scholarly journals Imidazole: Having Versatile Biological Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Amita Verma ◽  
Sunil Joshi ◽  
Deepika Singh
Keyword(s):  
Natural Products ◽  
Nucleic Acid ◽  
Biological Activities ◽  
Imidazole Ring ◽  
Heterocyclic Ring ◽  
Heterocyclic Chemistry ◽  
The Past ◽  
Poorly Soluble ◽  
Anti Hiv ◽  
Imidazole Compounds

Imidazoles have occupied a unique position in heterocyclic chemistry, and its derivatives have attracted considerable interests in recent years for their versatile properties in chemistry and pharmacology. Imidazole is nitrogen-containing heterocyclic ring which possesses biological and pharmaceutical importance. Thus, imidazole compounds have been an interesting source for researchers for more than a century. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine, and nucleic acid. Being a polar and ionisable aromatic compound, it improves pharmacokinetic characteristics of lead molecules and thus is used as a remedy to optimize solubility and bioavailability parameters of proposed poorly soluble lead molecules. There are several methods used for the synthesis of imidazole-containing compounds, and also their various structure reactions offer enormous scope in the field of medicinal chemistry. The imidazole derivatives possess extensive spectrum of biological activities such as antibacterial, anticancer, antitubercular, antifungal, analgesic, and anti-HIV activities. This paper aims to review the biological activities of imidazole during the past years.

Imidazole Scaffold based Compounds in the Development of Therapeutic Drugs

2021 ◽  
Vol 21 ◽  
Author(s):  
Fanjie Hu ◽  
Lina Zhang ◽  
Kutty Selva Nandakumar ◽  
Kui Cheng
Keyword(s):  
Natural Products ◽  
Hydrogen Bonds ◽  
Biological Activities ◽  
Structural Characteristics ◽  
Imidazole Ring ◽  
Heterocyclic Ring ◽  
Pharmacological Activities ◽  
Therapeutic Drugs ◽  
Recent Developments ◽  
Aromatic Heterocyclic

: Imidazole has an important five-membered aromatic heterocyclic ring, which is available widely in natural products and synthetic molecules. The special structural characteristics of imidazole ring enable it to bind with various enzymes and receptors through hydrogen bonds, coordination, ion-dipole and cation-π interactions, hydrophobic effects, and Van der Waals forces. These interactions promote several biological activities involving anti-tumor, anti-inflammatory, anti-microbial and anti-viral properties. Herein, we review and discuss the recent developments occurred in using imidazole derivatives along with their special pharmacological activities for various diseases treatment.

Synthesis and Biological Activity of Quaternary Quinolinium Salts: A Review

2020 ◽  
Vol 23 (21) ◽  
pp. 2271-2294 ◽  
Author(s):  
Divya Utreja ◽  
Shivali Sharma ◽  
Akhil Goyal ◽  
Komalpreet Kaur ◽  
Sonia Kaushal
Keyword(s):  
Tyrosine Kinases ◽  
Biological Activities ◽  
Polymeric Materials ◽  
Tubulin Polymerization ◽  
Quinoline Derivatives ◽  
Heterocyclic Chemistry ◽  
Biological Profile ◽  
Drug Candidates ◽  
Anti Hiv ◽  
Quinolinium Salts

Heterocyclic chemistry is the only branch of chemistry that has applications in varied areas such as dyes, photosensitizers, coordination compounds, polymeric materials, biological, and many other fields. Quinoline and its derivatives have always engrossed both synthetic chemists and biologists because of their diverse chemical and pharmacological properties as these ring systems can be easily found in various natural products, especially in alkaloids. Among alkaloids, quinoline derivatives i.e. quinolinium salts have attracted much attention nowadays owing to their diverse biological profile such as antimicrobial, antitumor, antifungal, hypotensive, anti-HIV, analgesics and anti-inflammatory, etc. Quinoline and its analogs have recently been examined for their modes of function in the inhibition of tyrosine kinases, proteasome, tubulin polymerization, topoisomerase, and DNA repair. These observations have been guiding scientists for the expansion of new quinoline derivatives with improved and varied biological activities. Quinolinium salts have immense possibilities and scope to investigate these compounds as potential drug candidates. Therefore, we shall present a concise compilation of this work to aid in present knowledge and to help researchers explore an interesting quinoline class having medicinal potential.

scholarly journals Modern Synthetic Methods for the Stereoselective Construction of 1,3-Dienes

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 249
Author(s):  
Raquel G. Soengas ◽  
Humberto Rodríguez-Solla
Keyword(s):  
Organic Chemistry ◽  
Natural Products ◽  
Functional Group ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Bond Forming ◽  
Drug Candidates ◽  
The Past ◽  
Wide Range

The 1,3-butadiene motif is widely found in many natural products and drug candidates with relevant biological activities. Moreover, dienes are important targets for synthetic chemists, due to their ability to give access to a wide range of functional group transformations, including a broad range of C-C bond-forming processes. Therefore, the stereoselective preparation of dienes have attracted much attention over the past decades, and the search for new synthetic protocols continues unabated. The aim of this review is to give an overview of the diverse methodologies that have emerged in the last decade, with a focus on the synthetic processes that meet the requirements of efficiency and sustainability of modern organic chemistry.

scholarly journals Synthesis and Biological Activities of Some Pyrimidine Derivatives: A Review

2020 ◽  
Vol 36 (6) ◽  
pp. 1001-1015
Author(s):  
Nadia Ali Ahmed Elkanzi
Keyword(s):  
Nitrogen Atom ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Cardiovascular Agents ◽  
Anti Hiv ◽  
Biological And Pharmacological Activities

Nitrogen containing synthetically and biologically important heterocyclic ring system namely pyrimidine possess both biological and pharmacological activities, and defend as aromatic six heterocyclic with 1and 3 nitrogen atom in ring. Preparation of pyrimidine via different methods offer its importance in fields of medicinal chemistry and Chemistry. Pyrimidines and their derivatives act as anti-inflammatory, anti-malaria, anti-tumor, cardiovascular agents, anti-neoplastic, anti-tubercular, anti- HIV, diuretic ,anti-viral, anti-microbial, ,analgesic .This review give light up on biological and pharmacological activities of pyrimidine nucleus.

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 Lyngbouilloside and Related Macrolides from Marine Cyanobacteria

2013 ◽  
Vol 8 (7) ◽  
pp. 1934578X1300800
Author(s):  
Abdelatif ElMarrouni ◽  
Amandine Kolleth ◽  
Raphael Lebeuf ◽  
Julian Gebauer ◽  
Sébastien Prevost ◽  
...  
Keyword(s):  
Natural Products ◽  
Biological Activities ◽  
Marine Cyanobacteria ◽  
The Past

Lyngbouilloside and the related macrolides lyngbyaloside lyngbyaloside B and lyngbyaloside C have attracted a lot of attention over the past decade due to their intriguing architecture their natural scarcity and their potential biological activities. This review aims to showcase the various strategies that have been used to access these natural products.

scholarly journals ESPECTROSCOPIA COMPUTACIONAL APLICADA AO REASSINALAMENTO ESTRUTURAL DE MOLÉCULAS QUIRAIS: HELIANNUOL L

2020 ◽  
Author(s):  
Jordana T. Brito ◽  
Lucas H. Martorano ◽  
Ana Carolina F. de Albuquerque ◽  
Carlos Magno Rocha Ribeiro ◽  
Rodolfo Goetze Fiorot ◽  
...  
Keyword(s):  
Natural Products ◽  
Theoretical Calculations ◽  
Chemical Shifts ◽  
Biological Activities ◽  
Great Effort ◽  
The Past ◽  
Spectral Interpretation ◽  
Combined Use ◽  
Helianthus Annus

In the past, structure determination of natural products was an arduous process depending almost entirely on chemical synthesis, mainly by derivatization and degradation processes, taking years of effort. Recently, structural elucidation of natural products has undergone a revolution. Nowadays, with the combined use of different advanced spectroscopic methods, it became possible to completely assign the structure of natural products using small amounts of sample. However, despite the extraordinary ongoing advances in spectroscopy, the mischaracterization of natural products has been and remains a recurrent problem, especially in the presence of several chiral centers. The misinterpretation of NMR data has resulted in frequent reports addressing the issue of structural reassignment. In this context, a great effort has been devoted to the development of quantum chemical calculations to predict NMR parameters, and thus achieve a more accurate spectral interpretation. In this work, we applied a protocol for theoretical calculations of 1H NMR chemical shifts in order to establish the correct and unequivocal structure of Helianuol L, a member of the Heliannuol’s class, isolated from Helianthus annus. These secondary metabolites present a broad spectrum of biological activities, including the allelochemical activity, making them promising candidates as natural agrochemicals. It is worth mentioning, however, that the process of elucidating the structure of Heliannuol L was based on structural correlations with molecules already known in the literature, where few stereochemical analyses were performed. In this way, based on the fact that other compounds of the Heliannuol’s class had their structure previously reassigned, the verification of the proposed structure of Heliannuol L becomes of great importance.

Recent Advances in the Synthesis of Thiadiazoles

Synlett ◽  
2019 ◽  
Vol 30 (18) ◽  
pp. 2041-2050
Author(s):  
Yan Xiao ◽  
Song Sun ◽  
Jin-Tao Yu ◽  
Jiang Cheng
Keyword(s):  
Natural Products ◽  
Broad Spectrum ◽  
Biological Activities ◽  
Pharmaceutical Compounds ◽  
Antifungal Drugs ◽  
The Past ◽  
Recent Advances

Thiadiazole moieties are present in many natural products and pharmaceutical compounds that possess a broad spectrum of biological activities, serving as antidepressant, anxiolytic, antimicrobial, antitubercular, antiinflammatory, antidiabetic, anticancer, antihypertensive, or antifungal drugs. Many excellent methods have been reported for accessing such frameworks. In this review, we summarize advances made within the past ten years in the synthesis of various types of thiadiazole.1 Introduction2 Synthesis of Thiadiazoles2.1 Synthesis of 1,2,3-Thiadiazoles2.1.1 Synthesis of 1,2,3-Thiadiazoles from Diazo/Azide Compounds2.1.2 Synthesis of 1,2,3-Thiadiazoles from Sulfonyl Hydrazines or N-Tosylhydrazones2.2 Synthesis of 1,2,4-Thiadiazoles2.2.1 Synthesis of 1,2,4-Thiadiazoles from Thioamides or their Derivatives2.2.2 Synthesis of 1,2,4-Thiadiazoles from Amidines or 2-Aminopyridines2.3 Synthesis of 1,3,4-Thiadiazoles2.4 Synthesis of 1,2,5-Thiadiazoles3 Conclusion

scholarly journals ANTI-ULCER AGENTS: A PHARMACOLOGICAL UPDATE OF THE PAST TEN YEARS

2019 ◽  
pp. 37-41
Author(s):  
SUDIP KUMAR MANDAL ◽  
SUBHOJIT DAWN ◽  
ANINDYA BOSE
Keyword(s):  
Natural Products ◽  
Proton Pump Inhibitors ◽  
Proton Pump ◽  
Biological Activities ◽  
Mangifera Indica ◽  
Aloe Vera ◽  
Zingiber Officinale ◽  
Ocimum Sanctum ◽  
Cell Hyperplasia ◽  
The Past

New anti-ulcer substances are still vitally necessary for the people of countries such as India and South Africa to avoid high cost of the most prescribed marketed anti-ulcer drugs (proton-pump inhibitors). New candidate against gastric ulcer is also necessary to avoid the potential problem (enterochromaffin-like cell hyperplasia may be induced) associated with the long-term use of synthetic proton-pump inhibitors. However, the search for the novel entity against ulceration is challenging because of the complexity of the ulcer process and its role in host defense to infections. Nature is the source of remedies for the humankind. Among the different biological activities of the natural products that have been published till date, anti-ulcer is one of the most reported effects. Some single natural products such as curcumin, 1-hydroxy-3,7,8-trimethoxyxanthone, cinnamic acid, thymol, epoxycarvone, and menthol; single synthetic products such as, 4,6-diaryl-3, 4-dihydropyrimidin-2(1H)-thiones, 1,4-dihydropyrimidine derivatives, and dihydropyrimidinone and piperidine hybrids; plant products such as Aloe vera, Mangifera indica, Zingiber officinale, Azadirachta indica, Psidium guava, Carica papaya, Panax ginseng, Terminalia chebula, Ocimum sanctum, Daucus carota, and Mimosa pudica, Alpinia galangal; nutraceuticals such as garlic, cauliflower, banana, honey, cucumber, and cod liver oil with anti-ulcer effects have been discussed in this review. A complete review of literature was conducted using different databases on ScienceDirect, Scopus, PubMed, and Google Scholar. This review is a genuine attempt to explore the past 10 years’ pharmacological update of some anti-ulcer agents.

Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban
Keyword(s):  
Biological Activities ◽  
Synthetic Approach ◽  
Clinical Use ◽  
New Approach ◽  
Click Reactions ◽  
Drug Candidates ◽  
The Past ◽  
Low Toxicity ◽  
New Compounds ◽  
Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

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