl3. Also all designed structures as well as griseofulvin were docked into the active site of microtubule (1JFF), using Autodock program. The results showed that the reactions were carried out in the presence of CuCl2 in lower yields, and also the time of reaction was longer in comparison with FeCl3. The chemical structures of the new compounds were confirmed by spectral analyses. The compounds were investigated for antifungal activity against several fungi in comparison with griseofulvin. An indole-derived bis(α-aminophosphonates) with the best negative ΔG in docking study showed maximum antifungal activity against Microsporum canis, and other investigated compounds did not have a good antifungal activity.

scholarly journals Design, Synthesis, Characterisation & Anticonvulsant Activities of Novel Heterocyclic Substituted Isatin Derivatives

2020 ◽  
Vol 11 (4) ◽  
pp. 6351-6362
Author(s):  
Kosaraju Lahari ◽  
Raja Sundararajan
Keyword(s):  
Pharmacophore Model ◽  
Epileptic Activity ◽  
Anticonvulsant Drugs ◽  
Rotarod Test ◽  
Design Synthesis ◽  
Active Analog ◽  
Chemical Structures ◽  
Anticonvulsant Activities ◽  
Isoxazole Derivatives ◽  
Isatin Derivatives

Twelve new isoxazole/pyrazole/pyrimidine substituted 5-nitrosation analogues were designed according to the requirements of the anticonvulsant drugs pharmacophore model and synthesised from indole-2,3-dione. Entire prepared compounds chemical structures were established from its IR, proton-NMR, Mass spectrum & microanalysis data. Anticonvulsant potency of final isatin analogues was assessed by MES technique & sc PTZ technique. Besides rotarod test was used to assess the neurotoxicity of all potent title analogues. Title compounds exhibited a varying degree of anticonvulsant potency ranging from mild to good. In the present study, it was concluded that pyrazole derivatives exhibited higher anti-epileptic activity than isoxazole derivatives. However, pyrimidine analogues displayed inferior activity than isoxazole analogues. 4-(2-(4-(1-((Dimethylamino)methyl)-5-nitro-2-oxindole-3-ylideneamino)phenyl) hydrazone)-1-(4-chlorophenyl)-3-amino-1H-pyrazole-5(4H)-one 7c was established as the most active analog of this series. Hence this derivative can act as a pilot molecule for further progress of new effective anticonvulsant drugs.

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