scholarly journals An Overview of Coumarin as a Versatile and Readily Accessible Scaffold with Broad-Ranging Biological Activities

2020 ◽  
Vol 21 (13) ◽  
pp. 4618 ◽  
Author(s):  
Francesca Annunziata ◽  
Cecilia Pinna ◽  
Sabrina Dallavalle ◽  
Lucia Tamborini ◽  
Andrea Pinto
Keyword(s):  
Scientific Community ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Natural Compounds ◽  
Natural Sources ◽  
Wide Range ◽  
Living Organisms ◽  
Privileged Structures ◽  
Synthetic Approaches ◽  
Critical Overview

Privileged structures have been widely used as an effective template for the research and discovery of high value chemicals. Coumarin is a simple scaffold widespread in Nature and it can be found in a considerable number of plants as well as in some fungi and bacteria. In the last years, these natural compounds have been gaining an increasing attention from the scientific community for their wide range of biological activities, mainly due to their ability to interact with diverse enzymes and receptors in living organisms. In addition, coumarin nucleus has proved to be easily synthetized and decorated, giving the possibility of designing new coumarin-based compounds and investigating their potential in the treatment of various diseases. The versatility of coumarin scaffold finds applications not only in medicinal chemistry but also in the agrochemical field as well as in the cosmetic and fragrances industry. This review is intended to be a critical overview on coumarins, comprehensive of natural sources, metabolites, biological evaluations and synthetic approaches.

An Overview on Glyco-Macrocycles: Potential New Lead and their Future in Medicinal Chemistry

2020 ◽  
Vol 27 (20) ◽  
pp. 3386-3410
Author(s):  
Kartikey Singh ◽  
Rama Pati Tripathi
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry ◽  
Potential Role ◽  
Biological Activities ◽  
Natural Sources ◽  
Small Segment ◽  
Drug Candidates ◽  
Wide Range ◽  
Vast Range ◽  
Chiral Macrocycles

Macrocycles cover a small segment of molecules with a vast range of biological activity in the chemotherapeutic world. Primarily, the natural sources derived from macrocyclic drug candidates with a wide range of biological activities are known. Further evolutions of the medicinal chemistry towards macrocycle-based chemotherapeutics involve the functionalization of the natural product by hemisynthesis. More recently, macrocycles based on carbohydrates have evolved a considerable interest among the medicinal chemists worldwide. Carbohydrates provide an ideal scaffold to generate chiral macrocycles with well-defined pharmacophores in a decorated fashion to achieve the desired biological activity. We have given an overview on carbohydrate-derived macrocycle involving their synthesis in drug design and discovery and potential role in medicinal chemistry.

Potential Triazole-based Molecules for the Treatment of Neglected Diseases

2019 ◽  
Vol 26 (23) ◽  
pp. 4403-4434 ◽  
Author(s):  
Susimaire Pedersoli Mantoani ◽  
Peterson de Andrade ◽  
Talita Perez Cantuaria Chierrito ◽  
Andreza Silva Figueredo ◽  
Ivone Carvalho
Keyword(s):  
Effective Treatment ◽  
Chagas Disease ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Neglected Diseases ◽  
Triazole Derivatives ◽  
Wide Range ◽  
The World ◽  
Great Relevance ◽  
The Moment

Neglected Diseases (NDs) affect million of people, especially the poorest population around the world. Several efforts to an effective treatment have proved insufficient at the moment. In this context, triazole derivatives have shown great relevance in medicinal chemistry due to a wide range of biological activities. This review aims to describe some of the most relevant and recent research focused on 1,2,3- and 1,2,4-triazolebased molecules targeting four expressive NDs: Chagas disease, Malaria, Tuberculosis and Leishmaniasis.

Heterocycle Compounds with Antimicrobial Activity

2020 ◽  
Vol 26 (8) ◽  
pp. 867-904 ◽  
Author(s):  
Maria Fesatidou ◽  
Anthi Petrou ◽  
Geronikaki Athina
Keyword(s):  
Heterocyclic Compounds ◽  
Bacterial Infections ◽  
Scientific Community ◽  
Antimicrobial Agents ◽  
Fungal Infections ◽  
Biological Activities ◽  
Literature Survey ◽  
New Findings ◽  
Wide Range ◽  
Number Of Microorganisms

Background: Bacterial infections are a growing problem worldwide causing morbidity and mortality mainly in developing countries. Moreover, the increased number of microorganisms, developing multiple resistances to known drugs, due to abuse of antibiotics, is another serious problem. This problem becomes more serious for immunocompromised patients and those who are often disposed to opportunistic fungal infections. Objective: The objective of this manuscript is to give an overview of new findings in the field of antimicrobial agents among five-membered heterocyclic compounds. These heterocyclic compounds especially five-membered attracted the interest of the scientific community not only for their occurrence in nature but also due to their wide range of biological activities. Method: To reach our goal, a literature survey that covers the last decade was performed. Results: As a result, recent data on the biological activity of thiazole, thiazolidinone, benzothiazole and thiadiazole derivatives are mentioned. Conclusion: It should be mentioned that despite the progress in the development of new antimicrobial agents, there is still room for new findings. Thus, research still continues.

scholarly journals A IMPORTÂNCIA DAS CUMARINAS PARA A QUÍMICA MEDICINAL E O DESENVOLVIMENTO DE COMPOSTOS BIOATIVOS NOS ÚLTIMOS ANOS

Química Nova ◽  
2020 ◽  
Author(s):  
Daiana Franco ◽  
Thiago Pereira ◽  
Felipe Vitorio ◽  
Nathalia Nadur ◽  
Renata Lacerda ◽  
...  
Keyword(s):  
Chemical Space ◽  
Biological Activities ◽  
Research Projects ◽  
Wide Range ◽  
Non Covalent Interactions ◽  
Iupac Nomenclature ◽  
Living Organisms ◽  
Coumarin Compounds ◽  
New Treatments ◽  
Covalent Interactions

Coumarins are natural products characterized as 2H-chromen-2-one, according to IUPAC nomenclature, largely distributed in plants, as well as, in species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert non-covalent interactions with many enzymes an receptors in living organisms lead the coumarins to exhibit a wide range of biological activities and applications. Then, this manuscript provides an overview of the use of coumarin compounds in medicinal chemistry in treating many diseases. Important examples of the last years have been selected concerning the activities of coumarins as anticoagulant, anticancer, antioxidant, antiviral, antidiabetics, anti-inflammatory, antibacterial, antifungal, and anti-neurodegenerative agents. Thus, this work aims at contributing to the development of new rational research projects searching for new treatments and bioactive compounds for many pathologies using coumarin derivatives.

Identification of promising objects for the synthesis of thiosulphonate derivatives of benzoquinone and hydroquinone

2021 ◽  
Vol 4 (2) ◽  
pp. 47-53
Author(s):  
N. Y. Monka ◽  
◽  
N. E. Stadnytska ◽  
I. R. Buchkevych ◽  
K. O. Kaplia ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Experimental Studies ◽  
New Drugs ◽  
Reduced Form ◽  
Free Form ◽  
Wide Range ◽  
On Line ◽  
Living Organisms ◽  
Derivatives Of

Benzoquinone and its reduced form hydroquinone belong to phenolic compounds and are found in living organisms in free form or in glycosides. They are active substances of some medicinal plants and have a pharmacological effect on the human body. Accordingly, their derivatives are important objects for chemical synthesis and development of new drugs. This article presents the findings of the structural design of substances with benzoquinone or hydroquinone fragment and sulfur-containing compound. By use of appropriate on-line programs a predictive screening of the biological activity and cytotoxicity of thiosulfonate derivatives of benzoquinone and hydroquinone has been conducted. It has been found that they have immense methodological potential to be synthesized by substances with a wide range of biological activities and a high value of probable activity, which substantiates the feasibility of conducting experimental studies on their biological activity, particularly anticancer.

scholarly journals Recent Developments in the Synthesis of Pyrido[1,2-a]benzimidazoles

Synthesis ◽  
2018 ◽  
Vol 50 (11) ◽  
pp. 2131-2149 ◽  
Author(s):  
Kamal Kapoor ◽  
Parthasarathi Das ◽  
Rajni Khajuria ◽  
Sk. Rasheed ◽  
Chhavi Khajuria
Keyword(s):  
Transition Metal ◽  
Medicinal Chemistry ◽  
Type I ◽  
Type Ii ◽  
Aromatic Rings ◽  
Metal Free ◽  
Wide Range ◽  
Recent Developments ◽  
Metal Catalyzed ◽  
Synthetic Approaches

Pyrido[1,2-a]benzimidazole is one of the most important azaheterocyclic compounds consisting of three fused aromatic rings. Molecules containing this core have displayed a wide range of applications in the field of medicinal chemistry. The synthesis of pyrido[1,2-a]benzimidazole and its derivatives has attracted organic chemists because of its tremendous utility in interdisciplinary branches of chemistry. In this context, this review discusses the main advances in the synthesis of pyrido[1,2-a]benzimidazoles via metal-mediated and metal-free reactions from 2000 to 2016.1 Introduction2 Synthetic Approaches to Pyrido[1,2-a]benzimidazoles2.1 Type I: Transition-Metal-Catalyzed Methods2.2 Type II: Metal-Free Approaches3 Conclusion

scholarly journals Synthesis of 3-Amino-4-Substituted Monocyclic ß-Lactams—Important Structural Motifs in Medicinal Chemistry

2021 ◽  
Vol 23 (1) ◽  
pp. 360
Author(s):  
Katarina Grabrijan ◽  
Nika Strašek ◽  
Stanislav Gobec
Keyword(s):  
Important Determinant ◽  
Biological Activities ◽  
Cholesterol Absorption ◽  
Pharmacological Activities ◽  
Cerium Ammonium Nitrate ◽  
Wide Range ◽  
Cerium Ammonium ◽  
Ring Nitrogen ◽  
Inhibitory Activities ◽  
Synthetic Approaches

Monocyclic ß-lactams (azetidin-2-ones) exhibit a wide range of biological activities, the most important of which are antibacterial, anticancer, and cholesterol absorption inhibitory activities. The synthesis of decorated monocyclic ß-lactams is challenging because their ring is highly constrained and consequently reactive, which is also an important determinant of their biological activity. We present the optimized synthesis of orthogonally protected 3-amino-4-substituted monocyclic ß-lactams. Among several possible synthetic approaches, Staudinger cycloaddition proved to be the most promising method for initial ring formation, yielding monocyclic ß-lactams with different substituents at the C-4 position, a phthalimido-protected 3-amino group, and a (dimethoxy)benzyl protected ring nitrogen. Challenging deprotection methods were then investigated. Oxidative cleavage with cerium ammonium nitrate and ammonia-free Birch reduction was found to be most effective for selective removal of ring nitrogen protection. Hydrazine hydrate was used for deprotection of the phthalimido group, and the procedure had to be modified by the addition of HCl in the case of aromatic substituents at the C-4 position. The presented methods and the synthesized 3-amino-4-substituted monocyclic ß-lactam derivatives are an important step toward new ß-lactams with potential pharmacological activities.

scholarly journals NATURAL ANTIVIRALS FOR THE MANAGEMENT OF SARS-COVID-19: A REVIEW

2021 ◽  
Vol 12 (3) ◽  
pp. 113-117
Author(s):  
Vasavi M ◽  
Pujitha M ◽  
Raagini G ◽  
Ramaiah M ◽  
Ramalingeswara Rao K
Keyword(s):  
Side Effects ◽  
Natural Compounds ◽  
New Disease ◽  
Viral Pathogens ◽  
Health Crisis ◽  
Natural Sources ◽  
Significant Challenge ◽  
Wide Range ◽  
History Of ◽  
Antiviral Activities

Unlike previous outbreaks like SARS and MERS, caused by corona family viruses, COVID-19 became a much worse worldwide pandemic. SARS CoV-2, another coronavirus, causes it. Finding effective therapeutics against this global health crisis became a significant challenge for researchers. However, Allopathic medicine is effective to some extent with severe side effects, which cause concern. In this process, some researchers focused on natural compounds like plant-synthesized secondary metabolites (PSMs) for the treatment of COVID-19. Because these natural compounds like PSMs had a history of tackling a wide range of viral pathogens successfully without significant side effects. Many medicinal plants from different families have antiviral activities. This review intends to systematically evaluate the natural metabolites that could be used against this new disease looking at their natural sources, mechanism of action, and previous pharmacological usages. So, it can be a good initiation for the greater goal of finding effective natural therapeutics for the treatment of Covid-19 without any severe side effects.

scholarly journals Synthesis of Novel 2-(Pyridin-2-yl) Pyrimidine Derivatives and Study of Their Anti-Fibrosis Activity

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5226
Author(s):  
Yi-Fei Gu ◽  
Yue Zhang ◽  
Feng-li Yue ◽  
Shao-tong Li ◽  
Zhuo-qi Zhang ◽  
...  
Keyword(s):  
Biological Activities ◽  
Collagen Type I ◽  
Type I ◽  
The Novel ◽  
Pyrimidine Derivatives ◽  
Wide Range ◽  
Ic50 Values ◽  
Privileged Structures ◽  
Pyrimidine Moiety

A pyrimidine moiety exhibiting a wide range of pharmacological activities has been employed in the design of privileged structures in medicinal chemistry. To prepare libraries of novel heterocyclic compounds with potential biological activities, a series of novel 2-(pyridin-2-yl) pyrimidine derivatives were designed, synthesized and their biological activities were evaluated against immortalized rat hepatic stellate cells (HSC-T6). Fourteen compounds were found to present better anti-fibrotic activities than Pirfenidone and Bipy55′DC. Among them, compounds ethyl 6-(5-(p-tolylcarbamoyl)pyrimidin-2-yl)nicotinate (12m) and ethyl 6-(5-((3,4-difluorophenyl)carbamoyl)pyrimidin-2-yl)nicotinate (12q) show the best activities with IC50 values of 45.69 μM and 45.81 μM, respectively. Furthermore, the study of anti-fibrosis activity was evaluated by Picro-Sirius red staining, hydroxyproline assay and ELISA detection of Collagen type I alpha 1 (COL1A1) protein expression. Our study showed that compounds 12m and 12q effectively inhibited the expression of collagen, and the content of hydroxyproline in cell culture medium in vitro, indicating that compounds 12m and 12q might be developed the novel anti-fibrotic drugs.

Coumarin Compounds in Medicinal Chemistry: Some Important Examples from the Last Years

2018 ◽  
Vol 18 (2) ◽  
pp. 124-148 ◽  
Author(s):  
Thiago Moreira Pereira ◽  
Daiana Portella Franco ◽  
Felipe Vitorio ◽  
Arthur Eugen Kummerle
Keyword(s):  
Medicinal Chemistry ◽  
Chemical Space ◽  
Noncovalent Interactions ◽  
Biological Activities ◽  
Fluorescent Sensors ◽  
Coumarin Derivatives ◽  
Research Projects ◽  
Wide Range ◽  
Coumarin Compounds ◽  
Treatment And Diagnosis

Coumarins are natural products characterized as 1,2 benzopyrones widely distributed in plants, as well as, in many species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert noncovalent interactions with many enzymes and receptors in live organisms lead the coumarins to exhibit a wide range of biological activities and applications. Then, this manuscript provides an overview of the use of coumarins compounds in medicinal chemistry in treating many diseases. Important examples of the last years have been selected concerning the activities of coumarins as anticoagulant, anticancer, antioxidant, antiviral, anti-diabetics, anti-inflammatory, antibacterial, antifungal and anti-neurodegerative agents. Additionally, it also includes applications of coumarins as fluorescent sensors for biological systems. Thus, this work aims to contribute to the development of new rational research projects for the treatment and diagnosis of pathologies using coumarin derivatives.

Sign in / Sign up

Export Citation Format

Share Document