scholarly journals Convenient Synthesis and Biological Activity of 4-minomethylene 1-phenylpyrazolidine-3,5-diones

2017 ◽  
Vol 59 (3) ◽  
Author(s):  
Eman A. Ahmed
Keyword(s):  
Biological Activity ◽  
Nucleophilic Substitution ◽  
Hydrazine Hydrate ◽  
New Products ◽  
Antimicrobial Effect ◽  
Antimicrobial Activities ◽  
Dimethylamino Group ◽  
Convenient Synthesis ◽  
Anti Inflammatory ◽  
High Yields

Reaction of (<em>Z</em>)-4-((dimethylamino)methylene)-1-phenylpyrazolidine-3,5-dione (<strong>1</strong>) with different nucleophiles is described. Treatment of enaminone <strong>1 </strong>with phenylhydrazine led to 3-oxo-<em>N’</em>,2-diphenyl-2,3-dihydro-1<em>H</em>-pyrazole-4-carbohydrazide <strong>7</strong>. New enaminone derivatives <strong>2–6 </strong>and <strong>12–14 </strong>were conveniently obtained in high yields via nucleophilic substitution of the dimethylamino group in enaminone <strong>1 </strong>when reacted with <em>o</em>-aminophenol, <em>o</em>-aminothiophenol, ethanolamine, cysteamine hydrochloride, piperidine, morpholine, 2-aminopyridine and glycine. Reaction of enaminone <strong>1 </strong>with diaza-nucleophiles, such as hydrazine hydrate, ethylenediamine and <em>o</em>-phenylenediamine, afforded the corresponding <em>bis</em>-enaminones <strong>9–11</strong>. Anti-inflammatory and antimicrobial activities of some new products were evaluated. Compounds <strong>1, 2, 4, 7, 12a</strong>, and <strong>12b </strong>showed high anti- inflammatory activity compared with indomethacin as the reference, while the highest antimicrobial effect was observed in the case of compound <strong>3</strong>.

scholarly journals Pharmacological Evaluation of Secondary Metabolites and Their Simultaneous Determination in the Arabian Medicinal Plant Plicosepalus curviflorus Using HPTLC Validated Method

2019 ◽  
Vol 2019 ◽  
pp. 1-8 ◽  
Author(s):  
Raha Orfali ◽  
Shagufta Perveen ◽  
Nasir Ali Siddiqui ◽  
Perwez Alam ◽  
Tawfeq Abdullah Alhowiriny ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Antimicrobial Effect ◽  
Antimicrobial Activities ◽  
Simultaneous Estimation ◽  
Peroxisome Proliferator ◽  
Activation Effect ◽  
Aerial Parts ◽  
Flavonoid Quercetin ◽  
Anti Inflammatory ◽  
Peroxisome Proliferator Activated Receptors

Plicosepalus is an important genus of the Loranthaceae family, and it is a semiparasitic plant grown in Saudi Arabia, traditionally used as a cure for diabetes and cancer in human and for increasing lactation in cattle. A flavonoid quercetin (P1), (-)-catechin (P2), and a flavane gallate 2S,3R-3,3′,4′,5,7-pentahydroxyflavane-5-O-gallate (P3) were isolated from the methanol extract of the aerial parts of P. curviflorus (PCME). The PCME and the isolated compounds were subjected to pharmacological assays to estimate peroxisome proliferator-activated receptors PPARα and PPARγ agonistic, anti-inflammatory, cytotoxic, and antimicrobial activities. Results proved for the first time the dual PPAR activation effect of the PCME and catechin (P2), in addition to the promising anti-inflammatory activity of the flavonoid quercetin (P1). Interestingly, both PCME and isolated compounds showed potent antioxidant activities while no antimicrobial effect against certain microbial strains had been reported from the extract and the isolated compounds. Based on the pharmacological importance of these compounds, an HPTLC validated method was developed for the simultaneous estimation of these compounds in PCME. It was found to furnish a compact and sharp band of compounds P1, P2, and P3 at Rf = 0.34, 0.47, and 0.65, respectively, using dichloromethane, methanol, and formic acid (90 : 9.5 : 0.5, (v/v/v)) as the mobile phase. Compounds P1, P2, and P3 were found to be 11.06, 10.9, 6.96 μg/mg, respectively, in PCME. The proposed HPTLC method offers a sensitive, precise, and specific analytical tool for the quantification of quercetin, catechin, and flavane gallates in P. curviflorus.

A Review: Therapeutic and Biological Activity of Benzothiazole Derivatives

2017 ◽  
Vol 4 (3) ◽  
Author(s):  
Suresh Choudhary ◽  
G Jeyabalan ◽  
Naresh Kalra
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
New Products ◽  
Therapeutic Agents ◽  
Present Review ◽  
Benzothiazole Derivatives ◽  
Anti Inflammatory

The Benzothiazole nucleus is present in compounds involved in research aimed at evaluating new products that possess interesting biological activities, such as antitumor, antimicrobial, anthelmintic, antileishmanial, anticonvulsant and anti-inflammatory. The present review focuses on the benzothiazoles with potential activities that are now in development. The synthesized benzothiazole derivatives could be considered as lead molecule for the development of therapeutic agents.

Anti-Inflammatory and Antimicrobial Activities of Aqueous Extracts of Wild Mushrooms from Japan

2019 ◽  
Vol 21 (5) ◽  
pp. 469-486
Author(s):  
Sayumi Yamada ◽  
Mai Tanaka ◽  
Rina Miura ◽  
Chiaki Takeuchi ◽  
Zhihao Tu ◽  
...  
Keyword(s):  
Antimicrobial Activities ◽  
Aqueous Extracts ◽  
Wild Mushrooms ◽  
Anti Inflammatory

Study of Physico-chemical Characteristics and Pharmacological Effects of 1-Ethyl-Salicyldene-bis-Ethylene-Diamine and Its Complex with Mn(II)

2019 ◽  
Vol 70 (7) ◽  
pp. 2534-2537
Author(s):  
Gladiola Tantaru ◽  
Mihai Apostu ◽  
Antonia Poiata ◽  
Mihai Nichifor ◽  
Nela Bibire ◽  
...  
Keyword(s):  
Schiff Base ◽  
Chemical Structure ◽  
Antimicrobial Activities ◽  
Ethylene Diamine ◽  
Chemical Characteristics ◽  
Gram Negative Bacteria ◽  
Pharmacological Effects ◽  
Physico Chemical ◽  
Anti Inflammatory ◽  
Inflammatory Effect

The paper presents the synthesis of a new complex combination of a Bis-Schiff base with Mn(II) ions with great potential for antimicrobial and anti-inflammatory activity. A new complex of the Salen-type ligand, 1-ethyl-salicylidene-bis-ethylene diamine was synthetized using Mn(II) ions. The chemical structure was confirmed through 1H-NMR and IR spectroscopy. The antimicrobial activities of the Bis-Schiff base and its complex were tested in comparison with Ampicillin, Chloramphenicol, Tetracycline, Ofloxacin and Nystatin. Those compounds were found to be active against Gram-positive or Gram-negative bacteria, and had an anti-inflammatory effect comparable to that of Indomethacin.

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

2019 ◽  
Vol 16 (7) ◽  
pp. 953-967 ◽  
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.

Assessment of Cota altissima (L.) J. Gay for phytochemical composition and antioxidant, anti-inflammatory, antidiabetic and antimicrobial activities

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Gamze Göger ◽  
Muhammed Allak ◽  
Ali Şen ◽  
Fatih Göger ◽  
Mehmet Tekin ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Essential Oil ◽  
Antioxidant Activities ◽  
Antimicrobial Activities ◽  
Antidiabetic Activity ◽  
Gram Negative Bacteria ◽  
Inhibitory Effects ◽  
Dicaffeoylquinic Acid ◽  
Anti Inflammatory ◽  
Phytochemical Profiles

Abstract Phytochemical profiles of essential oil (EO), fatty acids, and n-hexane (CAH), diethyl ether (CAD), ethyl acetate (CAE) and methanol extracts (CAM) of Cota altissima L. J. Gay (syn. Anthemis altissima L.) were investigated as well as their antioxidant, anti-inflammatory, antidiabetic and antimicrobial activites. The essential oil was characterized by the content of acetophenone (35.8%) and β-caryophyllene (10.3%) by GC-MS/FID. Linoleic and oleic acid were found as main fatty acids. The major constituents of the extracts were found to be 5-caffeoylquinic acid, 3,5-dicaffeoylquinic acid, isorhamnetin glucoside, quercetin and quercetin glucoside by LC-MS/MS. Antioxidant activities of the extracts were determined by scavenging of DPPH and ABTS free radicals. Also, the inhibitory effects on lipoxygenase and α-glucosidase enzymes were determined. Antimicrobial activity was evaluated against Gram positive, Gram negative bacteria and yeast pathogens. CAM showed the highest antioxidant activity against DPPH and ABTS radicals with IC50 values of 126.60 and 144.40 μg/mL, respectively. In the anti-inflammatory activity, CAE demonstrated the highest antilipoxygenase activity with an IC50 value of 105.40 μg/mL, whereas, CAD showed the best inhibition of α-glucosidase with an IC50 value of 396.40 μg/mL in the antidiabetic activity. CAH was effective against Staphylococcus aureus at MIC = 312.5 µg/mL. This is the first report on antidiabetic, anti-inflammatory and antimicrobial activities of different extracts of C. altissima.

scholarly journals New Haloterpenes from the Marine Red Alga Laurencia papillosa: Structure Elucidation and Biological Activity

Marine Drugs ◽  
2021 ◽  
Vol 19 (1) ◽  
pp. 35
Author(s):  
Mohamed Shaaban ◽  
Ghada S. E. Abou-El-Wafa ◽  
Christopher Golz ◽  
Hartmut Laatsch
Keyword(s):  
Biological Activity ◽  
Crude Extract ◽  
Structure Elucidation ◽  
Antimicrobial Activities ◽  
Red Alga ◽  
Spectroscopic Methods ◽  
X Ray Diffraction ◽  
X Ray ◽  
Chemical Structures ◽  
Terpene Derivatives

Analysis of the air-dried marine red alga Laurencia papillosa, collected near Ras-Bakr at the Suez gulf (Red Sea) in Egypt delivered five new halogenated terpene derivatives: aplysiolic acid (1), 7-acetyl-aplysiol (2), aplysiol-7-one (3), 11,14-dihydroaplysia-5,11,14,15-tetrol (5a), and a new maneonene derivative 6, named 5-epi-maneolactone. The chemical structures of these metabolites were characterized employing spectroscopic methods, and the relative and absolute configurations were determined by comparison of experimental and ab initio-calculated NMR, NOE, ECD, and ORD data, and by X-ray diffraction of 2 and 6. The antimicrobial activities of the crude extract and compounds 1–3, 5a and 6 were studied.

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