scholarly journals Synthesis of Imidazole-Based Medicinal Molecules Utilizing the van Leusen Imidazole Synthesis

2020 ◽  
Vol 13 (3) ◽  
pp. 37 ◽  
Author(s):  
Xunan Zheng ◽  
Zhengning Ma ◽  
Dawei Zhang
Keyword(s):  
Drug Discovery ◽  
Chemical Synthesis ◽  
Small Molecules ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Structural Features ◽  
Pharmaceutical Companies ◽  
Recent Developments ◽  
Van Leusen Reaction

Imidazole and its derivatives are one of the most vital and universal heterocycles in medicinal chemistry. Owing to their special structural features, these compounds exhibit a widespread spectrum of significant pharmacological or biological activities, and are widely researched and applied by pharmaceutical companies for drug discovery. The van Leusen reaction based on tosylmethylisocyanides (TosMICs) is one of the most appropriate strategies to synthetize imidazole-based medicinal molecules, which has been increasingly developed on account of its advantages. In this review, we summarize the recent developments of the chemical synthesis and bioactivity of imidazole-containing medicinal small molecules, utilizing the van Leusen imidazole synthesis from 1977.

1,8-naphthyridine derivatives: an updated review on recent advancements of their myriad biological activities

2021 ◽  
Author(s):  
Shivani Mithula ◽  
Adinarayana Nandikolla ◽  
Sankaranarayanan Murugesan ◽  
Venkata GCS Kondapalli
Keyword(s):  
Drug Discovery ◽  
Broad Spectrum ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
The Past ◽  
Anti Hiv ◽  
Past Half ◽  
Half Decade

Among all nitrogen-containing heterocycles, the 1,8-naphthyridine scaffold has recently gained an immense amount of curiosity from numerous researchers across fields of medicinal chemistry and drug discovery. This new attention can be ascribed to its versatility of synthesis, its reactiveness and the variety of biological activities it has exhibited. Over the past half-decade, numerous diverse biological evaluations have been conducted on 1,8-naphthyridine and its derivatives in a quest to unravel novel pharmacological facets to this scaffold. Its potency to treat neurodegenerative and immunomodulatory disorders, along with its anti-HIV, antidepressant and antioxidant properties, has enticed researchers to look beyond its broad-spectrum activities, providing further scope for exploration. This review is a consolidated update of previous works on 1,8-naphthyridines and their analogs, focusing on the past 5 years.

scholarly journals An Overview of Bioactive 1,3-Oxazole-Containing Alkaloids from Marine Organisms

2021 ◽  
Vol 14 (12) ◽  
pp. 1274
Author(s):  
Jinyun Chen ◽  
Sunyan Lv ◽  
Jia Liu ◽  
Yanlei Yu ◽  
Hong Wang ◽  
...  
Keyword(s):  
Nitrogen Atom ◽  
Chemical Synthesis ◽  
Biological Activities ◽  
Structural Features ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Marine Organisms ◽  
Chemical Structures ◽  
First Time ◽  
Oxazole Derivatives

1,3-Oxazole chemicals are a unique class of five-membered monocyclic heteroarenes, containing a nitrogen atom and an oxygen. These alkaloids have attracted extensive attention from medicinal chemists and pharmacologists owing to their diverse arrays of chemical structures and biological activities, and a series of 1,3-oxazole derivatives has been developed into therapeutic agents (e.g., almoxatone, befloxatone, cabotegravir, delpazolid, fenpipalone, haloxazolam, inavolisib). A growing amount of evidence indicates that marine organisms are one of important sources of 1,3-oxazole-containing alkaloids. To improve our knowledge regarding these marine-derived substances, as many as 285 compounds are summarized in this review, which, for the first time, highlights their sources, structural features and biological properties, as well as their biosynthesis and chemical synthesis. Perspective for the future discovery of new 1,3-oxazole compounds from marine organisms is also provided.

Chromone a Privileged Scaffold in Drug Discovery: Developments on the Synthesis and Bioactivity

2021 ◽  
Vol 21 ◽  
Author(s):  
Anjitha Theres Benny ◽  
Sonia D. Arikkatt ◽  
Cijo George Vazhappilly ◽  
Sathananthan Kannadasan ◽  
Renjan Thomas ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Medicinal Chemistry ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antiplatelet Agents ◽  
Materials Synthesis ◽  
Biological Responses ◽  
Metal Metal ◽  
Methods Of Synthesis ◽  
Drug Discovery Program

: Chromones are the class of secondary metabolites broadly occurred in the plant kingdom in a noticeable quantity. This rigid bicyclic system has been categorized “as privileged scaffolds in compounds” in medicinal chemistry. The wide biological responses made them an important moiety in a drug discovery program. This review provides updates on the various methods of synthesis of chromones and biological applications in medicinal chemistry. Various synthetic strategies for the construction of chromones include readily available phenols, salicylic acid and its derivatives, ynones, chalcones, enaminones, chalcones and 2-hydroxyarylalkylketones as starting materials. Synthesis of chromones by using metal, metal free, nanomaterials and different catalysts are included. Details of diverse biological activities such as anti-cancer agents, antimicrobial agents, anti-viral property, anti-inflammatory agents, antioxidants, Monoamine Oxidase-B (MAO-B) Inhibitors, anti-Alzheimer’s agents, anti-diabetic agent, antihistaminic potential, antiplatelet agents of chromone derivatives are diecussed.

scholarly journals A review of the total syntheses of triptolide

2019 ◽  
Vol 15 ◽  
pp. 1984-1995 ◽  
Author(s):  
Xiang Zhang ◽  
Zaozao Xiao ◽  
Hongtao Xu
Keyword(s):  
Organic Chemistry ◽  
Natural Product ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Structural Features ◽  
Total Syntheses ◽  
Future Studies

Triptolide is a complex triepoxide diterpene natural product that has attracted considerable interest in the organic chemistry and medicinal chemistry societies due to its intriguing structural features and multiple promising biological activities. In this review, progress in the total syntheses of triptolide are systematically summarized. We hope to gain a better understanding of the field and provide constructive suggestions for future studies of triptolide.

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.

Recent Applications of Benzimidazole as a Privileged Scaffold in Drug Discovery

2020 ◽  
Vol 20 ◽  
Author(s):  
Yongzhen Guo ◽  
Xuben Hou ◽  
Hao Fang
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Great Influence ◽  
Parasitic Infections ◽  
Peptic Ulcers ◽  
Lead Compounds ◽  
Privileged Scaffold

: Benzimidazole is an aromatic bicyclic heterocycle that is regarded as a valuable privileged scaffold in medicinal chemistry. Many marketed drugs and natural products containing benzimidazole scaffolds exert great influence in fighting various diseases, such as hypertension, peptic ulcers, parasitic infections, and cancer. In this review, we introduce the pharmacological applications of some marketed drugs and lead compounds with a focus on anticancer agents, reporting the corresponding data to show the biological activities at their targets. The publications in this review encompass those from 2014 to 2019.

scholarly journals Arylnaphthalene lactones: structures and pharmacological potentials

2021 ◽  
Author(s):  
Soyoung Park ◽  
Seungsu Kim ◽  
Dongyun Shin
Keyword(s):  
Drug Discovery ◽  
Medicinal Plants ◽  
Biological Activities ◽  
Structural Diversity ◽  
Structural Features ◽  
Type I ◽  
Type Ii ◽  
Pharmacological Activities ◽  
Naturally Occurring ◽  
Anti Hiv

AbstractNatural arylnaphthalene lactones are representative lignans that are found in various dietary and medicinal plants. Their unique structural features and significant pharmacological activity have attracted considerable attention from both synthetic and medicinal chemists. Owing to their unique structural features such as relative rigid tetracyclic skeleton, structural diversity of more than five substituents, and no chiral center, arylnaphthalene lactones are recognized as a valuable scaffold for drug discovery, in addition to their significant pharmacological activities. This review covers the structures and isolation of all naturally occurring arylnaphthalene lactone congeners reported. Based on the aryl substituents, they were categorized as Type I and Type II and further classified according to the oxidation state of the ring and glycosylation level. Special attention has been paid to natural arylnaphthalene lactones owing to their broad spectrum of biological activities such as cytotoxic, antiplatelet, antiviral, anti-HIV, antifungal, neuroprotective, and anti-inflammatory properties. All the products were reorganized based on their biological activities, and selected data are presented.

scholarly journals Recent Developments and Biological Activities of 5-Oxo-Imidazolones Derivatives: A Review

2021 ◽  
pp. 287-305
Author(s):  
N. Yellasubbaiah ◽  
V. Velmurugan ◽  
B. Nagasudha
Keyword(s):  
Drug Discovery ◽  
Biological Property ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Ring System ◽  
Present Review ◽  
Modern Drug ◽  
Recent Developments ◽  
Biological Potency

Heterocyclic compounds are essential primary units for both the synthetic and natural starting points. 5-oxo-imidazolone is a 5-member ring system that contains 3 carbons and 2 nitrogens that are arranged at 3 and 1 positions, and ─C═O at the 5th position of the ring. 5-oxo-imidazolone is known as a privileged molecule because of its all biological potency. This biological property increased the attention of many investigators to analyze this ring system and expose several activities. The present review aims to outline the various activities reported on the synthesis and the biological potencies of 5-oxo-imidazolone derivatives. 5-oxo-imidazolone is an important pharmacophore in modern drug discovery.

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.

Recent Advances for the Synthesis of Selenium-containing Small Molecules as Potent Antitumor Agents

2018 ◽  
Vol 25 (17) ◽  
pp. 2009-2033 ◽  
Author(s):  
Qi Miao ◽  
Jinyi Xu ◽  
Aijun Lin ◽  
Xiaoming Wu ◽  
Liang Wu ◽  
...  
Keyword(s):  
Small Molecules ◽  
Antitumor Agents ◽  
Biological Activities ◽  
Structural Features ◽  
Organoselenium Compounds ◽  
Antitumor Effects ◽  
Anticancer Compounds ◽  
Design And Synthesis ◽  
Promising Area ◽  
Synthetic Approaches

Selenium-containing small molecules have attracted considerable attention of chemical and medicinal researchers owing to their various biological activities, such as antitumor effects, cardiovascular protection, antibacterial or antiviral effects, immunoregulation and nerve protection, among which the most promising area is antineoplasm. In the past several decades, different kinds of organoselenium compounds, such as selenides, seleno(iso)cyanates, substituted selenoureas, selenious esters and Se-containing heterocycles have been reported as candidates of anti-cancer agents. Current reviews of Se-containing anticancer compounds mainly concerned about the investigation of their bioactivities, whereas, few attention has been addressed on their synthetic approaches. Herein, we summarized methodologies recently developed to synthesize organoselenium compounds with potent antineoplastic properties, which would be helpful for further design and synthesis of new bioactive Se-containing molecules with diverse structural features.

Sign in / Sign up

Export Citation Format

Share Document