The Potential of Biologically Active Brazilian Plant Species as a Strategy to Search for Molecular Models for Mosquito Control

Planta Medica ◽  
2020 ◽  
Author(s):  
Marilia Valli ◽  
Letícia Cristina Vieira Atanázio ◽  
Gustavo Claro Monteiro ◽  
Roberta Ramos Coelho ◽  
Daniel Pecoraro Demarque ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Vector Control ◽  
Plant Species ◽  
Mosquito Control ◽  
Biologically Active ◽  
Molecular Models ◽  
Public Health Importance ◽  
Active Compounds ◽  
Brazilian Biodiversity

AbstractNatural products are a valuable source of biologically active compounds and continue to play an important role in modern drug discovery due to their great structural diversity and unique biological properties. Brazilian biodiversity is one of the most extensive in the world and could be an effective source of new chemical entities for drug discovery. Mosquitoes are vectors for the transmission of dengue, Zika, chikungunya, yellow fever, and many other diseases of public health importance. These diseases have a major impact on tropical and subtropical countries, and their incidence has increased dramatically in recent decades, reaching billions of people at risk worldwide. The prevention of these diseases is mainly through vector control, which is becoming more difficult because of the emergence of resistant mosquito populations to the chemical insecticides. Strategies to provide efficient and safe vector control are needed, and secondary metabolites from plant species from the Brazilian biodiversity, especially Cerrado, that are biologically active for mosquito control are herein highlighted. Also, this is a literature revision of targets as insights to promote advances in the task of developing active compounds for vector control. In view of the expansion and occurrence of arboviruses diseases worldwide, scientific reviews on bioactive natural products are important to provide molecular models for vector control and contribute with effective measures to reduce their incidence.

Natural products from Brazilian biodiversity as a source of new models for medicinal chemistry

2012 ◽  
Vol 84 (9) ◽  
pp. 1837-1846 ◽  
Author(s):  
Vanderlan da Silva Bolzani ◽  
Marilia Valli ◽  
Marcos Pivatto ◽  
Cláudio Viegas
Keyword(s):  
Natural Products ◽  
Combinatorial Chemistry ◽  
Medicinal Chemistry ◽  
Therapeutic Agents ◽  
Molecular Structures ◽  
Biologically Active ◽  
Ache Inhibitors ◽  
Tropical Environments ◽  
Modern Drug ◽  
Brazilian Biodiversity

Natural products are the inspiration for many valuable therapeutic agents and attest to biodiversity being a rich source of new molecular structures. Their value as templates for medicinal chemistry remains undisputed, even after the growth of the combinatorial chemistry era. Tropical environments, such as Brazilian biomes, offer a particularly rich potential for biologically active compounds with unique structures and continue to contribute toward modern drug discovery. Our bioprospecting of plant species of the Cerrado and Atlantic Forest biomes has yielded promising bioactive secondary metabolites, and we describe some of these molecules and semisynthetic derivatives as potential acetylcholinesterase (AChE) inhibitors.

scholarly journals Ecopharmacognosy: Exploring The Chemical And Biological Potential Of Nature For Human Health

2014 ◽  
Vol 3 (1) ◽  
pp. 1 ◽  
Author(s):  
Geoffrey A. Cordell
Keyword(s):  
Health Care ◽  
Natural Products ◽  
Drug Discovery ◽  
Natural Product ◽  
Developed Countries ◽  
Biologically Active ◽  
Minor Role ◽  
Natural Product Research ◽  
Biological Potential ◽  
The World

“Why didn’t they develop natural product drugs in a sustainable manner at the beginning of this century?”  In 2035, when about 10.0 billion will inhabit Earth, will this be our legacy as the world contemplates the costs and availability of synthetic and gene-based products for primary health care?  Acknowledging the recent history of the relationship between humankind and the Earth, it is essential that the health care issues being left for our descendants be considered in terms of resources. For most people in the world, there are two vast health care “gaps”, access to quality drugs and the development of drugs for major global and local diseases.  Consequently for all of these people, plants, in their various forms, remain a primary source of health care.  In the developed countries, natural products derived from plants assume a relatively minor role in health care, as prescription and over-the-counter products, even with the widespread use of phytotherapeutical preparations.  Significantly, pharmaceutical companies have retrenched substantially in their disease areas of focus.  These research areas do not include the prevalent diseases of the middle- and lower-income countries, and important diseases of the developed world, such as drug resistance. What then is the vision for natural product research to maintain the choices of drug discovery and pharmaceutical development for future generations?  In this discussion some facets of how natural products must be involved globally, in a sustainable manner, for improving health care will be examined within the framework of the new term “ecopharmacognosy”, which invokes sustainability as the basis for research on biologically active natural products.  Access to the biome, the acquisition, analysis and dissemination of plant knowledge, natural product structure diversification, biotechnology development, strategies for natural product drug discovery, and aspects of multitarget therapy and synergy research will be discussed.  Options for the future will be presented which may be significant as countries decide how to develop approaches to relieve their own disease burden, and the needs of their population for improved access to medicinal agents.

Accessing Polycyclic Terpenoids from Zerumbone via Lewis Acid Catalyzed Synthetic Strategies

Synthesis ◽  
2020 ◽  
Vol 52 (14) ◽  
pp. 2045-2064 ◽  
Author(s):  
Puthiyaparambath Sharathna ◽  
Murugan Thulasi Meenu ◽  
Kokkuvayil Vasu Radhakrishnan ◽  
Bhandara Purayil Dhanya ◽  
Greeshma Gopalan ◽  
...  
Keyword(s):  
Natural Products ◽  
Lewis Acid ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Effective Strategy ◽  
Structural Elements ◽  
Nazarov Cyclization ◽  
Active Compounds ◽  
Acid Catalyzed

We herein disclose an effective strategy for the synthesis of [5.3.0] and [6.3.0] fused polycyclic terpenoids, which are important structural elements of natural products and biologically active compounds. The method comprises of Lewis acid catalyzed interrupted Nazarov cyclization of zerumbone derivatives such as zerumbone epoxide, triazole-appended zerumbone, zerumbal, and zerumbenone with a wide substrate scope with different indoles. Zerumbone epoxide furnished [5.3.0] and [6.3.0] fused structurally diverse sesquiterpenoids and all other zerumbone derivatives furnished the [6.3.0] fused motifs.

Developments toward the synthesis and application of 3-hydroxyindanones

2016 ◽  
Vol 14 (38) ◽  
pp. 8895-8910 ◽  
Author(s):  
Tanmoy Chanda ◽  
Maya Shankar Singh
Keyword(s):  
Natural Products ◽  
Functional Materials ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Comprehensive Overview ◽  
Active Compounds ◽  
Drug Candidates

3-Hydroxyindanone is an important scaffold in many natural products, biologically active compounds, and functional materials. This review provides a comprehensive overview of the construction of 3-hydroxyindanone derivatives and their applications towards pharmaceutically promising drug candidates.

Bioinformatics approach on bioisosterism softwares to be used in drug discovery and development

2021 ◽  
Vol 16 ◽  
Author(s):  
Nelson José Freitas da Silveira ◽  
Walter Filgueira de Azevedo Jr. ◽  
Rita Cardoso Guedes ◽  
Leandro Marcos Santos ◽  
Rodolfo Cabral Marcelino ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Mode Of Action ◽  
Wide Spectrum ◽  
Chemical Properties ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
New Drugs ◽  
Active Compounds ◽  
Research Areas ◽  
Reduced Toxicity

Background: In the rational drug development field, a bioisosterism is a tool that improves lead compounds performance, reffering to molecular fragment substitution that has similar physical-chemical properties. Thus, it is possible to modulate drug properties such as absorption, toxicity, and half-life increase. This modulation is of pivotal importance in the discovery, development, identification, and interpretation of the mode of action of biologically active compounds. Objective: Our purpose here is to review the development and application of bioisosterism in drug discovery. In this study history, applications, and use of bioisosteric molecules to create new drugs with high binding affinity in the protein-ligand complexes are described. Method: It is an approach for molecular modification of a prototype based on the replacement of molecular fragments with similar physicochemical properties, being related to the pharmacokinetic and pharmacodynamic phase, aiming at the optimization of the molecules. Results: Discovery, development, identification, and interpretation of the mode of action of biologically active compounds are the most important factors for drug design. The strategy adopted for the improvement of leading compounds is bioisosterism. Conclusion: Bioisosterism methodology is a great advance for obtaining new analogs to existing drugs, enabling the development of new drugs with reduced toxicity, in a comparative analysis with existing drugs. Bioisosterism has a wide spectrum to assist in several research areas.

Asymmetric Organocatalytic Syntheses of Bioactive Compounds

2021 ◽  
Vol 18 ◽  
Author(s):  
Estibaliz Sansinenea ◽  
Aurelio Ortiz
Keyword(s):  
Natural Products ◽  
Asymmetric Synthesis ◽  
Bioactive Compounds ◽  
Cascade Reactions ◽  
Biologically Active ◽  
Active Compounds ◽  
Total Syntheses ◽  
Main Structure ◽  
New Methodologies ◽  
High Stereoselectivity

Background: The total syntheses of complex natural products have evolved to include new methodologies to save time, simplifying the form to achieve these natural compounds. Objective: In this review, we have described the asymmetric synthesis of different natural products and biologically active compounds of the last ten years until the current day. Results: An asymmetric organocatalytic reaction is the key to generate stereoselectively the main structure with the required stereochemistry. Conclusion: Even more remarkable, the organocatalytic cascade reactions, which are carried out with high stereoselectivity, as well as a possible approximation of the organocatalysts activation with substrates are also described.

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