scholarly journals From Natural Products to New Synthetic Small Molecules: A Journey through the World of Xanthones

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 431
Author(s):  
Madalena M. M. Pinto ◽  
Andreia Palmeira ◽  
Carla Fernandes ◽  
Diana I. S. P. Resende ◽  
Emília Sousa ◽  
...  
Keyword(s):  
Liquid Chromatography ◽  
Small Molecules ◽  
Medicinal Chemistry ◽  
Enantiomeric Purity ◽  
Pharmacological Activities ◽  
Therapeutic Applications ◽  
Xanthone Derivatives ◽  
Analytical Applications ◽  
Resistance Reversal ◽  
The World

This work reviews the contributions of the corresponding author (M.M.M.P.) and her research group to Medicinal Chemistry concerning the isolation from plant and marine sources of xanthone derivatives as well as their synthesis, biological/pharmacological activities, formulation and analytical applications. Although her group activity has been spread over several chemical families with relevance in Medicinal Chemistry, the main focus of the investigation and research has been in the xanthone family. Xanthone derivatives have a variety of activities with great potential for therapeutic applications due to their versatile framework. The group has contributed with several libraries of xanthones derivatives, with a variety of activities such as antitumor, anticoagulant, antiplatelet, anti-inflammatory, antimalarial, antimicrobial, hepatoprotective, antioxidant, and multidrug resistance reversal effects. Besides therapeutic applications, our group has also developed xanthone derivatives with analytical applications as chiral selectors for liquid chromatography and for maritime application as antifouling agents for marine paints. Chemically, it has been challenging to afford green chemistry methods and achieve enantiomeric purity of chiral derivatives. In this review, the structures of the most significant compounds will be presented.

scholarly journals Importance of Fluorine in Benzazole Compounds

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4677
Author(s):  
Thuraya Al-Harthy ◽  
Wajdi Zoghaib ◽  
Raid Abdel-Jalil
Keyword(s):  
Small Molecules ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Short Review ◽  
Significant Enhancement ◽  
Pharmacological Activities ◽  
The Past ◽  
To Receive

Fluorine-containing heterocycles continue to receive considerable attention due to their unique properties. In medicinal chemistry, the incorporation of fluorine in small molecules imparts a significant enhancement their biological activities compared to non-fluorinated molecules. In this short review, we will highlight the importance of incorporating fluorine as a basic appendage in benzothiazole and benzimidazole skeletons. The chemistry and pharmacological activities of heterocycles containing fluorine during the past years are compiled and discussed.

Medicinal Chemistry Database GDBMedChem

2019 ◽  
Author(s):  
Mahendra Awale ◽  
Finton Sirockin ◽  
Nikolaus Stiefl ◽  
Jean-Louis Reymond
Keyword(s):  
Small Molecules ◽  
Natural Product ◽  
Medicinal Chemistry ◽  
3D Visualization ◽  
Molecular Size ◽  
Similarity Searching ◽  
Complex Molecules ◽  
Synthetic Accessibility ◽  
Simple Chemical ◽  
Reduced Complexity

<div>The generated database GDB17 enumerates 166.4 billion possible molecules up to 17 atoms of C, N, O, S and halogens following simple chemical stability and synthetic feasibility rules, however medicinal chemistry criteria are not taken into account. Here we applied rules inspired by medicinal chemistry to exclude problematic functional groups and complex molecules from GDB17, and sampled the resulting subset evenly across molecular size, stereochemistry and polarity to form GDBMedChem as a compact collection of 10 million small molecules.</div><div><br></div><div>This collection has reduced complexity and better synthetic accessibility than the entire GDB17 but retains higher sp 3 - carbon fraction and natural product likeness scores compared to known drugs. GDBMedChem molecules are more diverse and very different from known molecules in terms of substructures and represent an unprecedented source of diversity for drug design. GDBMedChem is available for 3D-visualization, similarity searching and for download at http://gdb.unibe.ch.</div>

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.

A Comprehensive Review on the Therapeutic Versatility of Imidazo [2,1-b]thiazoles

2020 ◽  
Vol 27 (40) ◽  
pp. 6864-6887 ◽  
Author(s):  
Mohd Adil Shareef ◽  
Irfan Khan ◽  
Bathini Nagendra Babu ◽  
Ahmed Kamal
Keyword(s):  
Literature Review ◽  
Medicinal Chemistry ◽  
Therapeutic Agents ◽  
Present Review ◽  
Thiazole Derivatives ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Derivatives Of

Background:: Imidazo[2,1-b]thiazole, a well-known fused five-membered hetrocycle is one of the most promising and versatile moieties in the area of medicinal chemistry. Derivatives of imidazo[2,1-b]thiazole have been investigated for the development of new derivatives that exhibit diverse pharmacological activities. This fused heterocycle is also a part of a number of therapeutic agents. Objective:: To review the extensive pharmacological activities of imidazo[2,1-b]thiazole derivatives and the new molecules developed between 2000-2018 and their usefulness. Method:: Thorough literature review of all relevant papers and patents was conducted. Conclusion:: The present review, covering a number of aspects, is expected to provide useful insights in the design of imidazo[2,1-b]thiazole-based compounds and would inspire the medicinal chemists for a comprehensive and target-oriented information to achieve a major breakthrough in the development of clinically viable candidates.

Medicinal and Biological Significance of Phenoxazine Derivatives

2020 ◽  
Vol 20 ◽  
Author(s):  
Jaya Dwivedi ◽  
Neetu Yaduvanshi ◽  
Shruti Shukla ◽  
Sonika Jain
Keyword(s):  
Drug Resistance ◽  
Biological Significance ◽  
Biological Application ◽  
Pharmacological Activities ◽  
Resistance Reversal ◽  
Anti Inflammatory ◽  
Pharmacological Application

: Since 1887, phenoxazine derivatives have attracted attention of chemist due to its versatile utility, industrially and pharmacologically. Literature is found abundant with various pharmacological activities of phenoxazine derivatives like antitumor, anticancer, antifungal, antibacterial, anti-inflammatory, anti-diabetic, anti-viral, anti-malarial, antidepressant, analgesic and many other drug resistance reversal activities. This review covers detailed over-view on pharmacological application of phenoxazine nucleus, its chemistry and reactivity and also illustrating the incorporation of different group at different positions enhancing its biological application, besides some synthetic procedures.

Recent Advances in Therapeutic Applications of Bisbenzimidazoles

2020 ◽  
Vol 16 (4) ◽  
pp. 454-486 ◽  
Author(s):  
Smita Verma ◽  
Vishnuvardh Ravichandiran ◽  
Nihar Ranjan ◽  
Swaran J.S. Flora
Keyword(s):  
Heterocyclic Compounds ◽  
Wide Spectrum ◽  
Dna Recognition ◽  
Present Review ◽  
Pharmacological Activities ◽  
Structural Motifs ◽  
Therapeutic Applications ◽  
The Past ◽  
Recent Advances

Nitrogen-containing heterocycles are one of the most common structural motifs in approximately 80% of the marketed drugs. Of these, benzimidazoles analogues are known to elicit a wide spectrum of pharmaceutical activities such as anticancer, antibacterial, antiparasitic, antiviral, antifungal as well as chemosensor effect. Based on the benzimidazole core fused heterocyclic compounds, crescent-shaped bisbenzimidazoles were developed which provided an early breakthrough in the sequence-specific DNA recognition. Over the years, a number of functional variations in the bisbenzimidazole core have led to the emergence of their unique properties and established them as versatile ligands against several classes of pathogens. The present review provides an overview of diverse pharmacological activities of the bisbenzimidazole analogues in the past decade with a brief account of its development through the years.

Quinone-Based Drugs: An Important Class of Molecules in Medicinal Chemistry

2020 ◽  
Vol 16 ◽  
Author(s):  
Vitor F. Ferreira ◽  
Alcione S. de Carvalho ◽  
Patricia G. Ferreira ◽  
Carolina G. S. Lima ◽  
Fernando de C. da Silva
Keyword(s):  
Drug Combination ◽  
Medicinal Chemistry ◽  
Pharmaceutical Market ◽  
Important Class ◽  
Therapeutic Applications ◽  
New Applications ◽  
Pharmaceutical Uses

Background: Several quinones are on the pharmaceutical market as drugs for the treatment of several diseases. Objective: The aim of this review was to provide an overview on the quinones that have become drugs for several therapeutic applications. Method: We have comprehensively and critically discussed all the information available in the literature about quinonebased drugs. Results: In this review, the various aspects of the chemistry and biochemistry of these drugs are highlighted, including their repositioning, drug combination and their new uses. Conclusion: The number of studies related to quinone drugs for different pharmaceutical uses shows that the interest in new applications still increasing in recent years.

Sulphonamide: Distribution, Toxicology, Environmental Characteristics, and Analysis - A Review

2020 ◽  
Vol 16 ◽  
Author(s):  
Kirubanandam Grace Pavithra ◽  
Vasudevan Jaikumar ◽  
Ponnusamy Senthil Kumar ◽  
PanneerSelvam SundarRajan
Keyword(s):  
Aqueous Solution ◽  
High Performance Liquid Chromatography ◽  
Capillary Electrophoresis ◽  
Liquid Chromatography ◽  
High Performance ◽  
Uv Spectroscopy ◽  
Relevant Information ◽  
Fluorometric Determination ◽  
Distinctive Features ◽  
The World

Background: Many antibiotics were widely used as medication based on their distinctive features. Among them, sulphonamides were commonly used, however their recalcitrant nature makes them difficult to dispose. Hence, their interaction with environment and analytic technique requires considerable attention globally. Objective: Therefore, this review aimed to provide detailed discussion about environmental as well as human health behaviour and analytic techniques corresponding to sulphonamides. Methods: Various results and discussion were extracted from technical journals and books published by different researchers from all over the world. The cited bibliographic references were intentionally investigated in order to extract relevant information related to proposed work. Results: In this review, the determination techniques such as UV-spectroscopy, Enthalpimetry, Immunosensor, Chromatography, Chemiluminescence, Photoinduced fluorometric determination, Capillary electrophoresis for sulphonamide determination were discussed in detail. Among them, High performance liquid chromatography (HPLC) and UV-spectroscopy was effective and extensively used for screening sulphonamide. Conclusion: Knowing the quantification and behaviour of sulphonamide in aqueous solution is mandatory to opt the suitable wastewater treatment required. Hence, choosing appropriate high precision and feasible screening techniques is necessary, which can be attained with this review.

Phytochemistry and Pharmacology of Genus Bombax

2019 ◽  
Vol 9 (3) ◽  
pp. 184-196
Author(s):  
Deepshikha Rathore ◽  
Geetanjali ◽  
Ram Singh
Keyword(s):  
Medicinal Plants ◽  
Health Care Needs ◽  
Human Beings ◽  
Care Needs ◽  
Pharmacological Activities ◽  
Therapeutic Applications ◽  
Chemical Structures ◽  
Supportive Role ◽  
The Family ◽  
History Of

Background: The history of traditional systems of medicine goes parallel with the history of human beings. Even today people have faith in traditional systems of medicine based on medicinal plants to meet primary health care needs. Hence, the scientific evaluation and documentation of extracts and active ingredients of medicinal plants always play a supportive role in their medicinal applications. Objective: This review aims to present the phytochemicals isolated from the genus Bombax and their pharmacological applications. Methods: The literature from research and review papers was analyzed and the information was compiled to present the pharmacological applications of various secondary metabolites from genus Bombax. Results: The genus Bombax belongs to the family Malvaceae and known for its therapeutic applications. The crude, semi-purified and purified extracts of different parts of this plant have shown potential therapeutic applications. A total of 96 articles including research and review papers were referred for the compilation of isolated phytochemicals and their chemical structures. Conclusion: We systematically summarized 176 isolated compounds from the genus Bombax. The findings show that this plant shows potential towards pharmacological activities. The activities were found more from extracts than the single isolated compounds.

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