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.

Ranajit Guha’s Historiography of Colonial India

2018 ◽  
Author(s):  
Vasant Kaiwar
Keyword(s):  
Latin American ◽  
Western Europe ◽  
Subaltern Studies ◽  
Latin American History ◽  
Indian History ◽  
Bengali Literature ◽  
Wide Range ◽  
The World ◽  
And Gender ◽  
The Moment

Ranajit Guha is one of the best-known and most innovative historians of modern India. The bulk of his best-known work was published between 1981 and 2002. The main historiographical issues that appear in his work include (a) the colonial appropriation of the Indian past and its representation as a “highly interesting portion of British history,” which together with the force of colonial conquest added up in Guha’s terminology to a colonial expropriation of Indian history; (b) the complicity of all branches of colonialist knowledge in the fact or force of conquest; (c) British rule in India as a “dominance without hegemony,” in which the moment of coercion outweighed the moment of persuasion by contrast with western Europe; (d) an Indian historiography of India that attempts to redress the expropriation of Indian history and make “the Indian people, constituted as a nation, the subject of their own history”; (e) a subaltern historiography that identifies the limitations of the mainstream Indian historiography of India and the need to pay attention to the “neglected dimension of subaltern autonomy in action, consciousness and culture,” the “contribution made by the people on their own”; and (f) a historiography that goes beyond “statism” to the everyday being-in-the-world of ordinary people, countering the pretensions of the “prose of world-history” with the “prose of the world.” These issues recur in various forms and combinations in Guha’s books and essays, notably the ones he contributed to Subaltern Studies, an edited series that he launched in 1982. The theoretical influences on Guha’s work are not limited to Marxism and its many offshoots. Guha used the concept of “subaltern” to signify anyone in India who did not belong to the “elite” and therefore included peasants, workers, impoverished landlords, and others whose behavior exhibited a combination of defiance and deference to the elite. It has many points of contact with Gramsci’s work. Guha drew freely on the philosophy of Hegel and Heidegger, Bengali literature, notably the works of Rabindranath Tagore, not to mention semiotics, linguistics, structuralism, and poststructuralism, the objective being not theoretical monism or purity but the mobilization of a wide range of references to shed light on history’s dark corners. The eclectic richness, if not elusiveness, of the concept of “subaltern” and Guha’s deployment of it in various forms to speak to caste, class, and gender issues has perhaps inspired its wider diffusion for rethinking the history of popular consciousness and mobilization in fields as far apart as Asian, African, and Latin American history.

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.

ALTERNATIVE ENERGY SOURCES AS A FACTOR OF THE DEVELOPMENT OF WORLD ENERGY INDUSTRY

2020 ◽  
Vol 2 (7) ◽  
pp. 158-165
Author(s):  
I. A. STRELKOVA ◽  
◽  
E. V. KHARMAKSHANOVA ◽  
Keyword(s):  
Alternative Energy ◽  
World Economy ◽  
Energy Sources ◽  
Alternative Energy Sources ◽  
World Energy ◽  
Wide Range ◽  
The World ◽  
Short And Long Term ◽  
Alternative Sources ◽  
The Moment

This article highlights the development of alternative sources of energy as capable of solving a wide range of environmental and economic problems. The main factors contributing to the transition to alternative energy sources are considered. Characteristics of the alternative energy sector at the moment is given, its place and role in the world economy is marked. Trends in the development of the industry, as well as prospects for the short and long term are analyzed. In conclusion, conclusions are drawn regarding the possibility of transition to alternative energy sources in the world economy.

Quinoline: an attractive scaffold in drug design

2021 ◽  
Vol 21 ◽  
Author(s):  
Lucas F. E. Moor ◽  
Thatyana R. A. Vasconcelos ◽  
Raisa da R. Reis ◽  
Ligia S. S. Pinto ◽  
Thamires M. da Costa
Keyword(s):  
Side Effects ◽  
Drug Design ◽  
Heterocyclic Compounds ◽  
Rational Design ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Bioactive Molecules ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range

: Quinoline and its derivatives comprise an important group of heterocyclic compounds that exhibits a wide range of pharmacological properties such as antibacterial, antiviral, anticancer, antiparasitic, anti-Alzheimer and anticholesterol. In fact, the quinoline nucleus is found in the structure of many drugs and in rational design in medicinal chemistry for the discovery of novel bioactive molecules. Persistent efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. This review highlights some discoveries on the development of quinoline-based compounds in recent years (2013-2019) focusing on their biological activities, including anticancer, antitubercular, antimalarial, anti-ZIKV, anti-DENV, anti-Leishmania and anti-Alzheimer’s disease.

Anti-neuropathic and anticonvulsant activities of various substituted triazoles analogues

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Review Article ◽  
Biological Profile ◽  
Triazole Derivatives ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Anticonvulsant Activities

Various heterocyclic compounds along their derivatives were evaluated for their biological activities as antiviral, antitumor, anticonvulsant, antibacterial, antifungal, antituberculosis, analgesic, anti-inflammatory, antidiabetic, antihistamine and other biological activities. The triazole moiety seems to be very small, but in the biological profile has attracted the attention of many researchers to explore this skeleton to its multiple potential against several activities. The triazole derivatives possess a great importance in medicinal chemistry and can be used for the synthesis of numerous heterocyclic compounds with different biological activities. This review article covers the information of triazoles derivatives having different psychopharmacological actions. Thus triazole acts as a promising medicinal agent for the scientists working over this field. This review can be helpful to develop various more new compounds possessing triazoles moiety that could be better in terms of efficacy and lesser toxicity.

Natural Products: Key Prototypes to Drug Discovery Against Neglected Diseases Caused by Trypanosomatids

2020 ◽  
Vol 27 (13) ◽  
pp. 2133-2146 ◽  
Author(s):  
Marina Themoteo Varela ◽  
João Paulo S. Fernandes
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Neglected Tropical Diseases ◽  
Biological Activities ◽  
Neglected Diseases ◽  
Synthetic Compounds ◽  
Structural Variety ◽  
The World ◽  
Leishmania Spp ◽  
Per Se

Background: Neglected tropical diseases are a group of infections caused by microorganisms and viruses that affect mainly poor regions of the world. In addition, most available drugs are associated with long periods of treatment and high toxicity which limits the application and patient compliance. Investment in research and development is not seen as an attractive deal by the pharmaceutical industry since the final product must ideally be cheap, not returning the amount invested. Natural products have always been an important source for bioactive compounds and are advantageous over synthetic compounds when considering the unique structural variety and biological activities. On the other hand, isolation difficulties and low yields, environmental impact and high cost usually limit their application as drug per se. Objective: In this review, the use of natural products as prototypes for the semi-synthesis or total synthesis, as well as natural products as promising hits is covered, specifically regarding compounds with activities against trypanosomatids such as Trypanosoma spp. and Leishmania spp. Methods: Selected reports from literature with this approach were retrieved. Conclusion: As summary, it can be concluded that natural products are an underestimated source for designing novel agents against these parasites.

Galangin: A metabolite that suppresses anti-neoplastic activities through modulation of oncogenic targets

2021 ◽  
pp. 153537022110625
Author(s):  
Hardeep Singh Tuli ◽  
Katrin Sak ◽  
Shubham Adhikary ◽  
Ginpreet Kaur ◽  
Diwakar Aggarwal ◽  
...  
Keyword(s):  
Cancer Incidence ◽  
Natural Compound ◽  
Biological Activities ◽  
Chemotherapeutic Drugs ◽  
Lead Compounds ◽  
Molecular Oncology ◽  
Wide Range ◽  
Anti Cancer ◽  
The World

With the dramatic increase in cancer incidence all over the world in the last decades, studies on identifying novel efficient anti-cancer agents have been intensified. Historically, natural products have represented one of the most important sources of new lead compounds with a wide range of biological activities. In this article, the multifaceted anti-cancer action of propolis-derived flavonoid, galangin, is presented, discussing its antioxidant, anti-inflammatory, antiproliferative, pro-apoptotic, anti-angiogenic, and anti-metastatic effects in various cancer cells. In addition, co-effects with standard chemotherapeutic drugs as well as other natural compounds are also under discussion, besides highlighting modern nanotechnological advancements for overcoming the low bioavailability issue characteristic of galangin. Although further studies are needed for confirming the anti-cancer potential of galangin in vivo malignant systems, exploring this natural compound might open new perspectives in molecular oncology.

Antidiabetic Potential of Naturally Occurring Sesquiterpenes: A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Anupam Maurya ◽  
Sweta Mohan ◽  
Subash C. Verma
Keyword(s):  
Herbal Medicine ◽  
Side Effect ◽  
Biological Activities ◽  
Blood Stream ◽  
Synthetic Drugs ◽  
Wide Range ◽  
The World ◽  
Suitable Treatment ◽  
Underlying Mechanisms ◽  
The Many

: Diabetes Mellitus (DM) is endocrine disease, which causes 3rd leading death in human; additionally, it’s one of the major key concerns over the globe. The high levels of the glucose in blood stream is as well characterized hyperglycemia, which lead to serious damage to heart, blood vessels kidney, eyes, and nerve. The best treatment of the DM is still not available; many scientists all over the world are trying hard to seek out suitable treatment of DM. Though, numerous synthetic drugs are developed for the treatment of diabetes, but their utility has been hampered because of several side effect and poor efficacy. Among the various approaches for the treatment of DM, an herbal medicine, enriched extracts and natural derived molecules are most effective. The herbal medicine and plants contain many bioactive phytochemicals such as terpenoids, alkaloids, flavonoids & phenolics etc. The plant derived molecules and their suitable structure modification have given many leads or drugs to the world which are used in the treatment of many diseases e.g. sesquiterpene; artemisinin and their derivatives artemether & artesunate as an antimalarial drug. Sesquiterpenes are available in human diet, and largely taken as components of the many folk medicines and dietary supplements. Sesquiterpenes have wide range of biological activities such as anti-cancer, anti-inflammatory, anti-nociceptive, immunomodulatory, antidiabetic and antimicrobial which make them potential targets for development of new therapeutics and their usage for medical purposes. The natural products have attracted attention of world due to their large number biological activities, high safety and less side effect. The review mainly focuses on sesquiterpenes such as β-Caryophyllene, dysidine, farnesol & eremanthin etc., a class of terpenoids that may play important role in treatment or prevention of this morbid disorder diabetes, including their underlying mechanisms for the blood glucose-lowering property.

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.

Good News: Research and Medicinal Chemists Making a Difference

ReAction! ◽  
2009 ◽  
Author(s):  
Mark A. Griep ◽  
Marjorie L. Mikasen
Keyword(s):  
Graduate School ◽  
Medicinal Chemistry ◽  
Good News ◽  
Loved One ◽  
Isaac Newton ◽  
External Evidence ◽  
The World ◽  
Making A Difference ◽  
Chemical Products ◽  
The Moment

Stories of people doing their jobs well, treating each other with respect, and trying to make the world a better place are all examples of “good news.” Such stories don’t generate many website hits, nor do they bring people into the theaters. Instead, it seems readers and movie viewers would rather have the double pleasure of learning about bad behavior and its comeuppance. Five movies in this chapter overcome this problem; they are based on true stories. The advantage of such stories is the sympathy viewers feel as they appreciate the adversities the chemist has overcome to make their celebrated findings. For instance, in the documentary Me & Isaac Newton, which explores the motivations of seven scientists, pharmaceutical chemist Gertrude Elion is warm and charming as she describes why she decided to become a chemist. When she later describes her struggles to enter graduate school and then get a job as a chemist, the viewer is struck by her matter-of-fact, water-under-the-bridge tone. This all happened before she understood there was a climate of active discrimination against women that had nothing to do with their drive or abilities. Still later, she says the ultimate reward for all her work comes when someone thanks her for having developed the drug that cured a loved one. The disadvantage of using true stories is the need to create dramatic tension. The important moments in people’s lives rarely coincide with obvious indications that “this is the moment when everything fell into place,” whereas a movie’s linear narrative has to make that point clear to the audience. Another problem for moviemakers is that most people just aren’t very curious about the origins of everyday things. This is a challenge because very few chemicals cause the imagination to soar (unless you are a chemist), which may explain why all five movies based on true stories are about medicinal chemistry, which can be seen as the external evidence of the chemist’s desire to do good things for other people. Fictional movie chemists are less likely to develop medicines. Like the chemistry professors in chapter 8, they tend to develop chemical products for more selfish reasons.

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