scholarly journals Development of New Synthetic Methods for Carbazole Compounds Aimed at Drug Discovery and Exploratory Research on Pharmaceutical Materials

2021 ◽  
Vol 141 (12) ◽  
pp. 1281-1288
Author(s):  
Takashi Nishiyama
Keyword(s):  
Drug Discovery ◽  
Synthetic Methods ◽  
Exploratory Research ◽  
Pharmaceutical Materials

scholarly journals Triazole-Modified Peptidomimetics: An Opportunity for Drug Discovery and Development

2021 ◽  
Vol 9 ◽  
Author(s):  
Agnieszka Staśkiewicz ◽  
Patrycja Ledwoń ◽  
Paolo Rovero ◽  
Anna Maria Papini ◽  
Rafal Latajka
Keyword(s):  
Biological Activity ◽  
Drug Discovery ◽  
Drug Design ◽  
Enzymatic Degradation ◽  
Biological Properties ◽  
Synthetic Methods ◽  
Drug Discovery And Development ◽  
Triazole Derivatives ◽  
Natural Peptides

Peptidomimetics play a fundamental role in drug design due to their preferential properties regarding natural peptides. In particular, compounds possessing nitrogen-containing heterocycles have been intensively studied in recent years. The triazolyl moiety incorporation decreases the molecule susceptibility to enzymatic degradation, reduction, hydrolysis, and oxidation. In fact, peptides containing triazole rings are a typical example of peptidomimetics. They have all the advantages over classic peptides. Both efficient synthetic methods and biological activity make these systems an interesting and promising object of research. Peptide triazole derivatives display a diversity of biological properties and can be obtained via numerous synthetic strategies. In this review, we have highlighted the importance of the triazole-modified peptidomimetics in the field of drug design. We present an overview on new achievements in triazolyl-containing peptidomimetics synthesis and their biological activity as inhibitors of enzymes or against cancer, viruses, bacteria, or fungi. The relevance of above-mentioned compounds was confirmed by their comparison with unmodified peptides.

The importance of synthetic chemistry in the pharmaceutical industry

Science ◽  
2019 ◽  
Vol 363 (6424) ◽  
pp. eaat0805 ◽  
Author(s):  
Kevin R. Campos ◽  
Paul J. Coleman ◽  
Juan C. Alvarez ◽  
Spencer D. Dreher ◽  
Robert M. Garbaccio ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Pharmaceutical Industry ◽  
Synthetic Methods ◽  
Past Century ◽  
Synthetic Chemistry ◽  
Drug Discovery And Development ◽  
The Past ◽  
New Concepts ◽  
The Face ◽  
Chemical Matter

Innovations in synthetic chemistry have enabled the discovery of many breakthrough therapies that have improved human health over the past century. In the face of increasing challenges in the pharmaceutical sector, continued innovation in chemistry is required to drive the discovery of the next wave of medicines. Novel synthetic methods not only unlock access to previously unattainable chemical matter, but also inspire new concepts as to how we design and build chemical matter. We identify some of the most important recent advances in synthetic chemistry as well as opportunities at the interface with partner disciplines that are poised to transform the practice of drug discovery and development.

F-Based Small Group Decoration of Heteroarenes via C-H Activation: Medicinal Chemistry Rationale and late-stage Synthetic Methods

2021 ◽  
Vol 25 ◽  
Author(s):  
Paolo Ronchi ◽  
Sara Guariento ◽  
Daniele Pala ◽  
Daniela Pizzirani ◽  
Claudio Fiorelli ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Small Molecules ◽  
Small Group ◽  
Small Groups ◽  
Late Stage ◽  
Medicinal Chemistry ◽  
Synthetic Methods ◽  
Type Reaction ◽  
Approved Drugs ◽  
Chemistry Community

: The use of F-based decorations in drug discovery started from the development of fluorocorticoids and fluorochinolones (1950s and 1980s, respectively), and has resulted in about 20% of approved drugs on the Market containing fluorine. From a medicinal chemistry perspective, the installation of F-based small groups (e.g., CF3, -CF2H, -OCF3, -OCF2H, -SCF3, -SCF2H) necessarily impacts on physicochemical, pharmacokinetics, pharmacodynamics and toxicological properties of small molecules. Accordingly, a huge interest in this topic is constantly arising in the medicinal chemistry community. Focusing on heteroarenes, the synthetic access to these substitutions is guaranteed by a number of effective reactions such as Minisci-type reaction, photochemistry or electrochemistry C-H activation. The aim of this work is to analyze the rationale in using these groups in medicinal chemistry and highlight the currently available synthetic toolbox of C-H activation for their introduction on heteroarenes of pharmaceutical interest. A particular focus has been given to those procedures amenable to the late-stage functionalisation process.

scholarly journals C–H functionalisation tolerant to polar groups could transform fragment-based drug discovery (FBDD)

2021 ◽  
Vol 12 (36) ◽  
pp. 11976-11985
Author(s):  
Gianni Chessari ◽  
Rachel Grainger ◽  
Rhian S. Holvey ◽  
R. Frederick Ludlow ◽  
Paul N. Mortenson ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Case Studies ◽  
Meta Analysis ◽  
Synthetic Methods ◽  
Polar Groups ◽  
Fragment Based Drug Discovery

An in depth meta analysis of 131 fragment-to-lead case-studies has shown the importance of synthetic methods that allow carbon-centred synthetic elaboration in the presence of polar pharmacophores.

scholarly journals Fluorine-Containing Chrysin Derivatives

2019 ◽  
Vol 14 (9) ◽  
pp. 1934578X1987892
Author(s):  
Yue Zhu ◽  
Xu Yao ◽  
Jin Long ◽  
Rong Li ◽  
Yi Liu ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Fluorine Atom ◽  
Medicinal Chemistry ◽  
Antiviral Drug ◽  
Antimicrobial Activities ◽  
Synthetic Methods ◽  
Reaction Process ◽  
Great Role ◽  
Substituent Group

Chrysin, a flavonoid, has played a great role in the fields of anticancer, antibacterial, and antiviral drug discovery. A large number of chrysin derivatives have been synthesized recently. The fluorine atom represents an important substituent group for a great number of natural products and pharmaceuticals. Taking into account the importance of both chrysin and the fluorine atom in medicinal chemistry, the synthesis of fluorine-containing chrysin derivatives has gained great interest. Chemically, the synthetic methods for these new chrysin derivatives have also been developed rapidly. In recent years, research on their synthesis has been focused on speeding up the reaction process by changing the catalyst. Biologically, the purpose of introducing fluorine into chrysin was to improve its lipophilicity, but today it is mainly focused on the enhancement and improvement of either its anticancer or antimicrobial activities by incorporating the special properties of fluorine atoms. In this review, synthetic methods for the introduction of fluorine atoms into chrysin are summarized, and their anticancer, antibacterial, antiviral, and hypoglycemic effects are discussed.

scholarly journals Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization

Organics ◽  
2021 ◽  
Vol 2 (4) ◽  
pp. 337-347
Author(s):  
Carolina Durand ◽  
Michal Szostak
Keyword(s):  
Drug Discovery ◽  
Medicinal Chemistry ◽  
Structural Diversity ◽  
Synthetic Methods ◽  
Nitrogen Heterocycle ◽  
Piperazine Ring ◽  
The Third ◽  
Recent Advances ◽  
Made In

Piperazine ranks as the third most common nitrogen heterocycle in drug discovery, and it is the key component of several blockbuster drugs, such as Imatinib (also marketed as Gleevec) or Sildenafil, sold as Viagra. Despite its wide use in medicinal chemistry, the structural diversity of piperazines is limited, with about 80% of piperazine-containing drugs containing substituents only at the nitrogen positions. Recently, major advances have been made in the C–H functionalization of the carbon atoms of the piperazine ring. Herein, we present an overview of the recent synthetic methods to afford functionalized piperazines with a focus on C–H functionalization.

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