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.

scholarly journals Recent advances in synthetic approaches for medicinal chemistry of C-nucleosides

2018 ◽  
Vol 14 ◽  
pp. 772-785 ◽  
Author(s):  
Kartik Temburnikar ◽  
Katherine L Seley-Radtke
Keyword(s):  
Drug Discovery ◽  
Drug Design ◽  
Nucleophilic Substitution ◽  
Medicinal Chemistry ◽  
Structural Diversity ◽  
Synthetic Analogues ◽  
Structural Modifications ◽  
Modular Synthesis ◽  
Recent Advances ◽  
Synthetic Approaches

C-nucleosides have intrigued biologists and medicinal chemists since their discovery in 1950's. In that regard, C-nucleosides and their synthetic analogues have resulted in promising leads in drug design. Concurrently, advances in chemical syntheses have contributed to structural diversity and drug discovery efforts. Convergent and modular approaches to synthesis have garnered much attention in this regard. Among them nucleophilic substitution at C1' has seen wide applications providing flexibility in synthesis, good yields, the ability to maneuver stereochemistry as well as to incorporate structural modifications. In this review, we describe recent reports on the modular synthesis of C-nucleosides with a focus on D-ribonolactone and sugar modifications that have resulted in potent lead molecules.

Advances in antibiotic drug discovery: reducing the barriers for antibiotic development

2020 ◽  
Vol 12 (22) ◽  
pp. 2067-2087
Author(s):  
Kyle E Murphy ◽  
Grace F Sloan ◽  
Grace V Lawhern ◽  
Grace E Volk ◽  
Jacob T Shumate ◽  
...  
Keyword(s):  
Public Health ◽  
Multidrug Resistance ◽  
Drug Discovery ◽  
Natural Product ◽  
Medicinal Chemistry ◽  
Health Crisis ◽  
Antibiotic Development ◽  
Public Health Crisis ◽  
Recent Advances ◽  
Antibiotic Drug

Antibiotic drug discovery has been an essential field of research since the early 1900s, but the threat from infectious bacteria has only increased over the decades because of the emergence of widespread multidrug resistance. In this review, we discuss the recent advances in natural product, computational and medicinal chemistry that have reinvigorated the field of antibiotic drug discovery while giving perspective on how easily, both in cost and in expertise, these methods can be implemented by other researchers with the goal of increasing the number of scientists contributing to this public health crisis.

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 Recent advances in Entamoeba biology: RNA interference, drug discovery, and gut microbiome

F1000Research ◽  
2016 ◽  
Vol 5 ◽  
pp. 2578 ◽  
Author(s):  
Pedro Morgado ◽  
Dipak Manna ◽  
Upinder Singh
Keyword(s):  
Gene Expression ◽  
Drug Discovery ◽  
Rna Interference ◽  
Cell Biology ◽  
Molecular Mechanisms ◽  
Global Impact ◽  
Human Parasite ◽  
Recent Advances ◽  
Substantial Progress ◽  
Made In

In recent years, substantial progress has been made in understanding the molecular and cell biology of the human parasite Entamoeba histolytica, an important pathogen with significant global impact. This review outlines some recent advances in the Entamoeba field in the last five years, focusing on areas that have not recently been discussed in detail: (i) molecular mechanisms regulating parasite gene expression, (ii) new efforts at drug discovery using high-throughput drug screens, and (iii) the effect of gut microbiota on amoebiasis.

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.

Recent advances in cyclization reactions of isatins or thioisatins via C-N or C-S bond cleavage

2021 ◽  
Author(s):  
Jinhui Shen ◽  
Lei Zhang ◽  
Xiangtai Meng
Keyword(s):  
Medicinal Chemistry ◽  
Raw Materials ◽  
Bond Cleavage ◽  
Synthetic Methods ◽  
Cyclization Reactions ◽  
Recent Advances ◽  
Efficient Construction

The exploration of new reactivity modes and synthetic methods has always been an attractive goal of organic and medicinal chemistry. As potential raw materials for the efficient construction of nitrogen-...

scholarly journals A medicinal chemistry perspective of drug repositioning: Recent advances and challenges in drug discovery

2020 ◽  
Vol 195 ◽  
pp. 112275 ◽  
Author(s):  
Thanigaimalai Pillaiyar ◽  
Sangeetha Meenakshisundaram ◽  
Manoj Manickam ◽  
Murugesan Sankaranarayanan
Keyword(s):  
Drug Discovery ◽  
Medicinal Chemistry ◽  
Drug Repositioning ◽  
Recent Advances

KERCH STRAIT IN KAMYSH-BURUN SPIT AREA: HIGH-RESOLUTION SEISMOACOUSTIC APPROACH

2018 ◽  
Author(s):  
В. Зинько ◽  
V. Zin'ko ◽  
А. Зверев ◽  
A. Zverev ◽  
М. Федин ◽  
...  
Keyword(s):  
High Resolution ◽  
Fracture Zone ◽  
Sedimentary Cover ◽  
Sedimentary Rocks ◽  
The West ◽  
Early Generation ◽  
The Third ◽  
Azov Sea ◽  
Kerch Strait ◽  
Made In

The seismoacoustical investigations was made in the western part of the Kerch strait (Azov sea) near Kamysh-Burun spit. The fracture zone with dislocated sedimentary rocks layers and buried erosional surface was revealed to the west of spit. Three seismofacial units was revealed to the east of spit. The first unit was modern sedimentary cover. The second ones has cross-bedding features and was, probably, the part of early generation of Kamysh-Burun spit, which lied to the east of its modern position. The lower border of the second unit is the erosional surface supposed of phanagorian age. The third unit is screened by acoustic shedows in large part.

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