N-arylmethylideneaminophthalimide: Design, Synthesis and Evaluation as Analgesic and Anti-inflammatory Agents

2019 ◽  
Vol 19 (8) ◽  
pp. 679-687 ◽  
Author(s):  
Nasimossadat Banarouei ◽  
Asghar Davood ◽  
Hamed Shafaroodi ◽  
Ghazaleh Saeedi ◽  
Abbas Shafiee
Keyword(s):  
Room Temperature ◽  
Antiinflammatory Activity ◽  
Chemical Characterization ◽  
Design Synthesis ◽  
Reference Drug ◽  
Anti Inflammatory ◽  
Pain Test ◽  
Derivatives Of

Background and Objective: N-aryl derivatives of phthalimide and 4-nitro phthalimide have demonstrated cyclooxygenase inhibitory activity. Also, they possess excellent analgesic and antiinflammatory activity. In this work, a new series of N-arylmethylideneamino derivatives of phthalimide and 4-nitro phthalimide were designed and synthesized. Methods: The designed compounds were synthesized by condensation of the appropriate aldehyde and N-aminophthalimide in ethanol at room temperature at PH around 3. Their analgesic and antiinflammatory activity were evaluated by acetic acid-induced pain test and carrageenan-induced paw edema test in mice and rats, respectively. Results and Conclusion:: The details of the synthesis and chemical characterization of the analogs are described. In vivo screening showed compounds 3a, 3b, 3f and 3h were the most potent analgesic compounds. In addition, compounds 3a, 3c, 3d, 3e and 3j indicated comparable anti-inflammatory activity to indomethacin as a reference drug.

scholarly journals Design, Synthesis and Characterization of Some Novel benzamide derivatives and it's Pharmacological Screening

2020 ◽  
pp. 68-74 ◽  
Author(s):  
Akshay R. Yadav ◽  
Shrinivas K. Mohite
Keyword(s):  
Chemical Structure ◽  
Design Synthesis ◽  
Different Types ◽  
Anti Inflammatory ◽  
Benzoyl Isothiocyanate ◽  
Pharmacological Screening ◽  
Benzamide Derivatives

The new series of substituted N-(phenylcarbamothioyl)benzamide derivatives (2a-2f) was designed, development and synthesized by using conventional and microwave method. In present work 6 different N-(phenylcarbamothioyl)benzamide were synthesized. Substituted benzoyl chloride is converted into benzoyl isothiocyanate by esterification. Benzoyl isothiocyanate is converted into Substituted (phenylcarbamothioyl)benzamide by treating with different types of substituted aniline. Confirmation of the chemical structure of the synthesized was substantiated by TLC, IR, 1H NMR, MS spectroscopy.Novel synthesized compounds screened for their in vivo and in-vitro anti-inflammatory studies and compound 2f shows promising anti-inflammatory activity.

Synthesis and Biological Evaluation of Some Pyrazole Derivatives, Containing (Thio) Semicarbazide, as Dual Anti-Inflammatory Antimicrobial Agents

2019 ◽  
Vol 16 (9) ◽  
pp. 1020-1030
Author(s):  
Zhaochang Liang ◽  
Yuping Huang ◽  
Shiben Wang ◽  
Xianqing Deng
Keyword(s):  
Antiinflammatory Activity ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Pyrazole Derivatives ◽  
Reference Drug ◽  
Tnf Α ◽  
Anti Inflammatory

Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1H NMR, 13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Their in vitro antimicrobial activities were evaluated using a serial dilution method against several gram-positive strains, gram-negative strains and a fungi strain. Results: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF- α at the concentration of 20 µg/mL Compounds 5i, 6b, and 7b had comparable in vivo antiinflammatory activity to the reference drug dexamethasone at the dose of 50 mg/kg. In addition, several compounds showed antimicrobial activity against different strains, and compounds 5g and 5h exhibited potent inhibitory activities with the MIC value of 8 µg/mL against the Streptococcus pneumoniae CMCC 31968 and Staphylococcus aureus CMCC 25923, respectively. Compound 7b, which exhibited both anti-inflammatory and antimicrobial activities, should be studied as it is or after derivatization. Conclusion: It can be concluded that pyrazoles, with (thio)-semicarbazone moieties, have the potential to be developed into new anti-inflammatory agents.

Chemical Characterization and In Vivo Anti-Inflammatory Activities of Actinidia callosa var. ephippioides via Suppression of Proinflammatory Cytokines

2013 ◽  
Vol 41 (02) ◽  
pp. 405-423 ◽  
Author(s):  
Jung-Chun Liao ◽  
Shyh-Shyun Huang ◽  
Jeng-Shyan Deng ◽  
Chao-Ying Lee ◽  
Ying-Chih Lin ◽  
...  
Keyword(s):  
Chemical Characterization ◽  
Ethyl Acetate Fraction ◽  
Paw Edema ◽  
Inflammatory Mechanism ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Factor Α ◽  
Oxide Synthase

Actinidia callosa var. ephippioides (ACE) has been widely used to treat anti-pyretic, antinociceptive, anti-inflammation, abdominal pain and fever in Taiwan. This study aims to determine the mechanism of anti-inflammatory activities of ethyl acetate fraction of ACE (EA-ACE) using a model of λ-carrageenan (Carr)-induced paw edema in mouse model. In HPLC analysis, chemical characterization of EA-ACE was established. In order to investigate the anti-inflammatory mechanism of EA-ACE, we have detected the activities of catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx) and the levels of malondialdehyde (MDA) in the paw edema. Serum NO, tumor necrosis factor α (TNF-α), and interleukin-1β (IL-1β) were evaluated. Chemical characterization from HPLC indicated that EA-ACE contains betulinic acid, ursolic acid and oleanolic acid. In the anti-inflammatory test, EA-ACE decreased the paw edema after Carr administration, increased the activities of CAT, SOD, and GPx and decreased the MDA level in the edema paw at the 5th hr after Carr injection. EA-ACE affects the serum NO, TNF-α, and IL-1β levels at the 5th hr after Carr injection. EA-ACE decreased Carr-induced inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expressions by Western blotting. Actinidia callosa var. ephippioides have the potential to provide a therapeutic approach to inflammation-associated disorders.

scholarly journals Withania frutescens: Chemical characterization, analgesic, anti-inflammatory, and healing activities

2020 ◽  
Vol 18 (1) ◽  
pp. 927-935 ◽  
Author(s):  
Abdelfattah EL Moussaoui ◽  
Fatima Zahra Jawhari ◽  
Mohammed Bourhia ◽  
Imane Maliki ◽  
Fatiha Sounni ◽  
...  
Keyword(s):  
Inflammatory Diseases ◽  
Chemical Characterization ◽  
Phytochemical Analysis ◽  
Disease Treatment ◽  
Reference Drug ◽  
Maximum Inhibition ◽  
Anti Inflammatory ◽  
Effective Drugs ◽  
Promising Source

AbstractWithania frutescens (W. frutescens) is a medicinal plant that is largely used in the Morrocan pharmacopeia for disease treatment. This work was conducted to investigate the chemical characterization, analgesic, anti-inflammatory, and healing activities of W. frutescens. The chemical characterization of W. frutescens extract was done using HPLC; the anti-inflammatory test was performed with doses 300, 400 and 450 mg/kg, and the healing activity was assessed using two creams (extract 5% and extract 10%). Phytochemical analysis revealed the presence of phenolic compounds. The results of the anti-inflammatory test were more pronounced when compared with the reference drug with a maximum inhibition percentage of 82.20% ± 8.69 obtained at the dose of 450 mg/kg. Local application of 10% plant cream induced 80.17% ± 7.89 of inflammation inhibition when compared with the indomethacin drug 92.33% ± 11.27. The studied plant extract showed a promising healing activity with the following percentage: 99.03% ± 0.76 (extract 10%), 98.61% ± 1.91 (extract 5%), and 57.43% ± 2.97 (control); meanwhile, the value reached to 100% ± 0.02 for the drug that was used as a reference within the first 2 weeks. The plant studied in this work would be a promising source for conceptualizing effective drugs against inflammatory diseases.

scholarly journals Design, Synthesis, Structure and Properties of Ba-Doped Derivatives of SrCo0.95Ru0.05O3−δ Perovskite as Cathode Materials for SOFCs

Materials ◽  
2019 ◽  
Vol 12 (12) ◽  
pp. 1957
Author(s):  
Sabina Sydyknazar ◽  
Vanessa Cascos ◽  
Loreto Troncoso ◽  
Ana Laura Larralde ◽  
María Teresa Fernández-Díaz ◽  
...  
Keyword(s):  
Room Temperature ◽  
Solid Oxide ◽  
Structure And Properties ◽  
X Ray Diffraction ◽  
Design Synthesis ◽  
X Ray ◽  
Unit Cell Size ◽  
Maximum Conductivity ◽  
Derivatives Of

We have designed and prepared a novel cathode material for solid oxide fuel cell (SOFC) based on SrCo0.95Ru0.05O3−δ perovskite. We have partially replaced Sr by Ba in Sr0.9Ba0.1Co0.95Ru0.05O3−δ (SBCRO) in order to expand the unit-cell size, thereby improving the ionic diffusion of O2− through the crystal lattice. The characterization of this new oxide has been studied at room temperature by X-ray diffraction (XRD) and neutron powder diffraction (NPD) experiments. At room temperature, SBCRO perovskite crystallizes in the P4/mmm tetragonal space group, as observed from NDP data. The maximum conductivity value of 18.6 S cm−1 is observed at 850 °C. Polarization resistance measurements on LSGM electrolyte demonstrate an improvement in conductivity with respect to the parent Sr-only perovskite cathode. A good chemical compatibility and an adequate thermal expansion coefficient make this oxide auspicious for using it as a cathode in SOFC.

scholarly journals Design, Synthesis, and Acute Anti-inflammatory Assessment of New 2-methyl Benzoimidazole Derivatives Having 4-Thiazolidinone Nucleus

2019 ◽  
pp. 151-160
Keyword(s):  
Molecular Docking ◽  
Control Group ◽  
Design Synthesis ◽  
Reference Drug ◽  
Reference Ligand ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Cox 2 Inhibitors

New two derivatives of 2- methyl benzoimidazole were designed, synthesized and evaluated as a potential cyclooxygenase-2 [COX-2] inhibitors. The synthesized compounds have been recognized according to their spectral FT-IR, 1H-NMR data and physical pro- perties. The newly synthesized compounds were investigated in vivo for their anti-inflammatory activities using egg-white stimulated paw edema method with respect to the effect of propylene glycol 50%v/v [control group] and the ibuprofen [10mg/kg i.p.] was selected as a reference ligand. New compounds showed a significantly higher in vivo anti-inflammatory activity compared with ibuprofen as a reference drug. COX-2 selectivity evaluation through molecular docking via GOLD suite [v. 5.6.2.]. The new compounds via molecular docking showed significant higher activities when compared with ibuprofen as referenced drugs because of having hydrogen bonding interaction toward the key amino acids within COX-2 structure and all these results were compatible with the study of in vivo acute anti-inflammatory activities for tested compounds. ADME studies were performed to predict absorption, bioavailability, topological polar surface area, and drug-likeness. The results of ADME studies showed that all synthesized compounds absorbed from the gastrointestinal tract.

Anti-inflammatory, Antipyretic, and Antinociceptive Effects of a Cressa cretica Aqueous Extract

Planta Medica ◽  
2017 ◽  
Vol 83 (17) ◽  
pp. 1313-1320 ◽  
Author(s):  
Heba Abdallah ◽  
Abdelsamed Elshamy ◽  
Abd El Gendy ◽  
Ahmed Abd El-Gawad ◽  
Elsayed Omer ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Wide Spectrum ◽  
Chemical Characterization ◽  
Control Group ◽  
Standard Drug ◽  
Whole Plant ◽  
Antinociceptive Effects ◽  
Anti Inflammatory

Abstract Cressa cretica is a widely grown halophytic plant traditionally used for the treatment of different ailments. Previous investigations reported its biological activity on a wide spectrum of diseases. In this study, in vivo antinociceptive, anti-inflammatory, and antipyretic activities of C. cretica aqueous extract whole plant were evaluated. In addition, the total polyphenol content, the total flavonoid content, and the chemical characterization of the extract were performed. C. cretica showed writhing inhibition in acetic acid-induced peripheral nociception of 43 and 48 % at doses of 50 and 100 mg/kg, respectively. The same doses increased latency time in a hot plate model of central analgesia by 66 and 78 % compared to the control group, respectively. The acute anti-inflammatory effect of the extract was explored in the carrageenan-induced rat hind paw test. The inhibition of paw volume was better than that of the standard drug indomethacin. C. cretica significantly decreased rectal temperature in the rats injected with Brewerʼs yeast. C. cretica aqueous extract showed both central and peripheral antinociceptive activities and was effective as an anti-inflammatory and antipyretic. Phenolic compounds, including chlorogenic acids and flavonol glycosides, were identified by HPLC-PDA-ESI-MS techniques. These findings indicate the medicinal importance of this traditionally used plant as a therapeutic remedy for different ailments.

scholarly journals Chemical Composition, Antimicrobial and Antiparasitic Screening of the Essential Oil from Phania matricarioides (Spreng.) Griseb.

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1615 ◽  
Author(s):  
Yamilet Gutiérrez ◽  
Ramón Scull ◽  
Anabel Villa ◽  
Prabodh Satyal ◽  
Paul Cos ◽  
...  
Keyword(s):  
Fungal Growth ◽  
Chemical Characterization ◽  
Peritoneal Macrophages ◽  
In Vivo Studies ◽  
Parasitic Protozoa ◽  
Reference Drug ◽  
Ic50 Values

Essential oils (EOs) have gained increasing attention due to their pharmacological effectiveness, and they also constitute some of the most popular natural products. In this study, we present the chemical characterization of the EO from Phania matricarioides and the in vitro activity/selectivity against a wide panel of bacteria, fungi and parasitic protozoa. Forty-five compounds were identified in the studied EO, of which lavandulyl acetate (40.1%) and thymyl isobutyrate (13.9%) were the major components. The EO did not inhibit bacterial or fungal growth at the maximum concentration tested (64 µg/mL), although it displayed activity on all evaluated protozoa (IC50 values ranging from 2.2 to 56.6 µg/mL). In parallel, the EO demonstrated a noteworthy cytotoxic activity against peritoneal macrophages (CC50 values of 28.0 µg/mL). The most sensitive microorganism was Trypanosoma cruzi, which had a superior activity (IC50 = 2.2 µg/mL) and selectivity (SI = 13) in respect to other parasitic protozoa and the reference drug (p < 0.05). Further in vivo studies are needed to evaluate the potential use of this EO and the main compounds as antitrypanosomal agents. To our knowledge, this is the first report of chemical characterization and antimicrobial assessment of the EO from P. matricarioides.

scholarly journals Antioxidant Action and In Vivo Anti-Inflammatory and Antinociceptive Activities of Myrciaria floribunda Fruit Peels: Possible Involvement of Opioidergic System

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Izabelly Bianca da Silva Santos ◽  
Bruno Santos dos Santos ◽  
João Ricardhis Saturnino de Oliveira ◽  
Wêndeo Kennedy Costa ◽  
Adrielle Zagmignan ◽  
...  
Keyword(s):  
High Performance ◽  
Antioxidant Properties ◽  
Chemical Characterization ◽  
Opioidergic System ◽  
Anti Inflammatory ◽  
Inflammatory Action ◽  
Monomeric Anthocyanins

This work evaluated the antioxidant properties and in vivo antinociceptive and anti-inflammatory effects of extracts obtained from fruit peels of Myrciaria floribunda (H. West ex Willd.) O. Berg (Myrtaceae). This plant is popularly known in Brazil as Cambuí or camboim. Different extracts were submitted to comparative analysis to determine the content of selected phytochemical classes (levels of total phenols, flavonoids, and monomeric anthocyanins) and the in vitro antioxidant potentials. The extract with higher potential was selected for in vivo evaluation of its antinociceptive and anti-inflammatory action. Finally, the chemical characterization of this extract was performed by high-performance liquid chromatography (HPLC). MfAE (extract obtained using acetone as solvent) showed the higher levels of phenols (296 mg GAE/g) and anthocyanins contents (35.65 mg Cy-3-glcE/g) that were associated with higher antioxidant activity. MfAE also exhibited in vivo anti-inflammatory and analgesic propertiers. This fraction inhibited the inflammatory and neurogenic phases of pain, and this effect was reversed by naloxone (suggesting the involvement of opioidergic system). MfAE reduced the abdominal contortions induced by acetic acid. The HPLC analysis revealed the presence of gallic acid (and its derivatives) and ellagic acid. Taken together, these data support the use of M. floribunda fruit peels for development of functional foods and nutraceutics.

scholarly journals Synthesis and Biological Activities of 4-Aminoantipyrine Derivatives Derived from Betti-Type Reaction

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Ipsita Mohanram ◽  
Jyotsna Meshram
Keyword(s):  
Room Temperature ◽  
Biological Activities ◽  
Anthelmintic Activity ◽  
Reference Drug ◽  
Lipinski’S Rule ◽  
One Step ◽  
Lipinski’S Rule Of Five ◽  
Anti Inflammatory

The present work deals with the synthesis and evaluation of biological activities of 4-aminoantipyrine derivatives derived from a three-component Betti reaction. The synthesis was initiated by the condensation of aromatic aldehyde, 4-aminoantipyrine, and 8-hydroxyquinoline in presence of fluorite as catalyst in a simple one-step protocol. The reactions were stirred at room temperature for 10–15 min achieving 92–95% yield. The structures of synthesized derivatives were established on the basis of spectroscopic and elemental analysis. All derivatives 4(a–h) were screened in vivo and in vitro for anti-inflammatory and anthelmintic activity against a reference drug, Diclofenac and Albendazole, respectively. The screening results show that compounds 4c, 4d, 4f, and 4h were found to possess potential anti-inflammatory activity while compounds 4a, 4b, 4e, and 4g are potent anthelmintic agents when compared with reference drugs, respectively. The bioactivity of these derivatives has also been evaluated with respect to Lipinski’s rule of five using molinspiration cheminformatics software.

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