Unsymmetrically Substituted Dibenzo[b,f][1,5]-diazocine-6,12(5H,11H)dione—A Convenient Scaffold for Bioactive Molecule Design

A novel approach for the synthesis of unsymmetrically substituted dibenzo[b,f][1,5]diazocine-6,12(5H,11H)diones has been developed. This facile three-step method uses variously substituted 1H-benzo[d][1,3]oxazine-2,4-diones (isatoic anhydrides) and 2-aminobenzoic acids as a starting materials. The obtained products were further transformed into N-alkyl-, N-acetyl- and dithio analogues. Developed procedures allowed the synthesis of unsymmetrical dibenzo[b,f][1,5]diazocine-6,12(5H,11H)diones and three novel heterocyclic scaffolds: benzo[b]naphtho[2,3-f][1,5]diazocine-6,14(5H,13H)dione, pyrido[3,2-c][1,5]benzodiazocine-5,11(6H,12H)-dione and pyrazino[3,2-c][1,5]benzodiazocine-6,12(5H,11H)dione. For 11 of the compounds crystal structures were obtained. The preliminary cytotoxic effect against two cancer (HeLa, U87) and two normal lines (HEK293, EUFA30) as well as antibacterial activity were determined. The obtained dibenzo[b,f][1,5]diazocine(5H,11H)6,12-dione framework could serve as a privileged structure for the drug design and development.

Download Full-text

Acalypha Indica mediated MgO NPs: A novel approach in greener route with its antibacterial activity against pathogens

Nanoscale Reports ◽

10.26524/nr.3.12 ◽

2020 ◽

Vol 3 (2) ◽

Author(s):

Kavipriya K C ◽

Sudha A P ◽

Sujatha K ◽

Sowmya Lakshmi K

Keyword(s):

Antibacterial Activity ◽

Metal Oxides ◽

Bacterial Species ◽

Magnesium Nitrate ◽

Precipitation Method ◽

Average Crystalline Size ◽

Face Centered Cubic ◽

X Ray ◽

Novel Approach ◽

Acalypha Indica

The interest in miniaturization of particles revealed the hidden applications of metal oxides. The potential applications of the particles may vary when the size of the particle is reduced. One of the alternative routes to the conventional approach is the use of plant extract for the synthesis of metal oxides NPs. In the framework of this study, the ecofriendly MgO nanoparticles were synthesized using Acalypha Indica leaf extract,functioning as reducing and capping agent by co-precipitation method. The predecessor taken here was Magnesium Nitrate. The biologically synthesized MgO NPs were characterized by various techniques like X ray diffraction(XRD), Fourier Transform infrared spectroscopy(FTIR), Scanning electron microscope (SEM) with Energy Dispersive X-ray spectroscopy(EDX) profile and its antibacterial activity is evaluated against causative organisms. XRD studies confirmed the face centered cubic crystalline structure of MgO NPs and the average crystalline size of MgO NPs calculated using Scherer’s formula was found to be 13 nm. FTIR spectrum shows a significant Mg-O vibrational band. Purity, surface morphology and chemical composition of elements were confirmed by SEM with EDX. The SEM result shows the fine spherical morphology with the grain size range between 43nm to 62nm. Antimicrobial assay of MgO NPs was examined against gram positive and negative bacteria. Appreciated activity was observed on the Staphylococcus aureus bacterial species. In general, the renewed attempt of this facile approach gave the optimum results of multifunctional MgO NPs.

Download Full-text

Green synthesis, characterization of silver sulfide nanoparticles and antibacterial activity evaluation

10.31221/osf.io/8byuc ◽

2019 ◽

Author(s):

Chem Int

Keyword(s):

Antibacterial Activity ◽

Large Scale ◽

Research Work ◽

Silver Sulfide ◽

Morphological Properties ◽

Effective Diameter ◽

Novel Approach ◽

Transmission Electron ◽

Green Route ◽

Silver Sulfide Nanoparticles

This research work presents a facile and green route for synthesis silver sulfide (Ag2SNPs) nanoparticles from silver nitrate (AgNO3) and sodium sulfide nonahydrate (Na2S.9H2O) in the presence of rosemary leaves aqueous extract at ambient temperature (27 oC). Structural and morphological properties of Ag2SNPs nanoparticles were analyzed by X-ray diffraction (XRD) and transmission electron microscopy (TEM). The surface Plasmon resonance for Ag2SNPs was obtained around 355 nm. Ag2SNPs was spherical in shape with an effective diameter size of 14 nm. Our novel approach represents a promising and effective method to large scale synthesis of eco-friendly antibacterial activity silver sulfide nanoparticles.

Download Full-text

Ethanolamine: A Potential Promoiety with Additional Effects in the Brain

CNS & Neurological Disorders - Drug Targets ◽

10.2174/1871527319999201211204645 ◽

2020 ◽

Vol 19 ◽

Author(s):

Asfree Gwanyanya ◽

Christie Nicole Godsmark ◽

Roisin Kelly-Laubscher

Keyword(s):

Central Nervous System ◽

Nervous System ◽

Drug Design ◽

Cell Signaling ◽

Blood Brain Barrier ◽

Brain Barrier ◽

The Central Nervous System ◽

Bioactive Molecule ◽

Positive Functions ◽

The Brain

Abstract: Ethanolamine is a bioactive molecule found in several cells, including those in the central nervous system (CNS). In the brain, ethanolamine and ethanolamine-related molecules have emerged as prodrug moieties that can promote drug movement across the blood-brain barrier. This improvement in the ability to target drugs to the brain may also mean that in the process ethanolamine concentrations in the brain are increased enough for ethanolamine to exert its own neurological ac-tions. Ethanolamine and its associated products have various positive functions ranging from cell signaling to molecular storage, and alterations in their levels have been linked to neurodegenerative conditions such as Alzheimer’s disease. This mini-review focuses on the effects of ethanolamine in the CNS and highlights the possible implications of these effects for drug design.

Download Full-text

Structural insights into targeting of the colchicine binding site by ELR510444 and parbendazole to achieve rational drug design

RSC Advances ◽

10.1039/d1ra01173a ◽

2021 ◽

Vol 11 (31) ◽

pp. 18938-18944

Author(s):

Jia-Hong Lei ◽

Ling-Ling Ma ◽

Jing-Hong Xian ◽

Hai Chen ◽

Jian-Jian Zhou ◽

...

Keyword(s):

Drug Design ◽

Binding Site ◽

Crystal Structures ◽

Rational Drug Design ◽

Colchicine Binding Site ◽

Rational Drug ◽

Structural Insights

Crystal structures of tubulin complexed with ELR510444 and parbendazole facilitate the design of novel colchicine binding site inhibitors.

Download Full-text

Crystal structures of two inhibitors in complex with histone lysine demethylase 4D (KDM4D) provide new insights for rational drug design

Biochemical and Biophysical Research Communications ◽

10.1016/j.bbrc.2021.03.083 ◽

2021 ◽

Vol 554 ◽

pp. 71-75

Author(s):

Tianqi Wang ◽

Yang Liu ◽

Hailin Zhang ◽

Zhen Fang ◽

Rong Zhang ◽

...

Keyword(s):

Drug Design ◽

Crystal Structures ◽

Rational Drug Design ◽

Histone Lysine ◽

Rational Drug ◽

Histone Lysine Demethylase ◽

Lysine Demethylase

Download Full-text

Temperature Dependent On Activated Carbon For Their Biological Activity And Photocatalytical Degradation of Methylene Blue: A Novel Approach To Green Synthesis

10.21203/rs.3.rs-792713/v1 ◽

2021 ◽

Author(s):

Amalanathan.M ◽

Aravind.M ◽

Sony Michael Mary.M ◽

Razan A. Alshgari ◽

Asma A. Alothman ◽

...

Keyword(s):

Methylene Blue ◽

Antibacterial Activity ◽

Activated Carbon ◽

Hydrothermal Carbonization ◽

Microbial Pathogens ◽

X Ray Diffraction ◽

E Coli ◽

Novel Approach ◽

Transmission Electron ◽

Ft Ir

Abstract In this work, jasmine flower derived activated carbon were successfully synthesized by hydrothermal carbonization process at the different annealing temperature. The Crystallinity, phase, structural, morphological and optical properties of activated carbon were investigated using X-ray diffraction (XRD), Fourier Transform Infrared spectroscopy (FT-IR), Scanning electron microscopy (SEM), Transmission electron microscope (TEM), and UV-visible spectroscopy analysis. The graphitic phase of carbon was obtained from the XRD pattern. Surface morphology reveals irregular-shaped nanoparticles. The photodegradation of methylene blue (MB) was carried out under the visible light irradiation technique to study its photocatalytic activity. The activated carbon obtained at 400oC, 500oC and 600oC shows a photocatalytic degradation efficiency of 86%, 90%, and 94%, respectively. Antibacterial activity of activated carbon was examined against S. Aureus (MTCC-737) and E-Coli (MTCC- 443) microbial pathogens, and their potent antibacterial activity was examined from the zone of inhibition layer.

Download Full-text