scholarly journals Synthesis and antibacterial activities of quinazolin-4(3h)-one, 2-methyl-4(3h)-quinazolinone and 2–phenyl-4(3h)-quinazolinone

2021 ◽  
Vol 1 (2) ◽  
pp. 077-084
Author(s):  
Peter Osarodion Osarumwense ◽  
Mary Olire Edema ◽  
Cyril Odianosen Usifoh
Keyword(s):  
Biological Activities ◽  
Cyclic Compound ◽  
Antibacterial Activities ◽  
Biologically Active ◽  
Klebsiella Pneumonia ◽  
Active Nitrogen ◽  
Diverse Range ◽  
Methyl Group ◽  
Quinazolinone Derivatives

Background: Quinazoline and quinazolinone scaffolds represent an important class of biologically active nitrogen heterocyclic compounds. Many marketed drugs are based on these moieties. A diverse range of molecules with quinazoline/quinazolinone moieties have been reported to exhibit broad spectrum of biological activities Objective: This study is aimed at the synthesis of these quinazolinone derivatives, quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one and evaluate them for their antibacterial activities. Method: The consolidation of 2-amino-methyl-4-methoxybenzoate with acetic anhydride produced the cyclic compound 2-methyl-4, 5-disubstituted-1, 3-benzo-oxazine-4-one which also produce a novel 2,3-disubstituted quinazolin-4 ones via the reaction with hydrazine hydrate. The quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds synthesized were assuredly validated by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography Mass Spectrophotometer and Elemental analysis. The synthesized compounds were tested for their antibacterial activity.Compounds 1,2 and 3 showed significant antibacterial activities. Discussion: Compound 1 was identified by the absence of methyl group and the presence of methyl group for compound 2. The test analysed compounds exhibited significant antibacterial activities. The compounds synthesized exhibited promising antibacterial activities against the tested organisms. Conclusion: The compounds have high antibacterial activities. Compound 2 has a higher activity compared to Compound 1 and 3. Compound 2 has a higher antibacterial against Escherichia coli, Klebsiella pneumonia and Pseudomonas aeuriginosa

scholarly journals Synthesis And Anagesic activities of Quinazolin-4(3H)-One, 2-Methyl-4(3H)-Quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one

2020 ◽  
Vol 10 (4-s) ◽  
pp. 87-91
Author(s):  
P.O. Osarumwense ◽  
M.O. Edema ◽  
C.O. Usifoh
Keyword(s):  
Nuclear Magnetic Resonance ◽  
Analgesic Activity ◽  
Cyclic Compound ◽  
Test Sample ◽  
Control Test ◽  
Methyl Group ◽  
Analgesic Activities ◽  
Quinazolinone Derivatives ◽  
Activity Method

Background: Objective: The current study is aimed at the synthesis of these quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one and evaluate them for their analgesic activity. Method: The condensation of 2-amino-methyl-4-methoxybenzoate with acetic anhydride yielded the cyclic compound 2-methyl-4, 5-disubstituted-1, 3-benzo-oxazine-4-one which further produce a novel 2,3-disubstituted quinazolin-4 ones via the reaction with hydrazine hydrate The quinazolinone derivatives quinazolin-4(3H)-One,  2-Methyl-4(3H)-quinazolinone  and 2–Phenyl-4(3H)-quinazolin-4(3H)–one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds synthesized were unequivocally confirmed by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography Mass Spectrophotometer and Elemental analysis.The synthesized compounds were screened for their analgesic activity.Compounds 1,2 and 3 showed significant analgesic activity. Discussion: Compound 1 was characterized by the absence of methyl group and the presence of methyl group for compound 2. The test investigated compounds exhibited significant analgesic activity when compared with the control test sample. The compounds  synthesized  exhibited promising analgesic  activities against .  Conclusion: The compounds have high analgesic activity. Compound 3 has a higher activity  compared to Compound 2 and compound 2 has a higher analgesic activity compared to compound  1.  Compound 3 has a higher analgesic activity compared to the standard drugs Aspirin and Indomethacin. Keywords:  quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one quinazolin-4(3H)-one, analgesic activity.

Metabolomics of Healthy Berry Fruits

2019 ◽  
Vol 25 (37) ◽  
pp. 4888-4902 ◽  
Author(s):  
Gilda D'Urso ◽  
Sonia Piacente ◽  
Cosimo Pizza ◽  
Paola Montoro
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Bioactive Metabolites ◽  
Active Metabolites ◽  
Positive Effects ◽  
Cell Functions ◽  
Berry Fruits

The consumption of berry-type fruits has become very popular in recent years because of their positive effects on human health. Berries are in fact widely known for their health-promoting benefits, including prevention of chronic disease, cardiovascular disease and cancer. Berries are a rich source of bioactive metabolites, such as vitamins, minerals, and phenolic compounds, mainly anthocyanins. Numerous in vitro and in vivo studies recognized the health effects of berries and their function as bioactive modulators of various cell functions associated with oxidative stress. Plants have one of the largest metabolome databases, with over 1200 papers on plant metabolomics published only in the last decade. Mass spectrometry (MS) and NMR (Nuclear Magnetic Resonance) are the most important analytical technologies on which the emerging ''omics'' approaches are based. They may provide detection and quantization of thousands of biologically active metabolites from a tissue, working in a ''global'' or ''targeted'' manner, down to ultra-trace levels. In the present review, we highlighted the use of MS and NMR-based strategies and Multivariate Data Analysis for the valorization of berries known for their biological activities, important as food and often used in the preparation of nutraceutical formulations.

Arylpyrazoles: Heterocyclic Scaffold of Immense Therapeutic Application

2020 ◽  
Vol 24 (14) ◽  
pp. 1555-1581
Author(s):  
Garima Tripathi ◽  
Anil Kumar Singh ◽  
Abhijeet Kumar
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
Present Review ◽  
Pyrazole Derivatives ◽  
Therapeutic Application ◽  
Diverse Range ◽  
Major Class ◽  
Anti Inflammatory

Among the major class of heterocycles, the N-heterocycles, such as pyrazoles, are scaffolds of vast medicinal values. Various drugs and other biologically active molecules are known to contain these N-heterocycles as core motifs. Specifically, arylpyrazoles have exhibited a diverse range of biological activities, including anti-inflammatory, anticancerous, antimicrobial and various others. For instance, arylpyrazoles are present as core moieties in various insecticides, fungicides and drugs such as Celebrex and Trocoxil. The present review will be highlighting the significant therapeutic importance of pyrazole derivatives developed in the last few years.

scholarly journals Constitutive and Regulated Shedding of Soluble FGF Receptors Releases Biologically Active Inhibitors of FGF-2

2021 ◽  
Vol 22 (5) ◽  
pp. 2712
Author(s):  
Anne Hanneken ◽  
Maluz Mercado ◽  
Pamela Maher
Keyword(s):  
Cell Surface ◽  
Ligand Binding ◽  
Cellular Proliferation ◽  
Biological Activities ◽  
Biological Properties ◽  
Matrix Metalloproteases ◽  
Biologically Active ◽  
Ectodomain Shedding ◽  
High Affinity

The identification of soluble fibroblast growth factor (FGF) receptors in blood and the extracellular matrix has led to the prediction that these proteins modulate the diverse biological activities of the FGF family of ligands in vivo. A recent structural characterization of the soluble FGF receptors revealed that they are primarily generated by proteolytic cleavage of the FGFR-1 ectodomain. Efforts to examine their biological properties are now focused on understanding the functional consequences of FGFR-1 ectodomain shedding and how the shedding event is regulated. We have purified an FGFR-1 ectodomain that is constitutively cleaved from the full-length FGFR-1(IIIc) receptor and released into conditioned media. This shed receptor binds FGF-2; inhibits FGF-2-induced cellular proliferation; and competes with high affinity, cell surface FGF receptors for ligand binding. FGFR-1 ectodomain shedding downregulates the number of high affinity receptors from the cell surface. The shedding mechanism is regulated by ligand binding and by activators of PKC, and the two signaling pathways appear to be independent of each other. Deletions and substitutions at the proposed cleavage site of FGFR-1 do not prevent ectodomain shedding. Broad spectrum inhibitors of matrix metalloproteases decrease FGFR-1 ectodomain shedding, suggesting that the enzyme responsible for constitutive, ligand-activated, and protein kinase C-activated shedding is a matrix metalloprotease. In summary, shedding of the FGFR-1 ectodomain is a highly regulated event, sharing many features with a common system that governs the release of diverse membrane proteins from the cell surface. Most importantly, the FGFR ectodomains are biologically active after shedding and are capable of functioning as inhibitors of FGF-2.

Sixty Years Young: The Diverse Biological Activities of Metal Polypyridyl Complexes Pioneered by Francis P. Dwyer

2012 ◽  
Vol 65 (9) ◽  
pp. 1325 ◽  
Author(s):  
Nathan L. Kilah ◽  
Eric Meggers
Keyword(s):  
Inorganic Chemistry ◽  
Biological Activities ◽  
Biologically Active ◽  
Ruthenium Polypyridyl ◽  
Polypyridyl Complexes ◽  
Anti Cancer ◽  
Ruthenium Polypyridyl Complexes ◽  
Medicinal Inorganic Chemistry ◽  
Sixtieth Anniversary

Sixty years ago, the Australian chemist Francis P. Dwyer pioneered the use of ruthenium polypyridyl complexes as biologically active compounds. These chemically inert and configurationally stable complexes revealed an astonishing range of interesting biological activities, such as the inhibition of the enzyme acetylcholinesterase, anti-cancer activity in vivo, and bacteriostatic/bacteriocidal action. This review commemorates the sixtieth anniversary of Dwyer and co-workers’ landmark 1952 publication, summarises their broader achievements in biological inorganic chemistry, and discusses the contribution of this work to the development of modern biological and medicinal inorganic chemistry.

scholarly journals Chromatographic Analyses, In Vitro Biological Activities, and Cytotoxicity of Cannabis sativa L. Essential Oil: A Multidisciplinary Study

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3266 ◽  
Author(s):  
Gokhan Zengin ◽  
Luigi Menghini ◽  
Antonella Di Sotto ◽  
Romina Mancinelli ◽  
Francesca Sisto ◽  
...  
Keyword(s):  
Essential Oil ◽  
Galleria Mellonella ◽  
Cannabis Sativa ◽  
Biological Activities ◽  
Methodological Approach ◽  
Volatile Component ◽  
Biologically Active ◽  
Antioxidant Compounds

Due to renewed interest in the cultivation and production of Italian Cannabis sativa L., we proposed a multi-methodological approach to explore chemically and biologically both the essential oil and the aromatic water of this plant. We reported the chemical composition in terms of cannabinoid content, volatile component, phenolic and flavonoid pattern, and color characteristics. Then, we demonstrated the ethnopharmacological relevance of this plant cultivated in Italy as a source of antioxidant compounds toward a large panel of enzymes (pancreatic lipase, α-amylase, α-glucosidase, and cholinesterases) and selected clinically relevant, multidrug-sensible, and multidrug-resistant microbial strains (Staphylococcus aureus, Helicobacter pylori, Candida, and Malassezia spp.), evaluating the cytotoxic effects against normal and malignant cell lines. Preliminary in vivo cytotoxicity was also performed on Galleria mellonella larvae. The results corroborate the use of this natural product as a rich source of important biologically active molecules with particular emphasis on the role exerted by naringenin, one of the most important secondary metabolites.

scholarly journals Antibacterial Potential of Jatropha sp. Latex against Multidrug-Resistant Bacteria

2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Muhammad Evy Prastiyanto ◽  
Prayoda Deri Tama ◽  
Ninda Ananda ◽  
Wildiani Wilson ◽  
Ana Hidayati Mukaromah
Keyword(s):  
Agar Plate ◽  
Antibacterial Activities ◽  
Multidrug Resistant ◽  
Blood Agar Plate ◽  
Diffusion Method ◽  
Resistant Bacteria ◽  
Klebsiella Pneumonia ◽  
Extended Spectrum Beta Lactamase ◽  
Mueller Hinton

Objective. This study was aimed to evaluate the antibacterial activity of the latex of three species members of Jatropha (J. curcas, J. gossypilofia Linn., and J. multifida) against methicillin-resistant Staphylococcus aureus (MRSA), extended-spectrum beta-lactamase- (ESBL-) producing Escherichia coli and ESBL-producing Klebsiella pneumonia, carbapenemase-resistant Enterobacteriaceae (CRE)-E. coli, K. pneumoniae-carbapenemase (KPC), and carbapenemase-resistant Pseudomonas aeruginosa (CRPA). Method. The antibacterial activities were calculated based on the inhibition zones using the Mueller–Hinton agar diffusion method, minimum inhibitory concentration (MIC) using Mueller–Hinton broth in a microdilution method, and minimum bactericidal concentration (MBC) using blood agar plate. Results. The latex of Jatropha showed antibacterial activities against the MRSA and CRPA. All latex of Jatropha appeared to have the antibacterial activities against MRSA and CRPA in the diffusion method (20.4–23.7 mm and 12–15 mm), MIC (0.19–6.25%, and 25%), and MBC (0.39–12.5% and 50%). Phytochemical screening of latex indicated the presence of flavonoids. Conclusions. The latex of J. curcas, J. gossypilofia Linn., and J. multifida has the potential to be developed as antibacterial agents, especially against MRSA and CRPA strain, but further in vivo research and discovery of the mode of its action are required to shed the light on the effects.

scholarly journals Bee Venom: From Venom to Drug

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4941
Author(s):  
Abdelwahab Khalil ◽  
Basem H. Elesawy ◽  
Tarek M. Ali ◽  
Osama M. Ahmed
Keyword(s):  
Molecular Mechanisms ◽  
Biological Activities ◽  
Biologically Active ◽  
Bee Venom ◽  
Bee Sting ◽  
Anti Cancer ◽  
Defensive Substance ◽  
Injectable Form

Insects of the order Hymenoptera have a defensive substance that contains many biologically active compounds. Specifically, venom from honeybees (Apis mellifera) contains many enzymes and peptides that are effective against various diseases. Different research papers stated the possibility of using bee venom (a direct bee sting or in an injectable form) in treating several complications; either in vivo or in vitro. Other reports used the active fractions of bee venom clinically or at labratory scale. Many reports and publications have stated that bee venom and its constituents have multiple biological activities including anti-microbial, anti-protozoan, anti-cancer, anti-inflammatory, and anti-arthritic properties. The present review aims to refer to the use of bee venom itself or its fractions in treating several diseases and counteracting drug toxicities as an alternative protocol of therapy. The updated molecular mechanisms of actions of bee venom and its components are discussed in light of the previous updated publications. The review also summarizes the potential of venom loaded on nanoparticles as a drug delivery vehicle and its molecular mechanisms. Finally, the products of bee venom available in markets are also demonstrated.

scholarly journals Traditional Uses, Phytochemical Constituents and Pharmacological Properties of Averrhoa carambola L.: A Review

2021 ◽  
Vol 12 ◽  
Author(s):  
Fei Luan ◽  
Lixia Peng ◽  
Ziqin Lei ◽  
Xiyu Jia ◽  
Junbo Zou ◽  
...  
Keyword(s):  
Pharmaceutical Industry ◽  
Functional Food ◽  
Therapeutic Potential ◽  
Southern China ◽  
Biological Activities ◽  
Biologically Active ◽  
Averrhoa Carambola ◽  
Valuable Treatment

Averrhoa carambola L. (star fruit) is an edible fruit that is extensively cultivated in southern China, Southeast Asia, India, and northern South America. It has a sweet and juicy taste and is frequently used in fruit salads and fruit platters, as a garnish in cocktail drinks and beverages, or squeezed into juice and served as a beverage. Traditionally, it has been used for treating diabetes and diabetic nephropathy, arthralgia, vomiting, lithangiuria, coughing, hangovers, and chronic paroxysmal headache for thousands of years. Currently, approximately 132 compounds have been isolated from A. carambola. Among them, flavonoids, benzoquinone, and their glycosides have been considered as biologically active substances, which are responsible for various biological activities. Pharmacological studies have revealed that crude extracts or monomeric compounds from A. carambola exhibit multiple bioactivities, such as anti-oxidant, anti-hyperglycemic, anti-obesity, anti-hyperlipidemic, anti-tumor, anti-inflammatory, hepatoprotective, cardioprotective, anti-hypertensive, neuroprotective, and others. Thus, A. carambola is a valuable treatment in Chinese medicine with therapeutic potential for multiple diseases, especially diabetes and diabetes-related diseases. Even though it is a very promising candidate in the development of functional food and the pharmaceutical industry, reports on its bioactivities have only been conducted in vivo and in vitro and there is a gap in research regarding clinical settings and safety. This review therefore provides a comprehensive and systematic overview of current progress on botany, ethnopharmacology, phytochemistry, pharmacology, and toxicity of A. carambola, providing a valuable reference for further developments and applications of A. carambola in the pharmaceutical industry and functional food.

Synthesis and In silico Studies of Quinazolinone Derivatives as PARP-1 Inhibitors

2020 ◽  
Vol 17 (12) ◽  
pp. 1552-1565
Author(s):  
Sonia Verma ◽  
Akashdeep Singh Pathania ◽  
Somesh Baranwal ◽  
Pradeep Kumar
Keyword(s):  
In Silico ◽  
Biological Activities ◽  
Docking Studies ◽  
Biologically Active ◽  
Reference Drug ◽  
Drug Candidates ◽  
In Silico Studies ◽  
Antileishmanial Activities ◽  
Quinazolinone Derivatives ◽  
Parp 1

Background: Cancer is a leading cause of deaths worldwide, accounting for 9.6 million deaths in 2018. According to the WHO, the most common causes of cancer deaths are lung, colorectal, stomach liver and breast cancer. Introduction: PARP-1 has a crucial role in cell proliferation, survival and death due to its role in the regulation of multiple biological processes. Quinazolinone and its derivatives represent a large class of biologically active compounds that exhibit a broad spectrum of biological activities such as anti-HIV, anticancer, antifungal, antibacterial, anticonvulsant, anti-inflammatory, antidepressant, antimalarial, antioxidant and antileishmanial activities. Methods: In this study, we have synthesized quinazolinone derivatives by reaction of 2- aminobenzamide and substituted benzaldehydes. The synthesized compounds were also screened in silico for their PARP-1 binding affinities by molecular docking studies using Schrodinger 2016 software. In silico ADME studies were also performed for the synthesized compounds by using QikProp tool of Schrodinger software. Results: Results of in silico studies indicated that quinazolinone derivatives exhibited a good affinity towards the active site of PARP-1. Out of all synthesized compounds, SVA-11 exhibited a maximum dock score (-10.421). Results of ADME studies indicated the suitability of synthesized compounds as drug candidates. Conclusion: The synthesized compounds showed better docking scores than reference drug valiparib. Furthermore, they exhibited favorable ADME profile. Therefore, they may serve as lead compounds in the discovery of PARP-1 inhibitors.

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