Synthesis of Antimicrobial Benzimidazole–Pyrazole Compounds and Their Biological Activities

The synthesis of new compounds with antimicrobial and antiviral properties is a central objective today in the context of the COVID-19 pandemic. Benzimidazole and pyrazole compounds have remarkable biological properties, such as antimicrobial, antiviral, antitumor, analgesic, anti-inflammatory, anti-Alzheimer’s, antiulcer, antidiabetic. Moreover, recent literature mentions the syntheses and antimicrobial properties of some benzimidazole–pyrazole hybrids, as well as other biological properties thereof. In this review, we aim to review the methods of synthesis of these hybrids, the antimicrobial activities of the compounds, their correlation with various groups present on the molecule, as well as their pharmaceutical properties.

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Exploratory Assessment to Evaluate Seed Sprouting under Elevated CO2 Revealed Improved Biomass, Physiology, and Nutritional Value of Trachyspermum ammi

Agronomy ◽

10.3390/agronomy11050830 ◽

2021 ◽

Vol 11 (5) ◽

pp. 830

Author(s):

Abdelrahim H. A. Hassan ◽

Mohammad K. Okla ◽

Saud S. Al-amri ◽

Mohamed A. El-Tayeb ◽

Ihab M. Moussa ◽

...

Keyword(s):

Biological Activities ◽

Soluble Sugars ◽

Antimicrobial Properties ◽

Human Tumor ◽

Antimicrobial Activities ◽

Biological Properties ◽

Antioxidant Power ◽

Primary And Secondary Metabolites ◽

Elevated Atmospheric Co2 ◽

Trachyspermum Ammi

Elevated atmospheric CO2 (eCO2) can significantly enhance plant metabolism and improve their nutritional quality. Although several studies addressed the effect of eCO2 on plants, to our knowledge, there are no studies that have applied eCO2 to improve growth, chemical composition, and biological properties of ajwain (Trachyspermum ammi) during sprouting. Herein, eCO2 (620 µmol mol−1) was employed to enhance photosynthetic reactions. Improved photosynthesis induced primary and bioactive secondary metabolism, which led to improved biological activities of T. ammi sprouts in comparison with control sprouts and seeds. eCO2-treated sprouts showed significantly (p < 0.05) higher levels of most measured nutritional primary and secondary metabolites like soluble sugars, essential amino acids, organic acids, essential oils, phenolics, and flavonoids than control sprouts, which had significantly higher values than control seeds. eCO2 significantly improved the antimicrobial properties of T. ammi sprouts against 11 out of 13 microbial species than control sprouts, which had more potent antimicrobial activities than seeds. The significant increase in the antioxidant potential of treated sprouts was indicated by improved levels of ferric reducing antioxidant power (FRAP), DPPH, and oxygen radical absorbance capacity (ORAC). In addition, the anticancer activity against four different human tumor cell lines was significantly (p < 0.05) boosted by both sprouting and eCO2 exposure. Thus, the present study confirms the synergistic effect of sprouting with eCO2 exposure as promising approaches to produce ajwain sprouts with rich nutraceuticals, effective phytochemicals, and enhanced biological activities.

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Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

10.31221/osf.io/n5xvt ◽

2019 ◽

Author(s):

Chem Int

Keyword(s):

Heterocyclic Compounds ◽

Biological Activities ◽

Wide Spectrum ◽

Biological Properties ◽

Industrial Chemical ◽

Anti Inflammatory ◽

Pyridazinone Derivatives

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.

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The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds

Current Organic Synthesis ◽

10.2174/1570179416666190925162215 ◽

2019 ◽

Vol 16 (7) ◽

pp. 953-967 ◽

Cited By ~ 1

Author(s):

Ghodsi M. Ziarani ◽

Fatemeh Mohajer ◽

Razieh Moradi ◽

Parisa Mofatehnia

Keyword(s):

Biological Activities ◽

Biological Properties ◽

Biologically Active ◽

Microtubule Assembly ◽

Heterocyclic Molecules ◽

Biological Perspective ◽

Highly Active ◽

Anti Inflammatory ◽

High Yields ◽

Short Time

Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

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Competitive Biological Activities of Chitosan and Its Derivatives: Antimicrobial, Antioxidant, Anticancer, and Anti-Inflammatory Activities

International Journal of Polymer Science ◽

10.1155/2018/1708172 ◽

2018 ◽

Vol 2018 ◽

pp. 1-13 ◽

Cited By ~ 30

Author(s):

Suyeon Kim

Keyword(s):

Water Solubility ◽

Biological Activities ◽

Biological Properties ◽

Biomedical Science ◽

Amino Groups ◽

Chitosan Oligosaccharides ◽

Primary Amino ◽

Anti Inflammatory ◽

Key Functional Groups ◽

Application Fields

Chitosan is obtained from alkaline deacetylation of chitin, and acetamide groups are transformed into primary amino groups during the deacetylation. The diverse biological activities of chitosan and its derivatives are extensively studied that allows to widening the application fields in various sectors especially in biomedical science. The biological properties of chitosan are strongly depending on the solubility in water and other solvents. Deacetylation degree (DDA) and molecular weight (MW) are the most decisive parameters on the bioactivities since the primary amino groups are the key functional groups of chitosan where permits to interact with other molecules. Higher DDA and lower MW of chitosan and chitosan derivatives demonstrated higher antimicrobial, antioxidant, and anticancer capacities. Therefore, the chitosan oligosaccharides (COS) with a low polymerization degree are receiving a great attention in medical and pharmaceutical applications as they have higher water solubility and lower viscosity than chitosan. In this review articles, the antimicrobial, antioxidant, anticancer, anti-inflammatory activities of chitosan and its derivatives are highlighted. The influences of physicochemical parameters of chitosan like DDA and MW on bioactivities are also described.

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Antimicrobial Ionic Liquids with Fumarate Anion

Journal of Chemistry ◽

10.1155/2013/473153 ◽

2013 ◽

Vol 2013 ◽

pp. 1-7 ◽

Cited By ~ 7

Author(s):

Biyan He ◽

Guangnan Ou ◽

Changyi Zhou ◽

Meihong Wang ◽

Suyan Chen

Keyword(s):

Ionic Liquids ◽

Antimicrobial Agents ◽

Antimicrobial Properties ◽

Antimicrobial Activities ◽

Biological Properties ◽

Research Field ◽

Potassium Sorbate ◽

Gravimetric Analysis ◽

Antimicrobial Drugs ◽

Active Research

The shortage of new antimicrobial drugs and increasing resistance of microbe to antimicrobial agents have been of some concern. The formulation studies of new antibacterial and antifungal agents have been an active research field. Ionic liquids are known as designed liquids with controllable physical/chemical/biological properties and specific functions, which have been attracting considerable interest over recent years. However, no attention has been made towards the preparation of ionic liquids with antimicrobial activities. In this paper, a new class of ionic liquids (ILs) with fumarate anion was synthesized by neutralization of aqueous 1-butyl-3-methylimidazolium hydroxide with equimolar monoester fumarate and characterized using NMR and thermal gravimetric analysis. The ILs are soluble in water and polar organic solvents and also soluble in the common ILs. The antimicrobial activities of the ILs are more active than commercially available potassium sorbate and are greatly affected by the alkyl chain length. The significant antimicrobial properties observed in this research suggest that the ILs may have potential applications in the modern biotechnology.

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Essential oil from Piperaceae as a potential for biopesticide agents: a review

Food Research ◽

10.26656/fr.2017.4(s5).007 ◽

2020 ◽

Vol 4 (S5) ◽

pp. 1-10

Author(s):

N.A. Abdullah ◽

W.Z.W.M. Zain ◽

H.A. Hamid ◽

N.W. Ramli

Keyword(s):

Secondary Metabolites ◽

Essential Oils ◽

Biological Activities ◽

The United States ◽

Antimicrobial Activities ◽

Biological Properties ◽

Present Information ◽

United States Food ◽

Synthetic Pesticide ◽

States Food

This review is aimed to present information on the properties of Piperaceae which can be potentially used as a biopesticide. The chemical compounds involved in were different as each species consist of different amount of secondary metabolites which then leads to different properties. In recent years, several reports have been published regarding the composition and the biological activities of the essential oils of Piper species. These studies have highlighted the existence of marked chemical differences among oils extracted from different species or varieties. Analysis of volatile constituents from Piperaceae species has revealed the presence of monoterpenes, sesquiterpenes and arylpropanoids that have shown interesting biological properties including cytotoxic, fungistatic, insecticide, molluscicidal, antioxidant and antimicrobial activities. Essential oils are natural complex secondary metabolites characterized by strong odour, volatility and have generally lower density than water. Due to their volatility, essential oils are environmentally non-persistent. On top of that, essential oils are ‘generally recognized as safe’ by the United States Food and Drug Administration (FDA). Since technology has become more advanced, people started to replace synthetic pesticide with bio-pesticide. The demand for EO has increased as it has biological properties that can be used to replace synthetic pesticide

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Phytochemical Screening, Phenolic Compounds Content, Antioxidant, Anti-inflammatory, and Antimicrobial Properties of Pachylobus balsamifera Guillaum from Gabon

Phytothérapie ◽

10.3166/phyto-2018-0059 ◽

2018 ◽

Vol 16 (S1) ◽

pp. S65-S73 ◽

Cited By ~ 1

Author(s):

C. Sima-Obiang ◽

R.L. Ngoua-Meye-Misso ◽

G.R. Ndong-Atome ◽

J. Privat Ondo ◽

L.C. Obame-Engonga ◽

...

Keyword(s):

Phenolic Compounds ◽

Antioxidant Activities ◽

Antimicrobial Properties ◽

Water Extract ◽

Antioxidant Property ◽

Salmonella Typhi ◽

Antimicrobial Activities ◽

Antimicrobial Potential ◽

Anti Inflammatory ◽

Ethanol Extracts

The goal of this work is to evaluate the antioxidant anti-inflammatory properties, the phenolic compounds content, and antimicrobial potential of water–acetone, water–ethanol, and water extracts of Pachylobus balsamifera. The phenolic compounds content was evaluated to estimate their effect on the antioxidant, anti-inflammatory, and antimicrobial potential of the plant. Antioxidant activities were examined by DPPH (2,2-diphenyl-1- picrylhydrazyl) and ABTS (2,2′-azino-bis) assays. Antiinflammatory activity was determined by the proteins denaturation inhibition method. All plant extracts were evaluated against six reference strains, eleven clinical isolates, and two fungal strains. Phenols content was highest in the water–acetone and water–ethanol extracts. The water extract showed strong anti-inflammatory effect. The water–acetone extract presented a strong antioxidant property and the highest antimicrobial activities against Pseudomonas aeruginosa, Acinetobacter baumannii, Salmonella Sp., and Neisseria meningitidis. The tested microorganisms showed sensitivity to all extracts of the plant with the exception of Escherichia coli 105182 CIP, Listeria innocua LMG 135668 BHI, Salmonella enterica, Salmonella typhi, and Neisseria gonorrhea. Our results suggest that Pachylobus balsamifera extracts contain antioxidant, anti-inflammatory, and antimicrobial properties.

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An Overview on Pyranocoumarins: Synthesis and Biological Activities

Current Organic Chemistry ◽

10.2174/1385272823666191025151236 ◽

2020 ◽

Vol 23 (24) ◽

pp. 2679-2721 ◽

Cited By ~ 1

Author(s):

Evangelia-Eirini N. Vlachou ◽

Konstantinos E. Litinas

Keyword(s):

Organic Compounds ◽

Antifungal Agents ◽

Biological Activities ◽

Biological Properties ◽

Pyran Ring ◽

Naturally Occurring ◽

Anti Cancer ◽

Anti Inflammatory ◽

Antibacterial And Antifungal ◽

Anti Hiv

Pyrano- and dipyranocoumarins are classes of naturally occurring organic compounds with very interesting biological activities. This review focuses on the synthetic strategies for the synthesis of pyranocoumarins and dipyranocoumarins and the biological properties of those compounds. The synthesis involves the formation of the pyran ring, at first, from a coumarin or the formation of pyranone moiety from an existing pyran. Pyranocoumarins and dipyranocoumarins present anti-HIV, anti-cancer, neuroprotective, antidiabetic, antibacterial, antifungal, anti-inflammatory activities. Especially khellactones and calanolides are usually potent and selective in anti-HIV activity. Decursin and decursinol derivatives are effective as anticancer, neuroprotective, antidiabetic, antibacterial, and antifungal agents.

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Helenalin - A Sesquiterpene Lactone with Multidirectional Activity

Current Drug Targets ◽

10.2174/1389450119666181012125230 ◽

2019 ◽

Vol 20 (4) ◽

pp. 444-452 ◽

Cited By ~ 5

Author(s):

Joanna Drogosz ◽

Anna Janecka

Keyword(s):

Sesquiterpene Lactone ◽

Molecular Mechanisms ◽

Biological Activities ◽

Sesquiterpene Lactones ◽

Folk Medicine ◽

Biological Properties ◽

Pathological Conditions ◽

Anti Cancer ◽

Anti Inflammatory ◽

Minor Injuries

Sesquiterpene lactones, secondary metabolites of plants, present in a large number of species mostly from the Asteracea family, are used in the traditional medicine of many countries for the treatment of various pathological conditions. They exert a broad range of activities, including antiinflammatory, anti-bacterial and anti-cancer properties. The best-known sesquiterpene lactones which are already used as drugs or are used in clinical trials are artemisinin, thapsigargin and parthenolide. Yet another sesquiterpene lactone, helenalin, an active component of Arnica montana, known for its strong anti-inflammatory activity, has been used for centuries in folk medicine to treat minor injuries. Unfortunately, helenalin’s ability to cause allergic reactions and its toxicity to healthy tissues prevented so far the development of this sesquiterpene lactone as an anticancer or anti-inflammatory drug. Recently, the new interest in the biological properties, as well as in the synthesis of helenalin analogs has been observed. This review describes helenalin's major biological activities, molecular mechanisms of action, its toxicity and potential for further research.

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A Review on Recent Developments in the Anticancer Potential of Oleanolic acid and its analogs (2017-2020)

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557521666210810153627 ◽

2021 ◽

Vol 21 ◽

Author(s):

Nidhi Gupta

Keyword(s):

Clinical Trials ◽

Natural Product ◽

Oleanolic Acid ◽

Anticancer Agents ◽

Biological Activities ◽

Pentacyclic Triterpenoid ◽

Recent Developments ◽

Anti Inflammatory ◽

Pharmaceutical Properties

: Oleanolic acid (OA) is a pentacyclic triterpenoid class of natural product known to possess a broad range of biological activities, specifically, anticancer. Considering the anticancer potential of OA, a large number of analogs have been prepared by several researchers through modifications at C-3, C-12 and C-28 –COOH to develop the potent anticancer agents with improved cytotoxicity and pharmaceutical properties. Some of the synthesized derivatives have been assessed in clinical trials also. This review summarizes the most recent synthetic and biological efforts in the development of oleanolic acid and its analogs during the period 2017-2020. Reports published during this period revealed that both OA and its analogs possess a remarkable potential for the development of effective anticancer agents along with several others such as anti-inflammatory, anti-viral, anti-microbial and anti-diabetic agents.

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