1,4-Diazepines: A Review on Synthesis, Reactions and Biological Significance

Background:1,4-Diazepines are two nitrogen containing seven membered heterocyclic compounds and associated with a wide range of biological activities. Due to its medicinal importance, scientists are actively involved in the synthesis, reactions and biological evaluation of 1,4-diazepines since number of decades.Objective:The primary purpose of this review is to discuss the synthetic schemes and reactivity of 1,4- diazepines. This article also describes biological aspects of 1,4-diazepine derivatives, that can be usefully exploited for the pharmaceutical sector.Conclusion:This review summarizes the abundant literature on synthetic routes, chemical reactions and biological attributes of 1,4-diazepine derivatives. We concluded that 1,4-diazepines have significant importance due to their biological activities like antipsychotic, anxiolytic, anthelmintic, anticonvulsant, antibacterial, antifungal and anticancer. 1,4-diazepine derivatives with significant biological activities could be explored for potential use in the pharmaceutical industries.

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Chain-breaking/Preventive Antioxidant, Urate-lowering, and Anti-inflammatory Effects of Pure Curcumin

Current Nutrition & Food Science ◽

10.2174/1573401316999200421095134 ◽

2020 ◽

Vol 17 (1) ◽

pp. 66-74

Author(s):

Seghira Bisset ◽

Widad Sobhi ◽

Chawki Bensouici ◽

Abdelhalim Khenchouche

Keyword(s):

Uric Acid ◽

Xanthine Oxidase ◽

Acid Production ◽

Biological Activities ◽

Antioxidant Effect ◽

Metal Chelating ◽

Wide Range ◽

Chain Breaking ◽

Pharmaceutical Industries ◽

Anti Inflammatory

Background: Several researches have shown that therapeutic compounds or phytochemicals from natural sources are important in the food as it is valuable in pharmaceutical industries due to their fewer side effects and potent against various diseases. Curcumin, a major polyphenol derived from turmeric spice, which used in many foods, has a wide range of biological activities, with quite a safety. Objective: The goal of this study was to investigate the antioxidant, urate-lowering, and antiinflammatory effects of pure curcumin. Methods: The antioxidant activity was evaluated for chain-breaking antioxidant effect (radicalscavenging and reducing abilities assays) and for preventive antioxidant effect with metal chelating assay, the urate-lowering was assayed on aspectrophotometer by measuring the inhibition of uric acid production by xanthine oxidase (XO) enzyme, and the anti-inflammatory effect was estimated using in vitro albumin denaturation inhibition. Results: Curcumin showed a significant and good chain-breaking antioxidant effect, both in free radical- scavenging assays (Galvinoxyl radical, ABTS, and hydroxyl radical), and in reducing abilities methods (reducing power, Cupric ion reducing antioxidant capacity and O-phenanthroline assays). In preventive antioxidant effect, assessed with the metal chelating assay, curcumin showed significant effect but with high concentration compared with standard. In the xanthine/xanthine oxidase system, curcumin significantly inhibited uric acid production (IC50=0.71 ± 0.06 mg/mL). Regarding antiinflammatory activity, curcumin showed significant inhibition of albumin denaturation with an IC50 value of 1181.69 ± 1.11μg/mL. Conclusion: These results indicated that curcumin showed promising antioxidant, anti-gout and antiinflammatory properties and might be used as potential, natural drugs against oxidative and inflammation- related diseases.

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Non-Nucleoside Agonists of the Adenosine Receptors: An Overview

Pharmaceuticals ◽

10.3390/ph12040150 ◽

2019 ◽

Vol 12 (4) ◽

pp. 150 ◽

Cited By ~ 3

Author(s):

Dal Ben ◽

Lambertucci ◽

Buccioni ◽

Martí Navia ◽

Marucci ◽

...

Keyword(s):

Adenosine Receptors ◽

Biological Activities ◽

Great Majority ◽

Synthetic Route ◽

Wide Range ◽

Pharmacological Interest ◽

Molecular Modeling Studies ◽

Synthetic Routes ◽

Alternative Set ◽

Structural Classes

Potent and selective adenosine receptor (AR) agonists are of pharmacological interest for the treatment of a wide range of diseases and conditions. Among these derivatives, nucleoside-based agonists represent the great majority of molecules developed and reported to date. However, the limited availability of compounds selective for a specific AR subtype (i.e., A2BAR) and a generally long and complex synthetic route for largely substituted nucleosides are the main drawbacks of this category of molecules. Non-nucleoside agonists represent an alternative set of compounds able to stimulate the AR function and based on simplified structures. This review provides an updated overview on the structural classes of non-nucleoside AR agonists and their biological activities, with emphasis on the main derivatives reported in the literature. A focus is also given to the synthetic routes employed to develop these derivatives and on molecular modeling studies simulating their interaction with ARs.

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Recent Advancement of Pyrazole Scaffold Based Neuroprotective Agents: A Review

CNS & Neurological Disorders - Drug Targets ◽

10.2174/1871527320666210602152308 ◽

2021 ◽

Vol 20 ◽

Author(s):

Subham Das ◽

Saleem Akbar ◽

Bahar Ahmed ◽

Rikeshwar Prasad Dewangan ◽

Mohammad Kashif Iqubal ◽

...

Keyword(s):

Biological Activities ◽

Neuroprotective Agents ◽

Wide Range ◽

Recent Developments ◽

Ic50 Values ◽

Structural Activity Relationship ◽

Pharmaceutical Industries ◽

Neurological Conditions ◽

Nitrogen Containing Compounds

: As a source of therapeutic agents, heterocyclic nitrogen-containing compounds and their derivatives are still interesting and essential. Pyrazole, a five-member heteroaromatic ring with two nitrogen atoms, has a major impact on chemical industries as well as pharmaceutical industries. Due to its wide range of biological activities against various diseases, it has been identified as a biologically important heterocyclic scaffold. The treatment of neurological disorders has always been a difficult task. Therefore, identifying therapeutically effective molecules for neurological conditions remains an open challenge in biomedical research and development. For developing novel entities as neuroprotective agents, recently, pyrazole scaffold has attracted medicinal chemists worldwide. The major focus of research in this area is to discover novel molecules as neuroprotective agents with minimal adverse effects and better effectiveness in improving the neurological condition. This review mainly covers recent developments in the neuropharmacological role of pyrazole incorporated compounds, including their structural-activity relationship (SAR), which also further includes IC50 values (in mM as well as in μM), recent patents, and a brief history as neuroprotective agents.

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Room Temperature Synthesis and Antibacterial Activity of New Sulfonamides Containing N,N-Diethyl-Substituted Amido Moieties

International Journal of Medicinal Chemistry ◽

10.1155/2012/367815 ◽

2012 ◽

Vol 2012 ◽

pp. 1-13 ◽

Cited By ~ 2

Author(s):

Olayinka O. Ajani ◽

Oluwole B. Familoni ◽

Feipeng Wu ◽

Johnbull O. Echeme ◽

Zheng Sujiang

Keyword(s):

Antibacterial Activity ◽

Mass Spectra ◽

Room Temperature ◽

Biological Activities ◽

Chemical Structures ◽

Wide Range ◽

Synthetic Routes ◽

Mic Value ◽

C Nmr

Sulfonamide drugs which have brought about an antibiotic revolution in medicine are associated with a wide range of biological activities. We have synthesized a series of α-tolylsulfonamide, 1–11 and their substituted N,N-diethyl-2-(phenylmethylsulfonamido) alkanamide derivatives, 12–22 in improved and excellent yields in aqueous medium at room temperature through highly economical synthetic routes. The chemical structures of the synthesized compounds 1–22 were confirmed by analytical and spectral data such as IR, 1H- and 13C-NMR, and mass spectra. The in vitro antibacterial activity of these compounds along with standard clinical reference, streptomycin, was investigated on two key targeted organisms. It was observed that 1-(benzylsulfonyl)pyrrolidine-2-carboxylic acid, 2 emerged as the most active compound against Staphylococcus aureus at MIC value of 1.8 μg/mL while 4-(3-(diethylamino)-3-oxo-2-(phenylmethylsulfonamido) propyl)phenyl phenylmethanesulfonate, 22 was the most active sulfonamide scaffold on Escherichia coli at MIC value of 12.5 μg/mL.

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Acetylcholine esterase inhibitory activity of green synthesized nanosilver by naphthopyrones isolated from marine-derived Aspergillus niger

PLoS ONE ◽

10.1371/journal.pone.0257071 ◽

2021 ◽

Vol 16 (9) ◽

pp. e0257071

Author(s):

Ghada Mahmoud Abdelwahab ◽

Amira Mira ◽

Yuan-Bin Cheng ◽

Tarek A. Abdelaziz ◽

Mohamed Farid I. Lahloub ◽

...

Keyword(s):

Aspergillus Niger ◽

Inhibitory Activity ◽

Active Sites ◽

Biological Activities ◽

Biological Properties ◽

Biological Evaluation ◽

Acetylcholine Esterase ◽

Protective Effects ◽

Wide Range ◽

First Time

Aspergillus niger metabolites exhibited a wide range of biological properties including antioxidant and neuro-protective effects and some physical properties as green synthesis of silver nanoparticles AgNP. The present study presents a novel evidence for the various biological activities of green synthesized AgNPs. For the first time, some isolated naphtho-γ-pyrones from marine-derived Aspergillus niger, flavasperone (1), rubrofusarin B (2), aurasperone A (3), fonsecinone A (4) in addition to one alkaloid aspernigrin A (7) were invistigated for their inhibitory activity of acetylcholine esterase AChE, a hallmark of Alzheimer’s disease (AD). The ability to synthesize AgNPs by compounds 3, 4 and 7 has been also tested for the first time. Green synthesized AgNPs were well-dispersed, and their size was ranging from 8–30 nm in diameter, their morphology was obviously spherical capped with the organic compounds. Further biological evaluation of their AChE inhibitory activity was compared to the parent compounds. AgNps dramatically increased the inhibitory activity of Compounds 4, 3 and 7 by 84, 16 and 13 fold, respectively to be more potent than galanthamine as a positive control with IC50 value of 1.43 compared to 0.089, 0.311 and 1.53 of AgNPs of Compounds 4, 3 and 7, respectively. Also compound 2 showed moderate inhibitory activity. This is could be probably explained by closer fitting to the active sites or the synergistic effect of the stabilized AgNPs by the organic compouds. These results, in addition to other intrinsic chemical and biological properties of naphtho-γ-pyrones, suggest that the latter could be further explored with a view towards other neuroprotective studies for alleviating AD.

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Recent advances on oxadiazole motifs: Synthesis, reactions and biological activities

Mediterranean Journal of Chemistry ◽

10.13171/mjc10502005121200ooa ◽

2020 ◽

Vol 10 (5) ◽

pp. 418

Author(s):

Olayinka Oyewale Ajani ◽

King T. Iyaye

Keyword(s):

Industrial Development ◽

Medicinal Chemistry ◽

Light Emitting Diodes ◽

Biological Activities ◽

Light Emitting ◽

Oxadiazole Derivatives ◽

Synthetic Routes ◽

High Yields ◽

Synthesis Reactions ◽

Very High

<p>1,3,4-oxadiazole derivatives have shown to have diverse and vast applications, from medicinal chemistry for the treatment and possible treatment of various ailments to its application in the industrial development when used as corrosion inhibitions and light emitting diodes. These diverse applications can be as a result of the numerous viable synthetic pathways illustrated in this review. 1,3,4-oxadiazoles can be synthesized in very high yields, using green approaches and having various life-changing applications. This review explores the various recent synthetic routes available for the development of 1,3,4-oxadiazoles and their biological activities.</p>

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Anti-oxidant and in-vitro alpha amylase inhibitory activities of leaves and barks of Randia dumetorum

10.1101/2020.08.10.244236 ◽

2020 ◽

Author(s):

Deepak Timalsina

Keyword(s):

Biological Activities ◽

Food Poisoning ◽

Biologically Active ◽

Alpha Amylase ◽

Methanolic Extracts ◽

Therapeutic Uses ◽

Wide Range ◽

Pharmaceutical Industries ◽

The Rich

AbstractThe process of drug discovery and development in the world over a recent year has been increasingly shaped by the formulaic approaches and natural products, prioritized by popular pharmaceutical industries. In many countries like Nepal, Randia dumetorum (Maidal) is one of the popular alternatives for overcoming various symptoms such as acidity, food poisoning ulcers, diabetes and ulcers. It has been using by the people because of its wide range of therapeutic uses. Though, the considerable research had been conducted to reveal the biologically active compounds and its pharmacological effect, the rich constituent of this plant and its major biological perspective was yet to be studied comprehensively. Accordingly, the main focus of this study was the alpha amylase inhibition of methanolic extracts obtained from leaves and barks of Randia dumetorum plant. The plant extracts were obtained by dissolving dried plant with 100% methanol overnight and evaporating to the dryness. The obtained plant extract was used to study mentioned biological activities. The results obtained showed that the extract obtained from leaves and barks showed antioxidant and alpha amylase inhibition activities. This research can be helpful to discover new types of therapeutics in the future.

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Halogenated Flavones and Isoflavones: A State-of-Art on their Synthesis

Current Organic Synthesis ◽

10.2174/1570179417666200530213737 ◽

2020 ◽

Vol 17 (6) ◽

pp. 415-425

Author(s):

Ricardo Santos ◽

Diana Pinto ◽

Clara Magalhães ◽

Artur Silva

Keyword(s):

Biological Activities ◽

New Drugs ◽

Reaction Conditions ◽

Balanced Diet ◽

Wide Range ◽

The Everyday ◽

Synthetic Routes ◽

Scopus Database ◽

Reported Data ◽

Synthetic Approaches

Background: Flavonoid is a family of compounds present in the everyday consumption plants and fruits, contributing to a balanced diet and beneficial health effects. Being a scaffold for new drugs and presenting a wide range of applicability in the treatment of illnesses give them also an impact in medicine. Among the several types of flavonoids, flavone and isoflavone derivatives can be highlighted due to their prevalence in nature and biological activities already established. The standard synthetic route to obtain both halogenated flavones and isoflavones is through the use of already halogenated starting materials. Halogenation of the flavone and isoflavone core is less common because it is more complicated and involves some selectivity issues. Objective: Considering the importance of these flavonoids, we aim to present the main and more recent synthetic approaches towards their halogenation. Methods: The most prominent methodologies for the synthesis of halogenated flavones and isoflavones were reviewed. A careful survey of the reported data, using mainly the Scopus database and halogenation, flavones and isoflavones as keywords, was conducted. Results: Herein, a review is provided on the latest and more efficient halogenation protocols of flavones and isoflavones. Selective halogenation and the greener methodologies, including enzymatic and microbial halogenations, were reported. Nevertheless, some interesting protocols that allowed the synthesis of halogenated flavone and isoflavone derivatives in specific positions using halogenated reagents are also summarized. Conclusion: Halogenated flavones and isoflavones have risen as noticeable structures; however, most of the time, the synthetic procedures involve toxic reagents and harsh reaction conditions. Therefore, the development of new synthetic routes with low environmental impact is desirable.

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Design, Synthesis and Biological Evaluation of the Novel Antitumor Agent Aurone Derivatives

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.781-784.1235 ◽

2013 ◽

Vol 781-784 ◽

pp. 1235-1239

Author(s):

Qian Nan Guo ◽

Lei Lv ◽

Yao Zhou ◽

Peng Yu ◽

Yuou Teng

Keyword(s):

Biological Activities ◽

Antitumor Agent ◽

Biological Evaluation ◽

The Novel ◽

Pharmacological Activities ◽

Design Synthesis ◽

H Nmr ◽

Wide Range ◽

Inhibitory Activities ◽

Synthesis And Biological Evaluation

Aurones belong to a class of heterocyclic flavonoids which contains a benzofuran element associated with a benzylidene linked in position 2. Aurones possess a wide range of pharmacological activities and biological activities, such as antitumor, antifungal, phytoalexin and so on. A novel series of 2-ayl-yl (5-methacrylate) aurone analogues were synthesized in six steps with the overall yield of 11%-13% and characterized by 1H NMR. Among the key intermediates and target compounds, 2-(2-furan-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7a) and 2-(2-thienyl-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7b) have never been reported before. Primary biological activities evaluation showed that 7a exhibited good inhibitory activities against K562 with an IC50 of 2.18 μM and against HepG2 with an IC50 of 3.95μM.

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Biological Aspects of Emerging Benzothiazoles: A Short Review

Journal of Chemistry ◽

10.1155/2013/345198 ◽

2013 ◽

Vol 2013 ◽

pp. 1-12 ◽

Cited By ~ 19

Author(s):

Ruhi Ali ◽

Nadeem Siddiqui

Keyword(s):

Heterocyclic Compounds ◽

Scientific Literature ◽

Biological Activities ◽

Research Work ◽

Short Review ◽

Biological Properties ◽

Therapeutic Agents ◽

Benzothiazole Derivatives ◽

Wide Range ◽

Biological Aspects

In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Benzothiazole is among the usually occurring heterocyclic nuclei in many marine as well as natural plant products. Benzothiazole is a privileged bicyclic ring system with multiple applications. It is known to exhibit a wide range of biological properties including anticancer, antimicrobial, and antidiabetic, anticonvulsant, anti-inflammatory, antiviral, antitubercular activities. A large number of therapeutic agents are synthesized with the help of benzothiazole nucleus. During recent years there have been some interesting developments in the biological activities of benzothiazole derivatives. These compounds have special significance in the field of medicinal chemistry due to their remarkable pharmacological potentialities. This review is mainly an attempt to present the research work reported in the recent scientific literature on different biological activities of benzothiazole compounds.

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