scholarly journals UV Properties and Loading into Liposomes of Quinoline Derivatives

2021 ◽  
Vol 5 (2) ◽  
pp. 28
Author(s):  
Sara Battista ◽  
Vincenzo Marsicano ◽  
Antonio Arcadi ◽  
Luciano Galantini ◽  
Massimiliano Aschi ◽  
...  
Keyword(s):  
Encapsulation Efficiency ◽  
Molecular Level ◽  
Fine Tuning ◽  
Medical Applications ◽  
Computational Studies ◽  
Quinoline Derivatives ◽  
Molecular Scaffolds ◽  
Lipid Structure ◽  
Pharmaceutical Applications ◽  
Liposome Size

The scientific relevance of quinolines is strictly linked to the fine-tuning of their features by functionalizing the heterocyclic core. Consequently, the compounds of this class are very versatile and can be used as possible drugs for a lot of medical applications. In this work, the inclusion of eight synthetic quinoline derivatives in liposomes formulated with different lipids was investigated in terms of the encapsulation efficiency and to highlight the effect on the liposome size distribution and thermotropic behavior. Excellent encapsulation was accomplished with all the quinoline/phospholipid combinations. Differences in the interactions at the molecular level, dependent on the quinoline molecular scaffolds and lipid structure, were observed, which could significantly bias the interaction with the drug and its release in pharmaceutical applications. Experiments in combination with computational studies demonstrated that the UV absorption of quinolines with expanded conjugation could be affected by the environment polarity. This was probably due to a solvent-dependent ability of these quinolines to stack into aggregates, which could also occur upon inclusion into the lipid bilayer.

scholarly journals The Noisy and Marvelous Molecular World of Biology

Inventions ◽  
2019 ◽  
Vol 4 (2) ◽  
pp. 24
Author(s):  
Felix Ritort
Keyword(s):  
Single Molecule ◽  
Molecular Level ◽  
Second Law Of Thermodynamics ◽  
Physical World ◽  
Computational Studies ◽  
Biological Complexity ◽  
Concerted Action ◽  
Physical Information ◽  
Molecular Sequencing

At the molecular level biology is intrinsically noisy. The forces that regulate the myriad of molecular reactions in the cell are tiny, on the order of piconewtons (10−12 Newtons), yet they proceed in concerted action making life possible. Understanding how this is possible is one of the most fundamental questions biophysicists would like to understand. Single molecule experiments offer an opportunity to delve into the fundamental laws that make biological complexity surface in a physical world governed by the second law of thermodynamics. Techniques such as force spectroscopy, fluorescence, microfluidics, molecular sequencing, and computational studies project a view of the biomolecular world ruled by the conspiracy between the disorganizing forces due to thermal motion and the cosmic evolutionary drive. Here we will digress on some of the evidences in support of this view and the role of physical information in biology.

scholarly journals Electrospun Amphiphilic Nanofibers as Templates for In Situ Preparation of Chloramphenicol-Loaded Liposomes

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1742
Author(s):  
Ivo Laidmäe ◽  
Andres Meos ◽  
Irja Alainezhad Kjærvik ◽  
Sveinung G. Ingebrigtsen ◽  
Nataša Škalko-Basnet ◽  
...  
Keyword(s):  
Encapsulation Efficiency ◽  
Antibacterial Drug ◽  
Aqueous Dispersions ◽  
In Situ Preparation ◽  
Conventional Film ◽  
Liposome Preparation ◽  
Polymeric Nanofibers ◽  
Liposome Size

The hydration of phospholipids, electrospun into polymeric nanofibers and used as templates for liposome formation, offers pharmaceutical advantages as it avoids the storage of liposomes as aqueous dispersions. The objective of the present study was to electrospin and characterize amphiphilic nanofibers as templates for the preparation of antibiotic-loaded liposomes and compare this method with the conventional film-hydration method followed by extrusion. The comparison was based on particle size, encapsulation efficiency and drug-release behavior. Chloramphenicol (CAM) was used at different concentrations as a model antibacterial drug. Phosphatidylcoline (PC) with polyvinylpyrrolidone (PVP), using ethanol as a solvent, was found to be successful in fabricating the amphiphilic composite drug-loaded nanofibers as well as liposomes with both methods. The characterization of the nanofiber templates revealed that fiber diameter did not affect the liposome size. According to the optical microscopy results, the immediate hydration of phospholipids deposited on the amphiphilic nanofibers occurred within a few seconds, resulting in the formation of liposomes in water dispersions. The liposomes appeared to aggregate more readily in the concentrated than in the diluted solutions. The drug encapsulation efficiency for the fiber-hydrated liposomes varied between 14.9 and 28.1% and, for film-hydrated liposomes, between 22.0 and 77.1%, depending on the CAM concentrations and additional extrusion steps. The nanofiber hydration method was faster, as less steps were required for the in-situ liposome preparation than in the film-hydration method. The liposomes obtained using nanofiber hydration were smaller and more homogeneous than the conventional liposomes, but less drug was encapsulated.

scholarly journals Identifying Promiscuous Compounds with Activity against Different Target Classes

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4185 ◽  
Author(s):  
Christian Feldmann ◽  
Filip Miljković ◽  
Dimitar Yonchev ◽  
Jürgen Bajorath
Keyword(s):  
Small Molecules ◽  
Drug Targets ◽  
Molecular Level ◽  
Specific Interactions ◽  
Biological Screening ◽  
Systematic Analysis ◽  
X Ray ◽  
Binding Characteristics ◽  
Pharmaceutical Applications ◽  
Single Target

Compounds with multitarget activity are of high interest for polypharmacological drug discovery. Such promiscuous compounds might be active against closely related target proteins from the same family or against distantly related or unrelated targets. Compounds with activity against distinct targets are not only of interest for polypharmacology but also to better understand how small molecules might form specific interactions in different binding site environments. We have aimed to identify compounds with activity against drug targets from different classes. To these ends, a systematic analysis of public biological screening data was carried out. Care was taken to exclude compounds from further consideration that were prone to experimental artifacts and false positive activity readouts. Extensively assayed compounds were identified and found to contain molecules that were consistently inactive in all assays, active against a single target, or promiscuous. The latter included more than 1000 compounds that were active against 10 or more targets from different classes. These multiclass ligands were further analyzed and exemplary compounds were found in X-ray structures of complexes with distinct targets. Our collection of multiclass ligands should be of interest for pharmaceutical applications and further exploration of binding characteristics at the molecular level. Therefore, these highly promiscuous compounds are made publicly available.

Synthesis and pharmaceutical applications of Oxazine compounds derived from Pyronic, Salicylic, Antharanilic acids and Phenols

2021 ◽  
Vol 2 (2) ◽  
pp. 074-086
Author(s):  
Harith M. Al-ajely
Keyword(s):  
Organic Chemistry ◽  
Drug Discovery ◽  
Heterocyclic Compounds ◽  
Functional Group ◽  
Drug Action ◽  
Therapeutic Agents ◽  
Medical Applications ◽  
Important Class ◽  
Therapeutic Action ◽  
Pharmaceutical Applications

It is well known from FDA reports that More than 75% of the heterocyclic compounds are drugs and 90 of heterocyclic compounds are cancer drugs. The nitrogen-based heterocycles occupy an exclusive position as a valuable source of therapeutic agents in medicinal chemistry. Most drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties, More over heterocyclic compounds are important class of organic chemistry due to their widely spread in nature. Also there are many route for their action and many mechanistic pathways for their preparation and different metabolic actions. This comes from the easily building or removal of any functional group within the molecules. Changing just on group cause to change the metabolic pathway of the drug action and site of attack of the desired target accordingly. This great characteristic value make them much more important in drug discovery programs of many researchers and also encouraged us and drew attentions of other researchers to develop new ways for their synthesis. As a result different pharmacological and medical applications. Oxazie compounds are sub branch of heterocyclic compounds. These compounds having two hetero atoms, Oxygen and nitrogen within their structures make them much more important toward therapeutic studies. We are here in our investigation will focus on the methodologies and the therapeutic action of the titled compounds as well as other various applications.

Membrane Bioreactors for Pharmaceutical Applications: Optically Pure Enantiomers Production

2017 ◽  
Vol 23 (2) ◽  
pp. 250-262
Author(s):  
Emma Piacentini ◽  
Rosalinda Mazzei ◽  
Lidietta Giorno
Keyword(s):  
Kinetic Resolution ◽  
Molecular Level ◽  
Operation Mode ◽  
Academic Research ◽  
Membrane Bioreactors ◽  
Optical Isomers ◽  
Chiral Drugs ◽  
Natural Systems ◽  
Pharmaceutical Applications ◽  
Optically Pure

In biological systems, recognition at molecular level is governed by chiral interactions. Therefore, optical isomers have very different effect in natural systems. For example, one can have beneficial effect while the other can be very harmful. For these reasons, chiral drugs nowadays are mainly admitted in the optically pure form. Given these requirements, it is clear why demand for chiral drugs has grown dramatically and the singleenantiomer drug segment has become an important part of the overall pharmaceutical market. As a consequence, the development of new chiral separation techniques is a very hot topic in both academic research and industrial innovation. Membrane bioreactors have proven their feasibility in the production of optically pure enantiomers by combining enantiospecific biochemical reactions with mass transport through membranes. Conclusion: The principles and the applications of enantioselective membrane bioreactors in kinetic resolution for pharmaceutical applications will be discussed. Various membrane bioreactors configurations and operation mode will be illustrated. The type of enzymes utilized to produce chiral drugs or their intermediates will be also reported. Multistep syntheses, conducted in sequential reactions catalysed by spatially aligned biocatalysts, as promising technology for the synthesis of fine chemicals will be highlighted.

Synthetic Approaches of Pyrazolyl Quinolines

2019 ◽  
Vol 16 (4) ◽  
pp. 353-360 ◽  
Author(s):  
Rizk E. Khidre ◽  
Ibrahim Ali M. Radini ◽  
Diaa A. Ibrahim
Keyword(s):  
Glucose Transport ◽  
Pyrazole Ring ◽  
Review Article ◽  
Synthetic Methods ◽  
Medical Applications ◽  
Quinoline Derivatives ◽  
Quinoline Ring ◽  
Transport Inhibitors ◽  
Anti Inflammatory ◽  
Synthetic Approaches

This review article represents a survey of the synthetic strategies leading to pyrazolyl quinolines. The synthetic methods are divided into two main groups based on the type of starting reagents: 1) From quinoline ring onto a pyrazole scaffold, 2) From pyrazole ring onto a quinoline scaffold. Also, some medical applications of pyrazolyl quinoline derivatives are mentioned such as anticancer, cell proliferative disorder, glucose transport inhibitors, anti-inflammatory, and inhibitors of leukotriene production for the treatment of cardiovascular. The main purpose of this review is to present a survey of the literature on the synthetic approaches of pyrazolyl quinolines and provide useful and up-to-date data for organic and medicinal chemist since such compound has not been previously reviewed.

Molecular level investigation of 2,2,6,6-tetramethyl-3,5-heptanedione on Si(100)-2×1: Spectroscopic and computational studies

2008 ◽  
Vol 602 (13) ◽  
pp. 2222-2231 ◽  
Author(s):  
Kathryn A. Perrine ◽  
Dimitri B. Skliar ◽  
Brian G. Willis ◽  
Andrew V. Teplyakov
Keyword(s):  
Molecular Level ◽  
Computational Studies
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