scholarly journals Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery

2021 ◽  
Vol 14 (12) ◽  
pp. 1275
Author(s):  
Tony Ge ◽  
Jean-Christophe Cintrat
Keyword(s):  
Drug Discovery ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Building Blocks ◽  
Biological Properties ◽  
Extensive Review ◽  
Complex Molecules ◽  
New Chemical Entities ◽  
Amino Derivatives

Heterocyclic amino derivatives have been extensively synthesized and validated as potent bioactive compounds, and nowadays, numerous marketed drugs share these scaffolds, from very simple structures (monoamino, monocyclic compounds) to much more complex molecules (polycyclic derivatives with two or more nitrogen atoms within the (fused) rings). In a constant quest for new chemical entities in drug discovery, a few novel heterocycles have emerged in recent years as promising building blocks for the obtainment of bioactive modulators. In this context, pyrrolotriazinones have attracted attention, and some show promising biological activities. Here, we offer an extensive review of pyrrolo[2,1-f][1,2,4]triazin-4(1H)-one and pyrrolo[1,2-d][1,2,4]triazin-4(3H)-one, describing their biological properties en route to drug discovery.

scholarly journals Exploitation of Agro-Industrial Waste as Potential Source of Bioactive Compounds for Aquaculture

Foods ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 843
Author(s):  
Nayely Leyva-López ◽  
Cynthia E. Lizárraga-Velázquez ◽  
Crisantema Hernández ◽  
Erika Y. Sánchez-Gutiérrez
Keyword(s):  
Bioactive Compounds ◽  
Industrial Waste ◽  
Biological Activities ◽  
Biological Effects ◽  
Food Additives ◽  
Well Being ◽  
Biological Properties ◽  
Industrial Wastes ◽  
Added Value ◽  
Bodies Of Water

The agroindustry generates a large amount of waste. In postharvest, food losses can reach up to 50%. This waste represents a source of contamination of soil, air, and bodies of water. This represents a problem for the environment as well as for public health. However, this waste is an important source of bioactive compounds, such as phenolic compounds, terpenes, and β-glucans, among others. Several biological activities have been attributed to these compounds; for example, antioxidant, antimicrobial, gut microbiota, and immune system modulators. These properties have been associated with improvements in health. Recently, the approach of using these bioactive compounds as food additives for aquaculture have been addressed, where it is sought that organisms, in addition to growing, preserve their health and become disease resistant. The exploitation of agro-industrial waste as a source of bioactive compounds for aquaculture has a triple objective—to provide added value to production chains, reduce pollution, and improve the well-being of organisms through nutrition. However, to make use of the waste, it is necessary to revalue them, mainly by determining their biological effects in aquaculture organisms. The composition of bioactive compounds of agro-industrial wastes, their biological properties, and their application in aquaculture will be addressed here.

scholarly journals Characterization of Andean Blueberry in Bioactive Compounds, Evaluation of Biological Properties and in vitro Bioaccessibility

2020 ◽  
Author(s):  
Nieves Baenas ◽  
Jenny Ruales ◽  
Diego A. Moreno ◽  
Daniel Alejandro Barrio ◽  
Carla M. Stinco ◽  
...  
Keyword(s):  
Antioxidant Capacity ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
In Vitro Digestion ◽  
Biological Properties ◽  
Wide Range ◽  
Zebrafish Embryogenesis

Andean blueberries are wild berries grown and consumed in Ecuador which contain high values of bioactive compounds, mainly anthocyanins, with powerful antioxidant activity. The aim of this study was to evaluate the profile and contents of (poly)phenols and carotenoids in Andean blueberry by HPLC-DAD-MSn and determine a wide range of its biological activities. The antioxidant capacity of this fruit was evaluated in vitro by three different methods and in vivo using the zebrafish animal model, also the toxicity effect was determined by the zebrafish embryogenesis test. Besides, the antimicrobial activity and the capacity of Andean blueberry to produce hemagglutination in blood cells were evaluated. Finally, the bioaccessibility of (poly)phenols and related antioxidant capacity were determined in the different phases of an in vitro digestion. The global results indicated no toxicity of Andean blueberry, weakly bacteriostatic activity, and high contents of anthocyanins and antioxidant capacity, which were partially bioaccesible in vitro (~ 50 % at the final intestinal step), contributing to the knowledge of its health benefits for consumers and its potential use in the food and pharmaceutical industry as functional ingredient.

scholarly journals Drug Discovery Inspired by Mother Nature: Seeking Natural Biochemotypes and the Natural Assembly Rules of the Biochemome

2013 ◽  
Vol 16 (2) ◽  
pp. 331 ◽  
Author(s):  
Qiong Gu ◽  
Xin Yan ◽  
Jun Xu
Keyword(s):  
Drug Discovery ◽  
Periodic Table ◽  
Drug Targets ◽  
Biological Activities ◽  
Building Blocks ◽  
Genome Project ◽  
New Paradigm ◽  
Chemical Library ◽  
Chemical Structures ◽  
Natural Building

Purpose. The Human Genome Project is producing a new biological ‘periodic table’, which defines all genes for making macromolecules (proteins, DNA, RNA, etc) and the relations between genes and their biological functions. We now need to consider whether to initiate a biochemome project aimed at discovering biochemistry’s ‘periodic table’, which would define all molecular parts for making small molecules (natural products) and the relations between the parts and their functions to regulate genes. By understanding the Biochemome, we might be able to design biofunctional molecules based upon a set of molecular parts for drug innovation. Methods. A number of algorithms for processing chemical structures are used to systematically derive chemoyls (natural building blocks) from a database of compounds identified in Traditional Chinese Medicine (TCM). The rules to combine chemoyls for biological activities are then deduced by mining an annotated TCM structure-activity database (ATCMD). Based upon the rules and the basic chemoyls, a chemical library can be biochemically profiled, virtual synthetic routes can be planned, and lead compounds can be identified for a specific drug target. Conclusions. The Biochemome is the complete set of molecular components (chemoyls) in an organism and Biochemomics studies the rules governing their assembly and their evolution, together with the relations between the Biochemome and drug targets. This approach provides a new paradigm for drug discovery that is based on a comprehensive knowledge of the synthetic origins of biochemical diversity, and helps to direct biomimetic syntheses aimed at assembling quasi-natural product libraries for drug screening.   This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals A review on phytoconstituents of marine brown algae

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Masuma M. Hakim ◽  
Illa C. Patel
Keyword(s):  
Bioactive Compounds ◽  
Brown Algae ◽  
Marine Algae ◽  
Biological Activities ◽  
Bioactive Compound ◽  
Biological Properties ◽  
Main Body ◽  
Marine Brown Algae ◽  
Hard State ◽  
Gujarat Coast

Abstract Background From the last few years, the development and discovery of bioactive compounds and their potential properties from marine algae have been enhanced significantly. The coastal area is a huge storehouse for propitious algae. It has been the genuine reality that the consequence of marine algae as a source of different compounds is increasing. Main body Numerous advanced research devices are available for the discovery of synthetic compounds but still many researchers are working on natural bioactive compounds to discover their biological properties, which are useful to society. Marine algae are taking the preponderance of consideration from investigators owing to its phenomenon of biological activity like anti-cancer, anti-viral, cholesterol-reducing, and many more. A variety of compounds are collected from algae with specific purposes as they remain in an extremely ambitious and hard state; this condition is responsible for the synthesis of very particularly effective bioactive compounds. The present article is concentrating on the brown algae of the Gujarat coast, phlorotannins, polyphenol, phytosterol from brown algae, and their various applications. The main importance has been given to the secondary metabolites and various applications of marine brown algae. Conclusion From this review, it can be concluded that the prominent bioactive compounds from brown algae can cure many serious diseases. Besides, the potential biological activities of a special bioactive compound may represent the interest in the industry of pharmaceuticals, cosmeceutical, and functional foods.

Advances on Monosaccharides and Oligosaccharides: Structural Modifications and Bioactivities

2021 ◽  
Vol 21 ◽  
Author(s):  
Shaochen Li ◽  
Min Lv ◽  
Shaoyong Zhang ◽  
Hui Xu
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Biological Activities ◽  
Building Blocks ◽  
Biological Properties ◽  
Mechanisms Of Action ◽  
Biological Processes ◽  
Structural Modifications ◽  
Structure Activity ◽  
Derivatives Of

: Derivatives of monosaccharides and oligosaccharides play the important roles in biological processes. Monosaccharides are the single carbohydrate building blocks, such as glucose, xylose, and fructose. Oligosaccharides are composed of 2–10 monosaccharides including disaccharides and trisaccharides. Moreover, monosaccharides, oligosaccharides and their derivatives are vital molecules with various biological properties including anticancer activity, antiviral activity, insecticidal activity, antimicrobial activity, and antioxidant activity. This review covers a survey of structural modifications, biological activities, and mechanisms of action of monosaccharides, oligosaccharides and their derivatives. Additionally, their structure–activity relationships are also concluded.

scholarly journals Z-Selective Hydrofunctionalization of Dienes

2019 ◽  
Vol 2 (2) ◽  
pp. 77-78
Author(s):  
Clara Vicera ◽  
Raphael Dada ◽  
Rylan J. Lundgren
Keyword(s):  
Functional Groups ◽  
Internal Standard ◽  
Building Blocks ◽  
Biological Properties ◽  
Inert Atmosphere ◽  
Complex Molecules ◽  
Glucagon Receptor ◽  
Olefin Synthesis ◽  
Glucagon Receptor Antagonist ◽  
Treatment Of Diabetes

Olefins play a fundamental role in synthetic organic chemistry because they are useful building blocks that create molecules. However, geometry control (E- vs Z-) in olefin synthesis is of utmost importance because the olefin geometry has a tremendous impact on its physical, chemical and biological properties. Additionally, Z-olefins are less stable compared to their E-olefin counterparts; due to this difference, general methods to make olefins results in more cases of E-olefins production with relatively fewer Z-olefins caused by its instability. It has been reported that Z-olefins can be synthesized from dienes through a rhodium-catalyzed formate mediated transformation, with tolerance to several reducible functional groups.  With this successful method in hand, the focus is to make functionalized Z-alkenes while still maintaining tolerance to reducible functional groups under mild reaction conditions. Thus, this project presents the production of Z-olefins through rhodium-catalyzed hydrofunctionalization using the starting materials, dienes and aldehydes. This method requires an inert atmosphere and the reaction progress can be monitored by Nuclear Magnetic Resonance (NMR) using an internal standard to quantify the amount of product formed. In this process, it was observed that the starting material was consumed until more than 95% conversion. In addition, the possibility of using different dienes, such as diene esters and phenyl dienes, as well as different aldehydes could further broaden the scope of this method. The usefulness of this process can be applied to the production of complex molecules. For example, in the synthesis of a glucagon receptor antagonist, which is a drug that is used in the treatment of diabetes. Currently, there is a limited number of methods used to create Z-olefins; however, this proven procedure can be further applied in other hydrofunctionalization

scholarly journals Bioactive Phytochemical Constituents of Wild Edible Mushrooms from Southeast Asia

Molecules ◽  
2020 ◽  
Vol 25 (8) ◽  
pp. 1972 ◽  
Author(s):  
Zaw Min Thu ◽  
Ko Ko Myo ◽  
Hnin Thanda Aung ◽  
Marco Clericuzio ◽  
Chabaco Armijos ◽  
...  
Keyword(s):  
Southeast Asia ◽  
Bioactive Compounds ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Biological Effects ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Edible Mushrooms ◽  
Wild Edible Mushrooms ◽  
Phytochemical Constituents

Mushrooms have a long history of uses for their medicinal and nutritional properties. They have been consumed by people for thousands of years. Edible mushrooms are collected in the wild or cultivated worldwide. Recently, mushroom extracts and their secondary metabolites have acquired considerable attention due to their biological effects, which include antioxidant, antimicrobial, anti-cancer, anti-inflammatory, anti-obesity, and immunomodulatory activities. Thus, in addition to phytochemists, nutritionists and consumers are now deeply interested in the phytochemical constituents of mushrooms, which provide beneficial effects to humans in terms of health promotion and reduction of disease-related risks. In recent years, scientific reports on the nutritional, phytochemical and pharmacological properties of mushroom have been overwhelming. However, the bioactive compounds and biological properties of wild edible mushrooms growing in Southeast Asian countries have been rarely described. In this review, the bioactive compounds isolated from 25 selected wild edible mushrooms growing in Southeast Asia have been reviewed, together with their biological activities. Phytoconstituents with antioxidant and antimicrobial activities have been highlighted. Several evidences indicate that mushrooms are good sources for natural antioxidants and antimicrobial agents

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Industrial Chemical ◽  
Anti Inflammatory ◽  
Pyridazinone Derivatives

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.

Tamarix articulata (T. articulata) - An Important Halophytic Medicinal Plant with Potential Pharmacological Properties

2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah
Keyword(s):  
Medicinal Plant ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
In Vivo Model ◽  
Drug Candidate ◽  
Phytochemical Analysis ◽  
Pharmacological Properties

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.

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