scholarly journals Synthesis and Biological Evaluation of Some Piperazine Derivatives as Anti-Inflammatory Agents

2019 ◽  
Vol 9 (4-s) ◽  
pp. 353-358
Author(s):  
Nalini Patel ◽  
Vaishali Karkhanis ◽  
Pinkal Patel
Keyword(s):  
Mannich Bases ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Piperazine Derivatives ◽  
Rat Paw Edema ◽  
In Series ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Synthesis And Biological Evaluation

Some 1-((4-methylpiperazin-1yl)methyl)-1H-benzo[d]imidazole & 1-((4-phenylpiperazin-1yl)methyl)-1H-benzo[d]imidazole derivatives were synthesized through reaction of 1-substituted piperazines with different benzimidazole derivatives in methanol yielded the corresponding mannich bases (42-a to 42-i). All the synthesized compounds were elucidated by IR, 1H NMR and MASS spectroscopy. They were tested for anti-inflammatory activity using in-vivo (Carrageenan- induced rat paw edema model) method at a dose of 50mg/kg. result showed that compounds 42-c, 42-d and 42-h were found to be most potent in series. Keywords: 1,4-disubstituted Piperazine, Anti-inflammatory, Mannich Base.

Inhibition of iNOS by Benzimidazole Derivatives: Synthesis, Docking, and Biological Evaluations

2021 ◽  
Vol 17 ◽  
Author(s):  
Richa Minhas ◽  
Yogita Bansal
Keyword(s):  
Inflammatory Activity ◽  
Benzimidazole Derivatives ◽  
Critical Study ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Inos Inhibitors ◽  
Rat Paw

Background: Inducible nitric Oxide Synthase (iNOS) plays a key role in the progression of inflammatory diseases by accelerating the production of NO, which makes it an intriguing target to treat inflammation in complex diseases. Therefore, the search is on to develop molecules as selective iNOS inhibitors. Objective: The present work was aimed to design, synthesize and evaluate benzimidazole-coumarin coupled molecules as anti-iNOS agents through in silico and pharmacological studies. Methods: A critical study of literature reports on iNOS inhibitors led to the selection of a (un)substituted coumarin nucleus, 2-aminobenzimidazole, and a 4-atom linker as important structural components for iNOS inhibition. Two series of compounds (7-16 and 17-26) were designed and synthesized by coupling these components. The compounds were subjected to docking using iNOS (1QW4) and nNOS (1QW6) as targets. All compounds were evaluated for NO and iNOS inhibitory activities in vitro. The selected compound was finally evaluated for anti-inflammatory activity in vivo using the carrageenan-induced rat paw edema model. Results : All compounds showed moderate to good inhibition of NO and iNOS in vitro. Compound 12 was the most potent inhibitor of NO and iNOS. Hence, it was evaluated in vivo for toxicity and anti-inflammatory activity. It was found to be safe in acute toxicity studies, and effective in reducing the rat paw edema significantly. Its anti-inflammatory behaviour was similar to that of aminoguanidine, which is a selective iNOS inhibitor. Conclusion: The newly synthesized benzimidazole-coumarin hybrids may serve as potential leads for the development of novel anti-iNOS agents.

scholarly journals Bioactivity-Guided Investigation of the Anti-Inflammatory Activity of Hippophae rhamnoides Fruits

Planta Medica ◽  
2017 ◽  
Vol 84 (01) ◽  
pp. 26-33 ◽  
Author(s):  
Dóra Rédei ◽  
Norbert Kúsz ◽  
Nikoletta Jedlinszki ◽  
Gábor Blazsó ◽  
István Zupkó ◽  
...  
Keyword(s):  
Hippophae Rhamnoides ◽  
Inflammatory Activity ◽  
Hippophaë Rhamnoides ◽  
Rat Paw Edema ◽  
In Vivo Animal Models ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
First Time ◽  
Peel Extract

AbstractAccording to modern ethnobotanical records, the fruit of Hippophae rhamnoides is effective in the treatment of different allergic symptoms. In order to obtain pharmacological evidence for this observation, the fruit was investigated for anti-inflammatory activity using in vivo animal models. Aqueous and 70% MeOH extracts were tested in 48/80-induced rat paw edema assay after oral administration, and it was found that the 70% MeOH extract (500 mg/kg) reduced significantly edema volume (0.660 ± 0.082 mL vs. control 0.935 ± 0.041 mL). Extracts of different parts of the fruit (pulp, peel, seed) were investigated in the same assay, and the peel extract was shown to exhibit maximum edema-reducing effect (0.470 ± 0.124 mL vs. control 0.920 ± 0.111 mL). This extract was used to elucidate the mode of action. Different inflammation inducers (serotonin, histamine, dextran, bradykinin, and carrageenan) were applied in the rat paw model, but the extract inhibited only the compound 48/80 elicited inflammation. The active extract was then fractionated by solvent-solvent partitioning and chromatographic methods with the guidance of the 48/80-induced anti-inflammatory assay, and the main compounds responsible for the activity were identified as ursolic acid and oleanolic acid. Our data suggest that the activity is most probably based on a membrane stabilizing effect caused by the inhibition of degranulation of mast cells. Moreover, previously unknown 2,5-bis-aryl-3,4-dimethyltetrahydrofuran lignans, nectandrin B, fragransin A2, and saucernetindiol were isolated and identified from H. rhamnoides for the first time.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

scholarly journals Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole Bearing Pyridine Moiety

2019 ◽  
pp. 300-307
Author(s):  
Asma D. Ambekari ◽  
Shrinivas K. Mohite
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Pyridine Moiety ◽  
Anti Inflammatory ◽  
Physicochemical Data ◽  
Synthesis And Biological Evaluation

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.

Synthesis, Molecular Docking and In Vivo Biological Evaluation of Iminostilbene Linked 1,2,3-Triazole Pharmacophores as Promising AntiAnxiety and Anti-Inflammatory Agents

2021 ◽  
Vol 17 ◽  
Author(s):  
Kariyappa N. Ankali ◽  
Javarappa Rangaswamy ◽  
Mallappa Shalavadi ◽  
Nagaraja Naik
Keyword(s):  
Molecular Docking ◽  
Cycloaddition Reaction ◽  
Triazole Ring ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Gaba A ◽  
Chemical Structures ◽  
Rat Paw Edema ◽  
Anti Inflammatory

Background: Iminostilbene and 1,2,3-triazole ring containing compounds are considered as beneficial substrates in drug design. Objectives: This study was aimed at the synthesis of novel series of iminostilbene linked 1,2,3- triazole pharmacophores (7c-n) by Cu(I) catalyzed 1,3 dipolar cycloaddition reaction between 5- (Prop-2-yn-1-yl)-5H-dibenzo[b,f]azepine (7b) and various substituted azidobenzene derivatives (3cn). Methods: The chemical structures of compounds were confirmed by 1 H NMR, 13C NMR, LC-MS and molecular docking studies were carried out through HEX docking software. Results: The in vivo anti anxiety capacity of the compounds was evaluated by using “elevated plus maze” (EPM), anxiety model. The results exhibited that compounds (7d, 7e, 7j and 7k) have a higher anti anxiety effect close to diazepam. The anti-inflammatory activities of the synthesized compounds were evaluated by “Carrageenan-induced rat paw edema” model, compounds (7b, 7c, 7d, 7f, and 7j) demonstrated statistically significant inflammatory activity. Molecular docking analysis revealed that compounds (7d, 7e and 7j) bound to GABA(A) proteins show more efficiency when compared to the other analogues in the series. Conclusion: These results suggest that compounds (7b, 7c, 7d, 7e, 7f, and 7j) can be considered as novel candidates for anti-anxiety and anti-inflammatory agents. Moreover, docking method was used to elucidate anti-anxiety effect of compounds. This study furnished insight into the molecular interactions of synthesized compounds with their physiological targets, and the potential to develop bioactive heterocyclic compounds.

Synthesis of new ibuprofen hybrid conjugates as potential anti-inflammatory and analgesic agents

2020 ◽  
Vol 12 (15) ◽  
pp. 1369-1386
Author(s):  
Siva S Panda ◽  
Adel S Girgis ◽  
Hitesh H Honkanadavar ◽  
Riham F George ◽  
Aladdin M Srour
Keyword(s):  
Writhing Test ◽  
Rat Paw Edema ◽  
Analgesic Agents ◽  
Inflammatory Drugs ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Inhibition Studies

Background: A new set of hybrid conjugates derived from 2-(4-isobutylphenyl)propanoic acid (ibuprofen) is synthesized to overcome the drawbacks of the current non-steroidal anti-inflammatory drugs. Results & methodology: Synthesized conjugates were screened for their anti-inflammatory, analgesic and ulcerogenic properties. Few conjugates were found to have significant anti-inflammatory properties in the carrageenan-induced rat paw edema test, while a fair number of conjugates showed promising peripheral analgesic activity in the acetic acid-induced writhing test as well as central analgesic properties in the in vivo hot plate technique. The newly synthesized conjugates did not display any ulcerogenic liability. Conclusion: In vitro, COX-1 and COX-2 enzyme inhibition studies raveled compound 7e is more selective toward COX-2 compared with ibuprofen.

scholarly journals EFFECT OF TERPENES AS PENETRATION ENHANCERS ON THE RELEASE AND PERMEATION KINETICS OF MELOXICAM GELS FORMULATIONS

2020 ◽  
pp. 1-5
Author(s):  
Raj Kumari ◽  
Pallavi Matta ◽  
Meenakshi Sharma ◽  
Madhu Verma
Keyword(s):  
Penetration Enhancers ◽  
Peppermint Oil ◽  
Clove Oil ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Lemongrass Oil ◽  
Anti Inflammatory ◽  
Rat Paw

Introduction: The transdermal route of administration has been extensively accepted as one of the potential route for the local and systemic delivery of drugs. The greatest obstacle in drug absorption is the highly organized stratum corneum (SC), which hinder drug transport. The probable solution leads to inclusion of penetration enhancers for reversibly disorganizing the barrier characteristic of stratum corneum. Objective: The main objective of the research work was to study the influence of peppermint oil, lemongrass oil, clove oil and turpentine oil as penetration enhancers on the percutaneous absorption of Meloxicam (ME) from a Carbopol 934 based gel formulation. Materials and Methods: ME gel sample was divided into 5 batches i.e., F1, F2, F3, F4, F5. Except F1, all other batches were incorporated with penetration enhancers (5% w/w) namely peppermint oil, clove oil, lemongrass oil and turpentine oil. The formulations were further evaluated for in-vitro drug release studies using a standard cellophane membrane at 37± 0.5˚ C in phosphate buffer pH 7.4 and a comparative anti-inflammatory activity was conducted using rat paw edema method. Result and Discussion: In-vitro permeation studies using a standard cellophane membrane showed that the rank order of enhancement ratio (ERflux) for Meloxicam as peppermint oil (1.414) > clove oil (1.353) > lemongrass oil (1.326) > turpentine oil (1.272) proving peppermint oil as the most competent penetration enhancer for Meloxicam. Further In- vivo anti-inflammatory activity were carried out using the standard rat paw edema method. The in vivo studies revealed that gel containing peppermint, clove, lemongrass and turpentine exhibited 2.53, 2.0, 1.9 and 1.38 times higher anti-inflammatory effect as compared to meloxicam (standard). Conclusion: It can be concluded from the study that all the 4 terpenes significantly increases the permeation of meloxicam gels and can be used as effective penetration enhancers.

scholarly journals Anti-Inflammatory Evaluation of NLC (Nanostructured Lipid Carriers) Meloxicam In-Vivo

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
Widyaningrum I. ◽  
Hariyadi D. M. ◽  
Hendradi E.
Keyword(s):  
Particle Size ◽  
Research Result ◽  
Entrapment Efficiency ◽  
Solid Lipid ◽  
Rat Paw Edema ◽  
Auc Value ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Inflammatory Effect

Objective: The aim of this research study was to investigate the anti-inflammatory effect of NLC meloxicam. NLC contains solid and liquid lipid. Monostearin as solid lipid and Miglyol 808 as liquid lipid. Methods : NLC meloxicam was repared using emulsification methodwith three different lipid ratio. . NLC meloxicam was prepared and characterized for measuring the pH, viscocity, particle size, and entrapment efficiency. The rat paw edema test was performed to evaluate the antiinflammatory activity of three formulations NLC meoxicam. Results : based on research result shows that the smaller the solid lipid concentrations, particle size is the larger, the greater viscosity, thus increasing occlusive NLC to the skin. The third formula hasthe greatest solid lipid concentration shows the smallest AUC value but once in a statistical test known to be significantly different from the three formulas. Conclusions : NLC meloxicam showed that it had anti-inflammatory effectiveness

Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles

2019 ◽  
Vol 15 (5) ◽  
pp. 521-536 ◽  
Author(s):  
Natalya Agafonova ◽  
Evgeny Shchegolkov ◽  
Yanina Burgart ◽  
Victor Saloutin ◽  
Alexandra Trefilova ◽  
...  
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Antipyretic Activity ◽  
Starting Point ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Synthesis And Biological Evaluation ◽  
Cox 1

Background: Formally belonging to the non-steroidal anti-inflammatory drug class pyrazolones have long been used in medical practices. Objective: Our goal is to synthesize N-methylated 1-aryl-3-polyfluoroalkylpyrazolones as fluorinated analogs of antipyrine, their isomeric O-methylated derivatives resembling celecoxib structure and evaluate biological activities of obtained compounds. Methods: In vitro (permeability) and in vivo (anti-inflammatory and analgesic activities, acute toxicity, hyperalgesia, antipyretic activity, “open field” test) experiments. To suggest the mechanism of biological activity, molecular docking of the synthesized compounds was carried out into the tyrosine site of COX-1/2. Conclusion: The trifluoromethyl antipyrine represents a valuable starting point in design of the lead series for discovery new antipyretic analgesics with anti-inflammatory properties.

Evaluation of Biological Activity of Derivatives of 1,3,4 Thiadiazole, 1,3,4-Oxadiazole and 1,2,4-Triazole

2020 ◽  
Vol 20 ◽  
Author(s):  
Gaurav M. Doshi ◽  
Mayuresh U. Bansode ◽  
Rakesh R. Somani
Keyword(s):  
Erythrocyte Membrane ◽  
Paw Edema ◽  
Toxic Dose ◽  
Rat Paw Edema ◽  
Maximum Decrease ◽  
Inhibitory Activities ◽  
Anti Inflammatory ◽  
Rat Paw

Objectives: 1,3,4-thiadiazole (A), 1,3,4-oxadiazole (B) and 1,2,4-triazole (C) derivatives have been known for their immense pharmacotherpaeutic potential. The current research article attempts to further explore and understand the probable biochemical mechanism related to anti-inflammatory activity of derivatives. Methods: The screened A, B and C derivatives were investigated for both in-vitro (Erythrocyte Membrane stabilization activity, Proteinase enzyme inhibitory activities) and in-vivo correlation using acute and chronic anti-inflammatory potential by carrageenan induced rats paw edema and cotton pellet granuloma methods respectively. The activity was studied after interpreting acute toxicity studies results. Results: In vitro studiesin the case of Erythrocyte Membrane stability and Proteinase enzyme inhibitory activities exhibited by A, B, and C at 100 ppm were found to be 48.89%, 51.08% and 50.08% and 66.78%, 76.91% and 57.41% respectively. The maximum toxic dose was found to be 2000 mg/kg. The derivatives were studied for two-dose levels viz; Lower (100 mg/kg) and higher dose (200 mg/kg). In rat paw edema maximum decrease was obtained for A (50.05%), B (50.05%) and C (51.06%) at lower and higher dose at 68.76%, 55.61%, and 65.26% respectively for effect up to 24 h. In the chronic model of cotton pelletgranuloma viz; higher and lower doses of A, B and C exhibited 38.15%, 33.19% and 30.25 % and 19.45%, 18.55% and 17.55 % respectively. Conclusion: The studied models depicted that derivatives A, B and C have the probable potential as anti-inflammatory agents. Further studies need to undertaken to explore their potential in the different therapeutic areas.

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