scholarly journals Pyrido[2,3-d]pyrimidin-7(8H)-ones: Synthesis and Biomedical Applications

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4161 ◽  
Author(s):  
Guillem Jubete ◽  
Raimon Puig de la Bellacasa ◽  
Roger Estrada-Tejedor ◽  
Jordi Teixidó ◽  
José I. Borrell

Pyrido[2,3-d]pyrimidines (1) are a type of privileged heterocyclic scaffolds capable of providing ligands for several receptors in the body. Among such structures, our group and others have been particularly interested in pyrido[2,3-d]pyrimidine-7(8H)-ones (2) due to the similitude with nitrogen bases present in DNA and RNA. Currently there are more than 20,000 structures 2 described which correspond to around 2900 references (half of them being patents). Furthermore, the number of references containing compounds of general structure 2 have increased almost exponentially in the last 10 years. The present review covers the synthetic methods used for the synthesis of pyrido[2,3-d]pyrimidine-7(8H)-ones (2), both starting from a preformed pyrimidine ring or a pyridine ring, and the biomedical applications of such compounds.

2021 ◽  
Vol 14 (10) ◽  
pp. 1029
Author(s):  
Juan Marcos Oliveras ◽  
Raimon Puig de la Bellacasa ◽  
Roger Estrada-Tejedor ◽  
Jordi Teixidó ◽  
José I. Borrell

Naphthyridines, also known as diazanaphthalenes, are a group of heterocyclic compounds that include six isomeric bicyclic systems containing two pyridine rings. 1,6-Naphthyridines are one of the members of such a family capable of providing ligands for several receptors in the body. Among such structures, 1,6-naphthyridin-2(1H)-ones (7) are a subfamily that includes more than 17,000 compounds (with a single or double bond between C3 and C4) included in more than 1000 references (most of them patents). This review will cover the analysis of the diversity of the substituents present at positions N1, C3, C4, C5, C7, and C8 of 1,6-naphthyridin-2(1H)-ones, the synthetic methods used for their synthesis (both starting from a preformed pyridine or pyridone ring), and the biomedical applications of such compounds.


2019 ◽  
Vol 25 (34) ◽  
pp. 3608-3619 ◽  
Author(s):  
Uzma Arif ◽  
Sajjad Haider ◽  
Adnan Haider ◽  
Naeem Khan ◽  
Abdulaziz A. Alghyamah ◽  
...  

Background: Biocompatible polymers are gaining great interest in the field of biomedical applications. The term biocompatibility refers to the suitability of a polymer to body and body fluids exposure. Biocompatible polymers are both synthetic (man-made) and natural and aid in the close vicinity of a living system or work in intimacy with living cells. These are used to gauge, treat, boost, or substitute any tissue, organ or function of the body. A biocompatible polymer improves body functions without altering its normal functioning and triggering allergies or other side effects. It encompasses advances in tissue culture, tissue scaffolds, implantation, artificial grafts, wound fabrication, controlled drug delivery, bone filler material, etc. Objectives: This review provides an insight into the remarkable contribution made by some well-known biopolymers such as polylactic-co-glycolic acid, poly(ε-caprolactone) (PCL), polyLactic Acid, poly(3- hydroxybutyrate-co-3-hydroxyvalerate) (PHBV), Chitosan and Cellulose in the therapeutic measure for many biomedical applications. Methods: : Various techniques and methods have made biopolymers more significant in the biomedical fields such as augmentation (replaced petroleum based polymers), film processing, injection modeling, blow molding techniques, controlled / implantable drug delivery devices, biological grafting, nano technology, tissue engineering etc. Results: The fore mentioned techniques and other advanced techniques have resulted in improved biocompatibility, nontoxicity, renewability, mild processing conditions, health condition, reduced immunological reactions and minimized side effects that would occur if synthetic polymers are used in a host cell. Conclusion: Biopolymers have brought effective and attainable targets in pharmaceutics and therapeutics. There are huge numbers of biopolymers reported in the literature that has been used effectively and extensively.


2008 ◽  
Vol 396-398 ◽  
pp. 569-572
Author(s):  
Fumio Watari ◽  
Shigeaki Abe ◽  
I.D. Rosca ◽  
Atsuro Yokoyama ◽  
Motohiro Uo ◽  
...  

Nanoparticles may invade directly into the internal body through the respiratory or digestive system and diffuse inside body. The behavior of nanoparticles in the internal body is also essential to comprehend for the realization of DDS. Thus it is necessary to reveal the internal dynamics for the proper treatments and biomedical applications of nanoparticles. In the present study the plural methods with different principles such as X-ray scanning analytical microscope (XSAM), MRI and Fluorescent microscopy were applied to enable the observation of the internal diffusion of micro/nanoparticles in the (1) whole body level, (2) inner organ level and (3) tissue and intracellular level. Chemical analysis was also done by ICP-AES for organs and compared with the results of XSAM mapping.


Animals ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 226
Author(s):  
Silvio De Luca ◽  
Emanuela Zanardi ◽  
Giovanni Loris Alborali ◽  
Adriana Ianieri ◽  
Sergio Ghidini

The assessment of swine welfare requires feasible, reliable, and reasonable indicators. On-farm evaluation of pig welfare can provide valuable information to veterinarians and farmers. However, such protocols can result expensive and time-consuming. With this regard, an interest in the appraisal of swine welfare at abattoir has grown over the recent years. In particular, the use of certain lesions collected directly from slaughtered animals to determine the welfare status of pigs has been evaluated by several authors. In the present review, the different methods developed to score lesions collected directly from the body and the viscera of animals slaughtered in European abattoirs (“abattoir-based measures”) are presented. The text specifically focuses on the methods currently available in the literature for the scoring of body, pluck and gastric lesions during post-mortem activities. Moreover, the strengths and weaknesses of abattoir-based measures schemes are discussed. To conclude, the future perspectives of the assessment of pig welfare at the slaughterhouse are described, appealing for a benchmarking system that can be systematically used by veterinarians and other professional figures involved in the process.


2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Erfan Dashtimoghadam ◽  
Farahnaz Fahimipour ◽  
Andrew N. Keith ◽  
Foad Vashahi ◽  
Pavel Popryadukhin ◽  
...  

AbstractCurrent materials used in biomedical devices do not match tissue’s mechanical properties and leach various chemicals into the body. These deficiencies pose significant health risks that are further exacerbated by invasive implantation procedures. Herein, we leverage the brush-like polymer architecture to design and administer minimally invasive injectable elastomers that cure in vivo into leachable-free implants with mechanical properties matching the surrounding tissue. This strategy allows tuning curing time from minutes to hours, which empowers a broad range of biomedical applications from rapid wound sealing to time-intensive reconstructive surgery. These injectable elastomers support in vitro cell proliferation, while also demonstrating in vivo implant integrity with a mild inflammatory response and minimal fibrotic encapsulation.


Nanoscale ◽  
2021 ◽  
Author(s):  
Shagufta Haque ◽  
Sanchita Tripathy ◽  
Chitta Ranjan Patra

The present review article provides the insight of an overall survey on the recent advancements of manganese nanomaterials for biomedical nanotechnology and other fields.


2020 ◽  
Author(s):  
Erfan Dashtimoghadam ◽  
Farahnaz Fahimipour ◽  
Andrew Keith ◽  
Foad Vashahi ◽  
Pavel Popryadukhin ◽  
...  

Abstract Current materials used in biomedical devices do not match tissue’s mechanical properties and leach various chemicals into the body. These deficiencies pose significant health risks that are further exacerbated by invasive implantation procedures. Herein, we leverage the brush-like polymer architecture to design and administer minimally invasive injectable elastomers that cure in vivo into leachable-free implants with mechanical properties matching the surrounding tissue. This strategy allows tuning curing time from minutes to hours, which empowers a broad range of biomedical applications from rapid wound sealing to time-intensive reconstructive surgery. These injectable elastomers support in vitro cell proliferation, while also demonstrating in vivo implant integrity with a mild inflammatory response and minimal fibrotic encapsulation.


2016 ◽  
Vol 17 (1) ◽  
pp. 90-96 ◽  
Author(s):  
Kusai Baroudi ◽  
Rushabh Dagli ◽  
Namrata Dagli ◽  
Shrouq Darwish

ABSTRACT Background Recently, oral microbiome has gained popularity among scientists. Microorganisms are no longer considered as disease-producing pathogens, rather they are now considered as partners of human in maintaining health. Since ancient times, changes in our lifestyle have affected our microbiome and the balance with their human host has been perturbed. The present review includes the description about factors affecting oral microbiome and establishing symbiosis with the human host so that they contribute in maintaining health rather than eliciting diseases. Materials and methods A comprehensive literature search was performed on databases such as Google Scholar, PubMed and Medline until April 2015. First, articles were selected on the basis of their titles and then abstracts were screened and unwanted articles were excluded. Articles obtained from all the databases were checked and duplicate articles were removed. Articles obtained from various databases: PubMed = 35, Google Scholar = 8. Out of these 43 articles, total 29 articles were finally selected for this review. Results The published literature suggests that the modern oral microbiome is less biodiverse, and possess more pathogenic bacterial species and lesser beneficial bacteria. The possible factors mainly responsible for this shift in microbiome were found to be change in diet, industrial revolution and indiscriminate use of antibiotics. Conclusion Various changes in lifestyles have affected oral microbiome adversely and perturb the symbiosis between the microbiome and their hosts. The present oral microbiome is found to be less diverse and more pathogenic. The present review may be helpful in understanding the relationship between the microbiome and their human hosts so that microbiome contributes in maintaining healthy state of the body. How to cite this article Dagli N, Dagli R, Darwish S, Baroudi K. Oral Microbial Shift: Factors affecting the Microbiome and Prevention of Oral Disease. J Contemp Dent Pract 2016;17(1):90-96.


2020 ◽  
Vol 11 (1) ◽  
pp. 1-27
Author(s):  
Adil Hussain

Background: There exist natural antioxidants in plants that scavenge harmful free radicals from the body. Free radicals are species of chemical origin with an unpaired electron and play a pivotal role in combating against health-related problems like lung damage, inflammation, and cardiovascular ailments etc. Antioxidants halt the development of these free radicals called the reactive oxygen species either by chelating the trace elements or by enzymes inhibition. Objectives: The aim of present review was to collect information about Pakistani medicinally important plants with the exploration of their antioxidant potential. Methodology: Total 206 papers were looked over, which were obtained from numerous sources like; Google Scholar, Medline, PubMed, Research Gate, Science Direct, Scopus and Web of Science. Results: Overall, 93 plants representing 44 families with potential antioxidant activity reported from Pakistan have been presented in this review. Maximum number of species from Asteracea, Poaceae and Rutaceae familes were scrutinized for their potential antioxidant activity from Pakistan. Conclusion: The present review clearly designates that the presence of phytochemicals and antioxidant activity of medicinal plants from Pakistan vary with the species of the plants and material/extracts used. From this review, it is recommended to perform comprehensive experimental investigations based on toxicology and ethnopharmacology on these precious plants from Pakistan. It will be advantageous in the provision of trustworthy information to patients and determine further innovative compounds for safer and new drugs development with fewer side effects.


2021 ◽  
Author(s):  
Marlene Lúcio ◽  
Eduarda Fernandes ◽  
Hugo Gonçalves ◽  
Sofia Machado ◽  
Andreia C. Gomes ◽  
...  

Since its revolutionary discovery in 2004, graphene— a two-dimensional (2D) nanomaterial consisting of single-layer carbon atoms packed in a honeycomb lattice— was thoroughly discussed for a broad variety of applications including quantum physics, nanoelectronics, energy efficiency, and catalysis. Graphene and graphene-based nanomaterials (GBNs) have also captivated the interest of researchers for innovative biomedical applications since the first publication on the use of graphene as a nanocarrier for the delivery of anticancer drugs in 2008. Today, GBNs have evolved into hybrid combinations of graphene and other elements (e.g., drugs or other bioactive compounds, polymers, lipids, and nanoparticles). In the context of developing theranostic (therapeutic + diagnostic) tools, which combine multiple therapies with imaging strategies to track the distribution of therapeutic agents in the body, the multipurpose character of the GBNs hybrid systems has been further explored. Because each therapy and imaging strategy has inherent advantages and disadvantages, a mixture of complementary strategies is interesting as it will result in a synergistic theranostic effect. The flexibility of GBNs cannot be limited to their biomedical applications and, these nanosystems emerge as a viable choice for an indirect effect on health by their future use as environmental cleaners. Indeed, GBNs can be used in bioremediation approaches alone or combined with other techniques such as phytoremediation. In summary, without ignoring the difficulties that GBNs still present before being deemed translatable to clinical and environmental applications, the purpose of this chapter is to provide an overview of the remarkable potential of GBNs on health by presenting examples of their versatility as nanotools for theranostics and bioremediation.


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