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.

Natural Sesquiterpene Lactones in the Prevention and Treatment of Inflammatory Disorders and cancer: A Systematic Study of this Emerging Therapeutic Approach based on Chemical and Pharmacological Aspect

2020 ◽  
Vol 17 (9) ◽  
pp. 1102-1116
Author(s):  
Sudip Kumar Mandal ◽  
Utsab Debnath ◽  
Amresh Kumar ◽  
Sabu Thomas ◽  
Subhash Chandra Mandal ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Biological Activities ◽  
Sesquiterpene Lactones ◽  
Structural Diversity ◽  
Cancer Drug ◽  
Cancer Drug Discovery ◽  
Anti Cancer ◽  
Drug Discovery Program ◽  
Anti Inflammatory ◽  
Family Based

Background and Introduction: Sesquiterpene lactones are a class of secondary metabolite that contains sesquiterpenoids and lactone ring as pharmacophore moiety. A large group of bioactive secondary metabolites such as phytopharmaceuticals belong to this category. From the Asteraceae family-based medicinal plants, more than 5,000 sesquiterpene lactones have been reported so far. Sesquiterpene lactone-based pharmacophore moieties hold promise for broad-spectrum biological activities against cancer, inflammation, parasitic, bacterial, fungal, viral infection and other functional disorders. Moreover, these moiety based phytocompounds have been highlighted with a new dimension in the natural drug discovery program worldwide after the 2015 Medicine Nobel Prize achieved by the Artemisinin researchers. Objective: These bitter substances often contain an α, β-unsaturated-γ-lactone as a major structural backbone, which in recent studies has been explored to be associated with anti-tumor, cytotoxic, and anti-inflammatory action. Recently, the use of sesquiterpene lactones as phytomedicine has been increased. This study will review the prospect of sesquiterpene lactones against inflammation and cancer. Methods: Hence, we emphasized on the different features of this moiety by incorporating its structural diversity on biological activities to explore structure-activity relationships (SAR) against inflammation and cancer. Results: How the dual mode of action such as anti-inflammatory and anti-cancer has been exhibitedby these phytopharmaceuticals will be forecasted in this study. Furthermore, the correlation of anti-inflammatory and anti-cancer activity executed by the sesquiterpene lactones for fruitful phytotherapy will also be revealed in the present review in the milieu of pharmacophore activity relation and pharmacodynamics study as well. Conclusion: So, these metabolites are paramount in phytopharmacological aspects. The present discussion on the future prospect of this moiety based on the reported literature could be a guide for anti-inflammatory and anti-cancer drug discovery programs for the upcoming researchers.

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 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.

scholarly journals Styrylpyrazoles: Properties, Synthesis and Transformations

Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 5886
Author(s):  
Pedro M. O. Gomes ◽  
Pedro M. S. Ouro ◽  
Artur M. S. Silva ◽  
Vera L. M. Silva
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Review Article ◽  
Pyrazole Derivatives ◽  
Huge Number ◽  
Timely Review ◽  
Methods Of Synthesis ◽  
Reduced Forms ◽  
Over Time

The pyrazole nucleus and its reduced forms, pyrazolines and pyrazolidine, are privileged scaffolds in medicinal chemistry due to their remarkable biological activities. A huge number of pyrazole derivatives have been studied and reported over time. This review article gives an overview of pyrazole derivatives that contain a styryl (2-arylvinyl) group linked in different positions of the pyrazole backbone. Although there are studies on the synthesis of styrylpyrazoles dating back to the 1970s and even earlier, this type of compound has rarely been studied. This timely review intends to summarize the properties, biological activity, methods of synthesis and transformation of styrylpyrazoles; thus, highlighting the interest and huge potential for application of this kind of compound.

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 An Efficient Approach to the Synthesis of Novel Oxazolidinones as Potential Antimicrobial Agents

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Kavita Devi ◽  
Yumna Asmat ◽  
Sonika Jain ◽  
Swapnil Sharma ◽  
Jaya Dwivedi
Keyword(s):  
Medicinal Chemistry ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Disk Diffusion ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Disk Diffusion Method ◽  
E Coli ◽  
Efficient Approach ◽  
Fungal Strains

Oxazolidinone, either mononuclear or condensed with other heterocyclics, has established its importance in medicinal chemistry. A variety of biological activities have been reported by oxazolidinone derivatives. The present work describes the synthesis of several oxazolidinone derivatives, 3-(2-(7-chloroquinoline-4-ylamino)ethyl)-2-imino-5-(4-chloro/nitro/methoxy benzylidene)oxazolidin-4-one 4(a–c) and 4-(2-(7-chloroquinolin-4-ylamino)ethyl)-2(4-chloro/nitro/methoxy-benzylidene)-1,6-diox-4,9-di-azaspiro[4,4]nonane-3,8-dione 5(a–c). Synthesized compounds (1, 3, 4a, 5a, and 5c) were screened against bacterial strains such asS. aureus(MTCC 96) andE. coli(MTCC119) and fungal strainsA. niger(MTCC 1344) andC. albicans(MTCC 871) compared with penicillin for bacteria and fluconazole for fungi as reference drugs by disk diffusion method. All synthesized compounds were identified by the means of IR, NMR, and MS.

Barbiturates: A Review of Synthesis and Antimicrobial Research Progress

2021 ◽  
Vol 18 ◽  
Author(s):  
Madhvi ◽  
Divya Utreja ◽  
Shivali Sharma
Keyword(s):  
Barbituric Acid ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Research Progress ◽  
Antimicrobial Drugs ◽  
Anti Cancer ◽  
Methods Of Synthesis ◽  
Anti Oxidant ◽  
New Compounds ◽  
Barbituric Acid Derivatives

Background: Barbituric acid and its derivatives have turned heads for several years as an indispensable class of compounds in the pharmaceutical industry because of their vast assortment of biological activities such as anticonvulsants, hypnotics, anti-diabetic, antiviral, anti-AIDS, anti-cancer, anti-microbial and anti-oxidant etc. Plethoras of studies have shed light on the properties, synthesis, and reactivity of these compounds. The depiction of multiple biological activities by barbiturates compelled us and by virtue of which herein we have mediated over the progress of synthesis of numerous kinds of compounds derived from barbituric acid with well-known and typical examples from 2016 to the present. Objective: The review focuses on the advancements in methods of synthesis of barbituric acid derivatives and their applications as antimicrobial agents. Conclusion: This review will help future researchers to analyze the previous studies and to explore new compounds for the development of efficient antimicrobial drugs.

The Quinazoline-Chalcone and Quinazolinone-Chalcone Hybrids: A Promising Combination for Biological Activity.

2020 ◽  
Vol 20 ◽  
Author(s):  
Eduardo Bustos Mass ◽  
Gilmar Vieira Duarte ◽  
Dennis Russowsky
Keyword(s):  
Biological Activity ◽  
Drug Discovery ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Pharmaceutical Research ◽  
Antimicrobial Activities ◽  
Molecular Hybridization ◽  
Hybrid Compounds ◽  
Synthetic Methodologies ◽  
Number Of Publications

: Quinazoline and/or chalcones derivatives are important targets in several areas of chemical sciences, mainly, in the medicinal chemistry and pharmaceutical research. The purpose of this review is to systematize the information available in the literature, including patents, regarding the benefits exerted by the combination of these two pharmacophores into single molecules. These hybrid compounds can exhibit different biological activities, causing a synergistic or a new effect, compared to the individuals. The variability of biological activities includes anticancer, anti-Alzheimer, antiviral and antimicrobial activities, among others. Additionally, synthetic methodologies to prepare the different molecular architectures were discussed based on their similarities. The increasing number of publications indicates the importance of molecular hybridization on the field of drug discovery.

Structural Activity Relationship and Importance of Benzothiazole Derivatives in Medicinal Chemistry: A Comprehensive Review

2020 ◽  
Vol 17 (3) ◽  
pp. 323-350
Author(s):  
Mahesh Bhat ◽  
Shiddappa Lagamappa Belagali
Keyword(s):  
Medicinal Chemistry ◽  
Biological Activities ◽  
Bioactive Molecules ◽  
Thiazole Ring ◽  
Structural Variations ◽  
Pharmacological Activities ◽  
Benzothiazole Derivatives ◽  
Methods Of Synthesis ◽  
Structural Activity Relationship ◽  
Interesting Compound

:Benzothiazole (1, 3-benzothiazole) is one of the heterocyclic compounds, which is a weak base having varied biological activities. The unique methine center present in the thiazole ring makes benzothiazole as the most important heterocyclic compound. It is a common and integral structure of many natural and synthetic bioactive molecules. Benzothiazole derivatives show a variety of activities, with less toxic effects and their derivatives showed enhanced activities, which has proven Benzothiazole scaffold as one of the important moieties in medicinal chemistry. Benzothiazole ring containing compounds possess various pharmacological activities such as anti-viral, anti-microbial, antiallergic, anti-diabetic, anti-tumor, anti-inflammatory, anthelmitic and anti-cancer, which makes benzothiazole a rapidly developing and interesting compound in the medicinal chemistry. This review briefly explains the importance, common methods of synthesis of the benzothiazole scaffold and also explains the popular benzothiazole molecules which have applications in various fields of chemistry. A review has been carried out based on various pharmacological activities containing benzothiazole moieties and rationalize the activities based on the structural variations. Literature on benzothiazole derivatives reveals that substitution on the C-2 carbon atom and C-6 are the reasons for a variety of biological activities.

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