ITO/Poly-3-Methylaniline/Au Electrode for Electrochemical Water Splitting and Dye Removal

Application of aniline derivative semiconductor nanopolymer and its Au composite for H2 generation and dye removal were investigated. Electrochemical polymerization of poly-3-methylaniline (P3MA) on ITO glass was carried out for acid medium. Au nanoparticles with crystal sizes of 15 and 30 nm were sputter coated on the surface. Chemical structure of the polymer and its composite was characterized using FTIR, XRD, 1HNMR, SEM, and UV-Vis. All function groups were confirmed using FTIR analyses. XRD confirmed the formation of nanopolymer with a crystal size of ~15 nm. SEM confirmed the formation of smooth lamellar surface feature with a <20 nm nanoporous structure. Porosity and particle sizes increases with Au coating, confirmed using the modeling Image J program. Optical analysis also demonstrated that the strength of P3MA absorption peaks increases with rising Au coating time, in which the bandgap values changed from 1.64 to 1.63 eV for 15 and 30 nm Au, respectively. The photoelectrode ITO/PMT/30 nm Au was applied for H2 generation and dye removal. The current density (Jph) values were -0.3 and -1.6 mA.cm-2 in the absence and presence of the Congo red dye, respectively. The incident photon-to-current conversion efficiency (IPCE%) for the electrode was 2.3 at 390 nm. The activation energy (Ea) was 31.49 KJ mol-1. The enthalpy (∆H*) and entropy (∆S*) values were 114.49 and 160.46 JK-1 mol-1, respectively. A simple mechanism for the H2 generation and dye removal is mentioned

Design and Synthesis of an Aniline Derivative with Biological Activity on Heart Failure

Background: Several compounds have been synthesized as a therapeutic alternative for heart failure; however, its preparation requires special conditions. Objective: The aim of this study, was to synthesize some aniline derivatives (4-9) from 3-ethynylaniline to evaluate their biological activity against heart failure. Methods: The synthesis of aniline derivatives involved a series of reactions such as etherification, addition, and cyclization. The structure of all compounds obtained was confirmed by spectroscopic and spectrometric methods. In addition, to evaluate the biological activity of compounds an ischemia/reperfusion injury model was used. Results: The results showed that compound 8 decreases heart failure, which translates into a decrease in the infarction area compared to compounds 4-7 and 9. Conclusion: This study is reported a facile method for the preparation of aniline derivatives. This method offers some advantages such as; a simple procedure, low cost, and ease of work. In addition, compound 8 showed an interesting biological activity against heart failure. This phenomenon is particularly interesting because the biological activity induced by this compound could involve a molecular mechanism different compared with other drugs used for the treatment of heart failure.

Chemical Synthesis, Efficacy, and Safety of Antimalarial Hybrid Drug Comprising of Sarcosine and Aniline Pharmacophores as Scaffolds

Malaria is a disease caused by protozoans transmitted to humans by infected female Anopheles mosquitoes. According to the WHO report of 2015, there were 214 million cases of malaria with 438,000 deaths worldwide. Ninety percent of world’s malaria cases occur in Africa, where the disease is recognized as a serious impediment to economic and social development. Despite advancement in malaria research, the disease continues to be a global problem, especially in developing countries. Currently, there is no effective vaccine for malaria control. In addition, although there are effective drugs for treatment of malaria, this could be lost to the drug resistance in different Plasmodium species. The most lethal form is caused by P. falciparum which has developed resistance to many chemotherapeutic agents and possibly to the current drugs of choice. Reducing the impact of malaria is a key to achieving the sustainable development goals which are geared toward combating the disease. Covalent bitherapy is a rational and logical way of drug design which entails joining a couple of molecules with individual intrinsic action into a unique agent, hence packaging dual activity into one hybrid. This suggests the need to develop new antimalarial drugs that are effective against malaria parasites based on the new mode of action, molecular targets, and chemical structures. In silico studies have shown that sarcosine is able to bind to unique plasmodia proteins (P. falciparum ATCase), whereas aniline can be a ligand to target protein (enoyl acyl carrier protein reductase), hence suppressing the progression of the disease. The main objective of this study was to synthesize and determine the efficacy and safety of antiplasmodial hybrid drug comprising the sarcosine and aniline derivative for management of plasmodial infections. The hybrid drug was synthesized by adding thionyl chloride to sarcosine to form acyl chloride which was then added to aniline to form sarcosine-aniline hybrid molecule. The IC50 of sarcosine-aniline hybrid was 44.80 ± 4.70 ng/ml compared with that of aniline derivative which was 22.86 ± 1.26 ng/ml. The IC50 of control drugs was 2.63 ± 0.38 ng/ml and 5.69 ± 0.39 ng/ml for artesunate and chloroquine, respectively. There was a significant difference between IC50 of sarcosine-aniline hybrid and aniline derivative (p<0.05). There was also a significant difference between sarcosine-aniline hybrid and standard drugs used to treat malaria including artesunate and chloroquine (p<0.05). The ED50 of sarcosine-aniline hybrid drug was 6.49 mg/kg compared with that of aniline derivative which was 3.61 mg/kg. The ED50 of control drugs was 3.56 mg/kg, 2.94 mg/kg, and 1.78 mg/kg for artesunate-aniline hybrid, artesunate, and chloroquine, respectively. There was a significant difference (p<0.05) between ED50 of sarcosine-aniline hybrid and both controls such as aniline derivative, artesunate, artesunate-aniline hybrid, and chloroquine. Cytotoxicity results revealed that sarcosine-aniline hybrid was safe to vero cells with a CC50 of 50.18 ± 3.53 μg/ml. Sarcosine-aniline hybrid was significantly less toxic compared with artesunate, chloroquine, and doxorubicin. Sarcosine-aniline hybrid was efficacious and safe to mice. Therefore, covalent bitherapy should be used in drug development for drug resistance mitigation.

Dithienylpyrrole Electrografting on a Surface through the Electroreduction of Diazonium Salts

The control of the interface and the adhesion process are key issues for the development of new application based on electrochromic materials. In this work the functionalization of an electrode’s surface through electroreduction of diazonium generated in situ from 4-(2,5-di-thiophen-2-yl-pyrrol-1-yl)-phenylamine (SNS-An) has been proposed. The synthesis of the aniline derivative SNS-An was performed and the electrografting was investigated by cyclic voltammetry on various electrodes. Then the organic thin film was fully characterized by several techniques and XPS analysis confirms the presence of an organic film based on the chemical composition of the starting monomer and allows an estimation of its thickness confirmed by AFM scratching measurements. Depending on the number of electrodeposition cycles, the thickness varies from 2 nm to 10 nm, which corresponds to a few grafted oligomers. In addition, the grafted film showed a good electrochemical stability depending on the scan rates up to 400 V/s and the electrochemical response of the modified electrode towards several redox probes showed that the attached layer acts as a conductive switch. Therefore, the electrode behaves as a barrier to electron transfer when the standard redox potential of the probe is below the layer switching potential, whereas the layer can be considered as transparent towards the electron transfer for redox probes with a redox potential above it.

Nanoscale lipid vesicles functionalized with a nitro-aniline derivative for photoinduced nitric oxide (NO) delivery

Photo-controllable, non-toxic and bio-compatible nano-scale vesicles for the controllable release of nitric oxide (NO) have been reported.

Chemical Synthesis, Efficacy and Safety of Antimalarial Hybrid Drug Comprising of Sarcosine and Aniline Pharmacophores as Scaffolds

Background: Reducing the impact of malaria is a key to achieving the sustainable development goals which are geared towards eradicating the disease. The main objective of this study was to synthesize, determine the efficacy and safety of antiplasmodial hybrid drug comprising of sarcosine and aniline derivative for management of plasmodial infections. Results: The hybrid drug was synthesized by adding thionyl chloride to sarcosine in order to form acyl chloride which was then added to aniline to form sarcosine-aniline hybrid molecule. The IC50 of sarcosine-aniline hybrid was 44.80 &plusmn; 4.70 ng/ml compared to that of aniline derivative which was 22.86 &plusmn; 1.26 ng/ml. The IC50 of control drugs were 2.63 &plusmn; 0.38 ng/ml, 5.69 &plusmn; 0.39 ng/ml for artesunate and chloroquine respectively. There was a significant difference between IC50 of sarcosine-aniline hybrid and aniline derivative (P&lt;0.05). There was also a significant difference between sarcosine-aniline hybrid and standard drugs used to treat malaria including artesunate and chloroquine (P&lt;0.05). The ED50 of sarcosine-aniline hybrid drug was 6.49mg/kg compared to that of aniline derivative which was 3.61mg/kg. The ED50 of control drugs were 3.56 mg/kg, 2.94mg/kg and 1.78 mg/kg for artesunate-aniline hybrid, artesunate and chloroquine respectively. There was a significant difference (P&lt;0.05) between ED50 of sarcosine-aniline hybrid and both controls such as aniline derivative, artesunate, artesunate-aniline hybrid and chloroquine. Cytotoxicity results revealed that sarcosine-aniline hybrid was safe to vero cells with a CC50 of 50.18&plusmn;3.53&micro;g/ml. Sarcosine-aniline hybrid was significantly less toxic compared to artesunate, chloroquine and doxorubicin. Sarcosine-aniline hybrid was also safe to mice. Conclusion: Therefore, covalent bitherapy should be used in drug development for drug resistance mitigation.

New Synthesis of a Dibenzoperylene Motif Featuring a Doubly Boron–Nitrogen-Doped Bay Region

A dibenzoperylene motif featuring a doubly boron–nitrogen-doped bay region is accessible from an aniline derivative in six steps in good overall yield. Two n-butyl groups provide the BN-doped polycyclic aromatic hydrocarbon with sufficient solubility in common organic solvents. The synthesis sequence allows installation of a second boron atom next to a weakly nucleophilic nitrogen by using a protected boron species. The title compound shows blue fluorescence, an extremely high fluorescence quantum yield, and an interesting doped bay region.