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Oxaprozin prodrug as safer nonsteroidal anti‐inflammatory drug: Synthesis and pharmacological evaluation 下载免费PDF全文
Jaya P. Peesa Lakshmana R. Atmakuri Prasanna R. Yalavarthi Basaveswara R. Mandava Venkata Arun Rasheed Vengalrao Pachava 《Archiv der Pharmazie》2018,351(2)
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V. Alagarsamy S. Meena K.V. Ramseshu V. Raja Solomon K. Thirumurugan 《Drug development research》2008,69(4):226-233
A new series of 3‐(4‐chloro phenyl)‐2‐substituted‐3H‐quinazolin‐4‐ones were synthesized by reacting the amino group of 2‐hydrazino‐3‐(4‐chloro phenyl)‐3H‐quinazolin‐4‐one with different aldehydes and ketones. The compounds were investigated for their analgesic activity in albino mice, and for their anti‐inflammatory and ulcerogenic activities in Wistar rats. All test compounds exhibited analgesic and anti‐inflammatory activities. Compound VA2 (2‐(1‐ethylpropylidene‐hydrazino)‐3‐(4‐chloro phenyl)‐3H‐quinazolin‐4‐one) showed moderately more potent analgesic activity and compound VA3 (2‐(1‐methylbutylidene‐hydrazino)‐3‐(4‐chlorophenyl)‐3H‐quinazolin‐4‐one) showed moderately more potent anti‐inflammatory activity when compared with the reference standard, diclofenac sodium. The test compounds showed only mild ulcerogenic side effects when compared with aspirin. Drug Dev Res 69: 226–233, 2008 ©2008 Wiley‐Liss, Inc. 相似文献
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《Drug development research》2018,79(4):157-164
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In vitro evaluation of the effects of anti‐fungals,benzodiazepines and non‐steroidal anti‐inflammatory drugs on the glucuronidation of 19‐norandrosterone: implications on doping control analysis 下载免费PDF全文
Amelia Palermo Beatrice Alessi Francesco Botrè Xavier de la Torre Ilaria Fiacco Monica Mazzarino 《Drug testing and analysis》2016,8(9):930-939
We have studied whether the phase II metabolism of 19‐norandrosterone, the most representative metabolite of 19‐nortestosterone (nandrolone), can be altered in the presence of other drugs that are not presently included on the Prohibited List of the World Anti‐Doping Agency. In detail, we have evaluated the effect of non‐prohibited drugs belonging to the classes of anti‐fungals, benzodiazepines, and non‐steroidal anti‐inflammatory drugs on the glucuronidation of 19‐norandrosterone. In vitro assays based on the use of either pooled human liver microsomes or specific recombinant isoforms of uridine diphosphoglucuronosyl‐transferase were designed and performed to monitor the formation of 19‐norandrosterone glucuronide from 19‐norandrosterone. Determination of 19‐norandrosterone (free and conjugated fraction) was performed by gas chromatography – mass spectrometry after sample pretreatment consisting of an enzymatic hydrolysis (performed only for the conjugated fraction), liquid/liquid extraction with tert‐butylmethyl ether, and derivatization to form the trimethylsilyl derivative. In parallel, a method based on reversed‐phase liquid chromatography coupled to tandem mass spectrometry in positive electrospray ionization with acquisition in selected reaction monitoring mode was also developed to identify the non‐prohibited drugs considered in this study. Incubation experiments have preliminarily shown that the glucuronidation of 19‐norandrosterone is principally carried out by UGT2B7 (39%) and UGT2B17 (31%). Inhibition studies have shown that the yield of the glucuronidation reaction is reduced in the presence of the anti‐fungals itraconazole, ketoconazole, and miconazole, of the benzodiazepine triazolam and of the non‐steroidal anti‐inflammatory drugs diclofenac and ibuprofen, while no alteration was recorded in the presence of all other compounds considered in this study. Copyright © 2015 John Wiley & Sons, Ltd. 相似文献
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Nonsteroidal anti‐inflammatory drugs (NSAIDs) are commonly used in therapeutic doses in human and veterinary medicine for the treatment of inflammation, pain, and fever. A method for the simultaneous determination of nine NSAIDs, known as therapeutic prohibited substances, in equine urine was developed and fully validated according to the European Commission Decision 2002/657/EC and Association of Official Racing Chemists criteria. The validation was performed for naproxen, flunixin, ketoprofen, diclofenac, eltenac, meclofenamic acid, phenylbutazone, vedaprofen, and carprofen in equine urine in accordance with the International Screening Limits (ISL) regulated by International Federation of Horseracing Authorities. After basic hydrolysis, samples were extracted with a C18 cartridge using automated solid‐phase extraction. Several derivatization reagents were investigated, and trimethylphenylammonium hydroxide/methanol (20/80, v/v) was selected. Analyses were carried out using gas chromatography–mass spectrometry with selected ion monitoring mode, but the method can be applied to a large number of analytes. The within‐laboratory reproducibility was not more than 12.8% (≤15%), and mean relative recoveries ranged from 91.1% to 104.1% for inter‐day and intra‐day precision. The decision limits (CCα) and detection capabilities (CCβ) were evaluated at concentrations near the ISL for each therapeutic substance. The validation results demonstrated that the method is highly reproducible, easily applicable, and suitable for the analysis of some NSAIDs in equine urine that have not been previously published. Finally, the method was also applied to known positive samples. 相似文献
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Risks of hypertension associated with cyclosporine,nonsteroidal anti‐inflammatory drugs,and systemic glucocorticoids in patients with psoriasis: a nationwide population‐based nested case–control study in Taiwan 下载免费PDF全文
Meng‐Sui Lee Chia‐Hsuin Chang Ruey‐Yi Lin Mei‐Shu Lai 《Pharmacoepidemiology and drug safety》2016,25(2):133-140
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Ahmed Bari Daniel Grenier Jabrane Azelmat Saeed Ali Syed Abdulrahman M. Al‐Obaid Eric C. Hosten 《Chemical biology & drug design》2019,94(4):1750-1759
In continuation with our research program on the development of novel bioactive molecules, we report herein the design and synthesis of a series of diversified heterocycles ( 4 – 22 ). The synthesized compounds were evaluated for their anti‐inflammatory activity. The chemical structures of the newly synthesized compounds have been confirmed by NMR, FTIR, and microanalysis. 相似文献
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Hyun‐Joo Jung Eun‐Hee Park Chang‐Jin Lim 《The Journal of pharmacy and pharmacology》2009,61(10):1391-1395
Objectives This work aimed to assess some pharmacological activities of coenzyme Q10 (CoQ10) in animal experimental models. Methods The chick chorioallantoic membrane assay was used to evaluate anti‐angiogenic activity of CoQ10. Anti‐inflammatory activity of CoQ10 was confirmed using two animal models of inflammation. These were the vascular permeability and air pouch models, models of acute and sub‐acute inflammation, respectively. Antinociceptive activity was assessed by the acetic acid‐induced abdominal constriction response. Key findings CoQ10 dose‐dependently displayed inhibition of chick chorioallantoic membrane angiogenesis. In the acetic acid‐induced vascular permeability model in mice, CoQ10 at 50, 100 and 200 mg/kg reduced vascular permeability from 0.74 ± 0.01 (A590) to 0.67 ± 0.01 (P < 0.01), 0.46 ± 0.02 (P < 0.01) and 0.30 ± 0.01 (P < 0.01), respectively. In the carrageenan‐induced inflammation in the air pouch, CoQ10 was able to diminish exudate volume, the number of polymorphonulcear leucocytes and nitrite content in the air pouches. CoQ10 at 25, 50 and 100 mg/kg significantly reduced acetic acid‐induced abdominal constriction in mice from 27.0 ± 2.00 (number of abdominal constrictions) to 17.7 ± 0.33 (P < 0.01), 9.3 ± 0.67 (P < 0.01) and 1.3 ± 0.33 (P < 0.01), respectively, suggesting a strong antinociceptive activity. Conclusions CoQ10 possessed considerable anti‐angiogenic, anti‐inflammatory and antinociceptive activity, possibly via down‐regulating the level of nitric oxide, which partly supported its use as a dietary supplement and in combination therapy. 相似文献
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Flávia De Toni Uchôa Teresinha Goncalves da Silva Maria do Carmo Alves de Lima Suely Lins Galdino Ivan da Rocha Pitta Professor Teresa Dalla Costa 《The Journal of pharmacy and pharmacology》2009,61(3):339-345
Objectives Novel 5‐benzilidene thiazolidinones have been synthesized and exhibited anti‐inflammatory activity. In this work one of the compounds of the thiazolidinone chemical series, (5Z,E)‐3‐[2‐(4‐chlorophenyl)‐2‐oxoethyl]‐5‐(1H‐indol‐3‐ ylmethylene)‐thiazolidine‐2,4‐dione (PG15) was investigated aiming to determine the drug's anti‐inflammatory potential in pre‐clinical studies. Methods Methods used included the in‐vitro inhibition of cyclooxygenase‐1 and ‐2, in‐vivo evaluation of anti‐inflammatory activity by air pouch and peritonitis models and the pharmacokinetic profile after intravenous (3 mg/kg) and oral (3 and 6 mg/kg) dosing to rats. Key findings A two‐compartment model with a fast distribution and an elimination half‐life of 5.9 ± 3.8 h described the PG15 plasma profile after intravenous dosing. PG15 showed an erratic and rapid absorption following oral administration with peak concentrations between 0.5 and 1 h. PG15 0.1 μM inhibited more than 30% and 13% of purified cyclooxygenase‐1 and ‐2 activity in vitro, respectively. A lack of dose dependency was observed for the anti‐inflammatory effect in the dose range investigated (0.8–50 mg/kg), with a maximum of 67.2 ± 4.6% inhibition of leucocyte migration in the carrageenan‐induced air pouch model obtained with the 3 mg/kg dose, similar to that observed for indometacin 10 mg/kg. Conclusions The erratic absorption of PG15 observed after oral dosing could explain the lack of anti‐inflammatory dose dependency. 相似文献
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Synthesis,molecular docking,and pharmacological evaluation of N‐(2‐(3,5‐dimethoxyphenyl)benzoxazole‐5‐yl)benzamide derivatives as selective COX‐2 inhibitors and anti‐inflammatory agents 下载免费PDF全文
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2‐Hydrazinyl‐N‐(4‐sulfamoylphenyl)acetamide 3 was the key intermediate for the synthesis of novel hydrazones 4–10 and pyrazole derivatives 11–17 . All compounds were tested for their in vivo anti‐inflammatory activity and their ability to inhibit the production of PGE2 in serum samples of rats. IC50 values for the most active compounds for inhibition of COX‐1 and COX‐2 enzymes were determined in vitro, and they were also tested for their ulcerogenic effect. Molecular docking was performed on the active site of COX‐2 to predict their mode of binding to the amino acids. Most of the synthesized compounds showed good anti‐inflammatory activity especially compounds 3, 4, 8, 9, 15, and 17 which showed better activity than diclofenac as the reference drug. Compounds 3, 8, 9, 13, and 15–17 were less ulcerogenic than indomethacine as the reference drug. Most of the synthesized compounds interacted with Tyr 385 and Ser 530 in molecular docking study with additional hydrogen bond for compound 17 . Compound 17 showed good selectivity index value of 11.1 for COX‐1/COX‐2 inhibition in vitro. 相似文献
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V. Alagarsamy D. Shankar S. Meena K. Thirumurugan T. Durai Ananda Kumar 《Drug development research》2007,68(3):134-142
A variety of novel 2‐methylthio‐3‐substituted amino‐5,6‐dimethyl thieno [2,3‐d] pyrimidin‐4(3H)‐ones were synthesized by reacting 3‐amino‐2‐methylthio‐5,6‐dimethyl thieno [2,3‐d] pyrimidin‐4(3H)‐one with different aldehydes and ketones. The starting material 3‐amino‐2‐methylthio‐5,6‐dimethyl thieno [2,3‐d] pyrimidin‐4(3H)‐one was synthesized from 2‐amino‐3‐carbethoxy‐4,5‐dimethyl thiophene. The compounds were investigated for their analgesic activity in albino mice, and for their anti‐inflammatory and ulcerogenic index activities in Wistar rats. The compound 2‐(1‐ethylpropylideneamino)‐2‐methylthio‐5,6‐dimethyl thieno [2,3‐d] pyrimidin‐4(3H)‐one (AS2) showed the most potent analgesic activity of the series. It also showed more potent anti‐inflammatory activity when compared to the reference standard, diclofenac sodium. The test compounds showed only mild ulcerogenic potential when compared to aspirin. Drug Dev Res 68:134–142, 2007. © 2007 Wiley‐Liss, Inc. 相似文献
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Jonathan G Merrell Shaun W McLaughlin Lu Tie Cato T Laurencin Alex F Chen Lakshmi S Nair 《Clinical and experimental pharmacology & physiology》2009,36(12):1149-1156
- 1 Curcumin is a naturally occurring poly‐phenolic compound with a broad range of favourable biological functions, including anti‐cancer, anti‐oxidant and anti‐inflammatory activities. The low bioavailability and in vivo stability of curcumin require the development of suitable carrier vehicles to deliver the molecule in a sustained manner at therapeutic levels.
- 2 In the present study, we investigated the feasibility and potential of poly(caprolactone) (PCL) nanofibres as a delivery vehicle for curcumin for wound healing applications. By optimizing the electrospinning parameters, bead‐free curcumin‐loaded PCL nanofibres were developed.
- 3 The fibres showed sustained release of curcumin for 72 h and could be made to deliver a dose much lower than the reported cytotoxic concentration while remaining bioactive. Human foreskin fibroblast cells (HFF‐1) showed more than 70% viability on curcumin‐loaded nanofibres.
- 4 The anti‐oxidant activity of curcumin‐loaded nanofibres was demonstrated using an oxygen radical absorbance capacity (ORAC) assay and by the ability of the fibres to maintain the viability of HFF‐1 cells under conditions of oxidative stress.
- 5 The curcumin‐loaded nanofibres also reduced inflammatory induction, as evidenced by low levels of interleukin‐6 release from mouse monocyte–macrophages seeded onto the fibres following stimulation by Escherichia coli‐derived lipopolysaccharide.
- 6 The in vivo wound healing capability of the curcumin loaded PCL nanofibres was demonstrated by an increased rate of wound closure in a streptozotocin‐induced diabetic mice model.
- 7 These results demonstrate that the curcumin‐loaded PCL nanofibre matrix is bioactive and has potential as a wound dressing with anti‐oxidant and anti‐inflammatory properties.
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Anti‐inflammatory and analgesic activities of cupressuflavone from Cupressus macrocarpa: Impact on pro‐inflammatory mediators 下载免费PDF全文
Eman Al‐Sayed Haidy A. Gad Mohamed El‐Shazly Mohamed M. Abdel‐Daim Abdel Nasser Singab 《Drug development research》2018,79(1):22-28
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