Designed Synthesis of Diversely Substituted Hydantoins and Hydantoin-Based Hybrid Molecules: A Personal Account

Synlett ◽  
2021 ◽  
Author(s):  
Vinod Kumar

Hydantoin and its analogs such as thiohydantoin and iminohydantoin have received substantial attention both from a chemical and biological point of view. Several compounds of this class have shown useful pharmacological activities such as anticonvulsant, antitumor, antiarrhythmic, herbicidal, and others that lead in some cases to clinical applications. Because of broad-spectrum activities, intensive research efforts have been dedicated in industry and academia to the synthesis and structural modifications of hydantoin and its derivatives. Realizing the importance of hydantoin in organic and medicinal chemistry, we also initiated a research program to successfully design and develop the new routes/methods resulting in the formation of hydantoin, thiohydantoin, and iminohydantoin substituted at different positions particularly at the N-1 position without following protection-deprotection strategy. Given the fact that the combination of two or more pharmacophoric groups may lead to hybrid molecules which result in a mixed mechanism of action on the biological target. We, therefore, further extended the developed strategy for the synthesis of new types of hydantoin-based hybrid molecules by combining hydantoin with a triazole, isoxazoline, and phosphate scaffolds as another pharmacophoric group to exploit diverse biological functions.

Author(s):  
J.D. Shelburne ◽  
G.M. Roomans

Proper preparative procedures are a prerequisite for the validity of the results of x-ray microanalysis of biological tissue. Clinical applications of x-ray microanalysis are often concerned with diagnostic problems and the results may have profound practical significance for the patient. From this point of view it is especially important that specimen preparation for clinical applications is carried out correctly.Some clinical problems require very little tissue preparation. Hair, nails, and kidney and gallbladder stones may be examined and analyzed after carbon coating. High levels of zinc or copper in hair may be indicative of dermatological or systemic diseases. Nail clippings may be analyzed (as an alternative to the more conventional sweat test) to confirm a diagnosis of cystic fibrosis. X-ray microanalysis in combination with scanning electron microscopy has been shown to be the most reliable method for the identification of the components of kidney or gallbladder stones.A quantitatively very important clinical application of x-ray microanalysis is the identification and quantification of asbestos and other exogenous particles in lung.


2021 ◽  
Vol 20 (1) ◽  
Author(s):  
Xiao-Huan Tang ◽  
Ting Guo ◽  
Xiang-Yu Gao ◽  
Xiao-Long Wu ◽  
Xiao-Fang Xing ◽  
...  

AbstractExosomes are a subpopulation of the tumour microenvironment (TME) that transmit various biological molecules to promote intercellular communication. Exosomes are derived from nearly all types of cells and exist in all body fluids. Noncoding RNAs (ncRNAs) are among the most abundant contents in exosomes, and some ncRNAs with biological functions are specifically packaged into exosomes. Recent studies have revealed that exosome-derived ncRNAs play crucial roles in the tumorigenesis, progression and drug resistance of gastric cancer (GC). In addition, regulating the expression levels of exosomal ncRNAs can promote or suppress GC progression. Moreover, the membrane structures of exosomes protect ncRNAs from degradation by enzymes and other chemical substances, significantly increasing the stability of exosomal ncRNAs. Specific hallmarks within exosomes that can be used for exosome identification, and specific contents can be used to determine their origin. Therefore, exosomal ncRNAs are suitable for use as diagnostic and prognostic biomarkers or therapeutic targets. Regulating the biogenesis of exosomes and the expression levels of exosomal ncRNAs may represent a new way to block or eradicate GC. In this review, we summarized the origins and characteristics of exosomes and analysed the association between exosomal ncRNAs and GC development.


Author(s):  
Lav Singh ◽  
Atul K. Upadhyay ◽  
Pooja Dixit ◽  
Arpit Singh ◽  
Divyanshu yadav ◽  
...  

Background: Pinus and other related conifers belonging to family pinaceae are most commonly used medicinal plants in Indian North-western Himalayas. Various parts of these plants including needles are source of several well known alkaloids. Of all the alkaloids, piperidine group is one of important component and hold considerable medicinal importance. Methods: The group of alkaloids was initially identified from genus Piper through which a large variety of piperidine molecules have been extracted. The planar structure of this heterocyclic nucleus enables acetamide groups to be added at various ring configurations. Results: In the area of drug research, the piperidine heterocycle has gained considerable interest. To produce a new therapeutic profile, the broad range of its therapeutic application paved the way for researchers to implant the nucleus from time to time in diversified pharmacophores. Discussion: However, biological functions of piperidine metabolites have been mostly examined on a limited scale and that most of the findings are thus preliminary. We have tried to present different clinical applications of piperidine alkaloids in this study that researchers have already attempted to demystify from time to time. Conclusion: Given the importance of the piperidine nucleus, the study will enable the researcher to produce scaffolds of the highest therapeutic efficacy. We have also illustrated different types of piperidine, its sources in different member of family pinaceae with special emphasis on Pinus.


Marine Drugs ◽  
2018 ◽  
Vol 16 (10) ◽  
pp. 397 ◽  
Author(s):  
Isabel Viera ◽  
Antonio Pérez-Gálvez ◽  
María Roca

The benefit of carotenoids to human health is undeniable and consequently, their use for this purpose is growing rapidly. Additionally, the nutraceutical properties of carotenoids have attracted attention of the food industry, especially in a new market area, the ‘cosmeceuticals.’ Marine organisms (microalgae, seaweeds, animals, etc.) are a rich source of carotenoids, with optimal properties for industrial production and biotechnological manipulation. Consequently, several papers have reviewed the analysis, characterization, extraction and determination methods, biological functions and industrial applications. But, now, the bioaccessibility and bioactivity of marine carotenoids has not been focused of any review, although important achievements have been published. The specific and diverse characteristic of the marine matrix determines the bioavailability of carotenoids, some of them unique in the nature. Considering the importance of the bioavailability not just from the health and nutritional point of view but also to the food and pharmaceutical industry, we consider that the present review responds to an actual demand.


Author(s):  
Luan Wen ◽  
Ting He ◽  
AXiang Yu ◽  
Siqi Sun ◽  
Xiang Li ◽  
...  

Breviscapine is one of the extracts of several flavonoids of Erigeron breviscapus. Scutellarin is the main active component of breviscapine, and the qualitative or quantitative criteria as well. Scutellarin and its analogs share a similar skeleton of the flavonoids. Breviscapine has been widely used in the treatment of cerebral infarction and its sequelae, cerebral thrombus, coronary heart disease (CHD), and angina pectoris. Breviscapine has a broad spectrum of pharmacological activities, such as increasing blood flow, improving microcirculation, dilating blood vessels, decreasing blood viscosity, promoting fibrinolysis, inhibiting platelet aggregation, and thrombosis formation, etc. In addition, breviscapine and its analogs have significant value for drug research and development because of the superiority of those significant bioactivities. Furthermore, an increasing number of pharmacokinetic studies have explored the mechanism of scutellarin and its analogs. To provide a comprehensive understanding of the current research on breviscapine, scutellarin, and the analogs, the structural features, distribution situation, preparation method, content determination method, clinical applications, pharmacological action as well as pharmacokinetics are summarized in the present review.


2018 ◽  
Vol 941 ◽  
pp. 1686-1691 ◽  
Author(s):  
Pedro Poza ◽  
Paloma Sirvent ◽  
Álvaro Rico ◽  
Claudio J. Múnez ◽  
Miguel Ángel Garrido

Ti6Al4V coatings were cold sprayed onto the same bulk alloy using standard conditions and a set of parameters developed to improve the coating’s performance. In addition, the enhanced coating was heat treated to improve coating adhesion and reduce porosity. Wear tests were performed, onto the coatings and the substrate, in oscillating conditions, which simulate wear induced by the contact with bearing parts during vibration. Wear behaviour at room temperature is dominated by a mixed mechanism, which involves plastic deformation and transference from the counterbody forming mechanically mixed layers. As temperature is increased, the formation of mechanically mixed layers dominates wear. The wear resistance of the enhanced coatings is similar to the bulk alloy, or even better in some conditions. Consequently, cold sprayed improved coatings could be used for repairing titanium components from the contact wear point of view.


2020 ◽  
Vol 71 (16) ◽  
pp. 4677-4689 ◽  
Author(s):  
Dun-Xian Tan ◽  
Russel J Reiter

Abstract Plant melatonin research is a rapidly developing field. A variety of isoforms of melatonin’s biosynthetic enzymes are present in different plants. Due to the different origins, they exhibit independent responses to the variable environmental stimuli. The locations for melatonin biosynthesis in plants are chloroplasts and mitochondria. These organelles have inherited their melatonin biosynthetic capacities from their bacterial ancestors. Under ideal conditions, chloroplasts are the main sites of melatonin biosynthesis. If the chloroplast pathway is blocked for any reason, the mitochondrial pathway will be activated for melatonin biosynthesis to maintain its production. Melatonin metabolism in plants is a less studied field; its metabolism is quite different from that of animals even though they share similar metabolites. Several new enzymes for melatonin metabolism in plants have been cloned and these enzymes are absent in animals. It seems that the 2-hydroxymelatonin is a major metabolite of melatonin in plants and its level is ~400-fold higher than that of melatonin. In the current article, from an evolutionary point of view, we update the information on plant melatonin biosynthesis and metabolism. This review will help the reader to understand the complexity of these processes and promote research enthusiasm in these fields.


2020 ◽  
Vol 2020 ◽  
pp. 1-14 ◽  
Author(s):  
Rabia Shabir Ahmad ◽  
Muhammad Bilal Hussain ◽  
Muhammad Tauseef Sultan ◽  
Muhammad Sajid Arshad ◽  
Marwa Waheed ◽  
...  

Turmeric (Curcuma longa L.) is a popular natural drug, traditionally used for the treatment of a wide range of diseases. Its root, as its most popular part used for medicinal purposes, contains different types of phytochemicals and minerals. This review summarizes what is currently known on biochemistry, safety, pharmacological activities (mechanistically), and clinical applications of turmeric. In short, curcumin is considered as the fundamental constituent in ground turmeric rhizome. Turmeric possesses several biological activities including anti-inflammatory, antioxidant, anticancer, antimutagenic, antimicrobial, antiobesity, hypolipidemic, cardioprotective, and neuroprotective effects. These reported pharmacologic activities make turmeric an important option for further clinical research. Also, there is a discussion on its safety and toxicity.


2020 ◽  
Vol 11 ◽  
Author(s):  
Feng Zhao ◽  
Ping Wang ◽  
Yuanyuan Jiao ◽  
Xiaoxiao Zhang ◽  
Daquan Chen ◽  
...  

Hydroxysafflower yellow A (HSYA), as a principal natural ingredient extracted from safflower (Carthamus tinctorius L.), has significant pharmacological activities, such as antioxidant, anti-inflammatory, anticoagulant, and anticancer effects. However, chemical instability and low bioavailability have been severely hampering the clinical applications of HSYA during the treatment of cardiovascular and cerebrovascular disease. Therefore, this present review systematically summarized the materials about HSYA, including acquisition methods, extraction and detection methods, pharmacokinetics, pharmacological effects and molecular mechanism, especially focus on the possible causes and resolutions about the chemical instability and low bioavailability of HSYA, in order to provide relatively comprehensive basic data for the related research of HSYA.


Sign in / Sign up

Export Citation Format

Share Document