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Journal articles on the topic 'Indomethacin derivatives'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

Deng, Kui Lin, Chun Xiu Li, Ting Gao, et al. "Preparation and Drug Release Behavior from a Temperature-Sensitive Poly(aspartic Acid) Derivatives Hydrogel." Advanced Materials Research 711 (June 2013): 18–21. http://dx.doi.org/10.4028/www.scientific.net/amr.711.18.

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In this paper, a new pH/temperature-sensitive beads with semi-interpenetrating polymeric network based on sodium alginate(SA) and poly(aspartic acid) derivatives(M-E-PSI) were prepared using as drug delivery carrier. With indomethacin as a drug model，we investigated the release behaviors of indomethacin in different pH value, temperature and ratio of SA/ M-E-PSI. It turned out that the release amount of indomethacin in pH=2.1 phosphate buffer solution(PBS) was evidently higher than that in pH=7.4 PBS. And also, the release amount of indomethacin was also increased with increasing temperature a

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2

Abualhasan, Murad, Nidal Jaradat, Raghad Maslamani, Dana Nofal, and Linda Omar. "Synthesis of enhanced lipid solubility of indomethacin derivatives for topical formulations." Heterocyclic Communications 28, no. 1 (2022): 124–29. http://dx.doi.org/10.1515/hc-2022-0013.

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Abstract Indomethacin is a nonselective nonsteroidal anti-inflammatory drug with serious side effects such as depression, hallucination, and gastrointestinal irritation. This study aims to enhance indomethacin lipid solubility of indomethacin derivative to use it for the topical formulation since topical formulation may lower the unwanted side effects. The lipid solubility was achieved by adding various alkyl groups (methyl, ethyl, propyl, and isopropyl) to the drug via an ester linkage. The measured log p of these compounds was higher compared to the underivatized indomethacin. Furthermore, a

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3

Lauro, Figueroa-Valverde, Díaz-Cedillo Francisco, García-Cervera Elodia, et al. "Activity Exerted by a Testosterone Derivative on Myocardial Injury Using an Ischemia/Reperfusion Model." BioMed Research International 2014 (2014): 1–11. http://dx.doi.org/10.1155/2014/217865.

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Some reports indicate that several steroid derivatives have activity at cardiovascular level; nevertheless, there is scarce information about the activity exerted by the testosterone derivatives on cardiac injury caused by ischemia/reperfusion (I/R). Analyzing these data, in this study, a new testosterone derivative was synthetized with the objective of evaluating its effect on myocardial injury using an ischemia/reperfusion model. In addition, perfusion pressure and coronary resistance were evaluated in isolated rat hearts using the Langendorff technique. Additionally, molecular mechanism inv

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4

El-Gazzar, Abdel-Rahman, Hoda Hussein, and Hend Hafez. "Synthesis and biological evaluation of thieno[2,3-d]pyrimidine derivatives for anti-inflammatory, analgesic and ulcerogenic activity." Acta Pharmaceutica 57, no. 4 (2007): 395–411. http://dx.doi.org/10.2478/v10007-007-0032-6.

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Synthesis and biological evaluation of thieno[2,3-d]pyrimidine derivatives for anti-inflammatory, analgesic and ulcerogenic activity5-Methyl-6-phenyl-2-thioxothieno[2,3-d]pyrimidone derivative (2) reacted with hydrazonoyl chloride derivatives to afford triazolothienopyrimidones4a-f.Also, acetone-1-(2-amino-5-isopropyl-thiophene-3-carbonitrile) (3) reacted with functional and bifunctional groups to yield the corresponding compounds5-11. The new products showed anti-inflammatory, analgesic, and ulcerogenic activities comparable to that of indomethacin and acetylsalicylic acid, respectively.

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5

Kuźmycz, Olga, Aleksandra Kowalczyk, and Paweł Stączek. "Biological Activity of fac-[Re(CO)3(phen)(aspirin)], fac-[Re(CO)3(phen)(indomethacin)] and Their Original Counterparts against Ishikawa and HEC-1A Endometrial Cancer Cells." International Journal of Molecular Sciences 23, no. 19 (2022): 11568. http://dx.doi.org/10.3390/ijms231911568.

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Nonsteroidal anti-inflammatory drugs (NSAIDs) are inhibitors of cyclooxygenase enzyme (COX) and were found to have positive effects in reducing the risk of developing gynecological cancers. However, long-term administration of NSAIDs carries the risk of various side effects, including those in the digestive and circulatory systems. Therefore, there is a constant need to develop new NSAID derivatives. In this work, we investigated rhenium NSAIDs, comparing their effects on endometrial cancer cells with original NSAIDs, demonstrating the high activity of aspirin and indomethacin derivatives. The

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6

Serra Moreno, Judith, Dimitrios Agas, Maria Giovanna Sabbieti, Matteo Di Magno, Antonella Migliorini, and M. Antonietta Loreto. "Synthesis of novel pyrrolyl-indomethacin derivatives." European Journal of Medicinal Chemistry 57 (November 2012): 391–97. http://dx.doi.org/10.1016/j.ejmech.2012.09.008.

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7

Mahdi, Monther Faisal, Ashour H. Dawood, and Ahmed Kareem Hussein. "Design, Synthesis and Preliminary Pharmacological Evaluation of Mutual Prodrug of Non-Steroidal Anti-Inflammatory Drugs Coupling With Natural Anti-Oxidants Via Glycine." Al Mustansiriyah Journal of Pharmaceutical Sciences 13, no. 1 (2013): 155–69. http://dx.doi.org/10.32947/ajps.v13i1.211.

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Non-steroidal anti-inflammatory drugs (NSAIDs); naproxen and indomethacin have been conjugated with different antioxidants (thymol, menthol & guaiacol) having antiulcerogenic activity via glycine amino acid as spacer with the objective of obtaining NSAIDs-glycine- antioxidant prodrugs as gastrosparing NSAIDs devoid of ulcerogenic side effects and synergistically with anti-inflammatory action of glycine. Four mutual prodrugs (IIV) were synthesized using glycine as spacer and their structures were confirmed and characterized using elemental microanalysis (CHNO), IR, and some physiochemical p

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8

Benedek, G., P. Tóth-Daru, J. Janáky, A. Hortobágyi, F. Obál, and K. Colner-Sasi. "Indomethacin is Effective Against Neurogenic Hyperthermia Following Cranial Trauma or Brain Surgery." Canadian Journal of Neurological Sciences / Journal Canadien des Sciences Neurologiques 14, no. 2 (1987): 145–48. http://dx.doi.org/10.1017/s0317167100026275.

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Abstract:The effectiveness of indomethacin treatment (1 mg/kg) as an antipyretic was tested in patients after cranial trauma or brain surgery involving the centromedial forebrain. Indomethacin was effective in reducing temperature in 10 of 11 cases which showed a dipyrone-resistant hyperthermia developing in the first 24 hours after brain damage, while no significant antipyretic effect was seen in hyperthermic cases developing more than 72 hours after cranial trauma or brain surgery. Biochemical tests estimating the effect of indomethacin, and pyrazolone derivatives on the arachidonic acid met

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9

El-Kashef, Hussein, Talaat El-Emary, Pierre Verhaeghe, Patrice Vanelle, and Maha Samy. "Anticancer and Anti-Inflammatory Activities of Some New Pyrazolo[3,4-b]pyrazines." Molecules 23, no. 10 (2018): 2657. http://dx.doi.org/10.3390/molecules23102657.

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New derivatives of pyrazolo[3,4-b]pyrazines and related heterocycles were synthesized using 5-amino-3-methyl-4-nitroso-1-phenyl-pyrazole (1) as a starting material. The 5-acetyl derivative 15 was shown to be a useful key intermediate for the synthesis of several derivatives of pyrazolopyrazines. Some of the prepared compounds were evaluated for their anti-inflammatory and anti-breast cancer MCF-7 cell line activities. SAR study showed that compounds 15 and 29 exhibited remarkable anti-inflammatory activity, where 15 showed the same activity as that of the reference drug indomethacin. On the ot

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Haskologlu, Ismail Celil, Emine Erdag, Ahmet Ozer Sehirli, Orhan Uludag, and Nurettin Abacioglu. "Exploring the Therapeutic Potential of Benzoxazolone Derivatives on the Circadian Clock: An In Silico and Hypothetical Approach." Chronobiology in Medicine 6, no. 2 (2024): 87–99. http://dx.doi.org/10.33069/cim.2024.0012.

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Objective: Pain conditions exhibit variations linked to circadian rhythms. Circadian rhythms, regulated by clock proteins, impact melatonin levels and immune functions. Melatonin, structurally similar to indomethacin, a non-steroidal anti-inflammatory drug, serves as an alternative in pain-related conditions. Literature suggests a correlation between melatonin-dependent regulation of circadian rhythm and reductions in pain complaints. 2(3<i>H</i>)-Benzoxazolone, known for its anti-inflammatory and analgesic properties, is a promising scaffold for drug design. In this study, pharmac

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11

Gibson, P. R., and D. P. Jewell. "Sulphasalazine and Derivatives, Natural Killer Activity and Ulcerative Colitis." Clinical Science 69, no. 2 (1985): 177–84. http://dx.doi.org/10.1042/cs0690177.

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1. The effects of sulphasalazine, 5-aminosalicylic acid (5-ASA), sulphapyridine and azodisalicylic acid (ADS) in vitro on the natural killer (NK) activity of peripheral blood mononuclear cells (MNC) have been examined and compared with those of the lipoxygenase inhibitor, nordihydroguaiaretic acid (NDGA) and the cyclooxygenase inhibitor, indomethacin. 2. Sulphasalazine, sulphapyridine and ADS inhibited NK activity with 50% inhibitory concentrations (IC50) of 0.7, 2.5 and 4.0 mmol/l respectively. The effect was rapidly reversible. In contrast, 5-ASA minimally inhibited NK activity at 50 mmol/l

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12

Garg, Ajay Kumar, Ranjan Kumar Singh, Vaibhav Saxena, Saurabh Kr Sinha, and Sanjay Rao. "Synthesis, Characterization, and Anti-inflammatory activity of Some Novel Oxazole Derivatives." Journal of Drug Delivery and Therapeutics 13, no. 1 (2023): 26–28. http://dx.doi.org/10.22270/jddt.v13i1.5719.

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A series of novel oxazole derivatives (A, A1, A2) were synthesized starting from acetone and urea. The compound (A) was obtained by heating it with acetophenone and urea in iodine. Compound (A) on treatment with 4-amino benzaldehyde (Z)-N-(4-amino benzylidine)-4-((E)-Penta-2, 4-diene-2) oxazole-2-amine afforded (A1). Acylation of compound (A) with 4-amino benzoyl chloride to obtain the corresponding N-(4 phenyl oxazole-2- yl)- benzamide (A2). The structures of compounds have been established employing FTIR and 1H-NMR spectral analysis. All oxazole derivatives were evaluated for anti-inflammato

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13

Dvořáková, Kristýna, Petr Štěpánek, Jiřina Kroupová, and Jarmila Zbytovská. "N-Alkylmorpholines: Potent Dermal and Transdermal Skin Permeation Enhancers." Pharmaceutics 14, no. 1 (2021): 64. http://dx.doi.org/10.3390/pharmaceutics14010064.

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Transdermal drug delivery is an attractive non-invasive method offering numerous advantages over the conventional routes of administration. The main obstacle to drug transport is, however, the powerful skin barrier that needs to be modulated, for example, by transdermal permeation enhancers. Unfortunately, there are still only a few enhancers showing optimum properties including low toxicity and reversibility of enhancing effects. For this reason, we investigated a series of new N-alkylmorpholines with various side chains as potential enhancers in an in vitro permeation study, using three mode

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14

Nora, Amer Hussien, Y. Hussien Hyffaa, and H. Abdulrahman Shaymaa. "Predictive biological activity of newly synthesized hydrazone compounds derived from indomethacin." Journal of Wildlife and Biodiversity 7, Special Issue (2023): 391–402. https://doi.org/10.5281/zenodo.10246323.

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New derivatives of hydrazone have been successfully created, specifically 2-(1-(Aryl)-5-methoxy-2-methyl-1H-indol-3-yl)-N'-(2-chlorobenzylidene) acetohydrazide. The transformation of Indomethacin ester into hydrazide was achieved through a reaction with hydrazine hydrate in absolute ethanol, followed by the reaction of the resulting hydrazide with aromatic aldehydes. The structures of these newly synthesized hydrazones were validated through IR, 1HNMR, and 13CNMR analyses. Each compound's energies were optimized by utilizing density functional theory (DFT) for theoretical calculations. By empl

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15

Mustafa Taha Abdull, Monther F. Mahdi, and Ayad k. Khan. "Molecular docking, Synthesis and Characterization of New Indomethacin and Mefenamic Acid Analogues as Potential Anti-inflammatory Agents." Al Mustansiriyah Journal of Pharmaceutical Sciences 23, no. 3 (2023): 336–44. http://dx.doi.org/10.32947/ajps.v23i3.1052.

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In this work the pharmacological study and synthesis of new thiadiazine bearing on triazole which obtained from hippuric acid , indomethacin and mefenamic acid that have carboxylic acid moiety, Drugs with carboxylic groups and thiocarbohydrazide interacted to produce the 4-amino-5-aryl-4H-1,2,4-triazole-3-thiol (1a-c). and the starting products 4-amino-5-aryl-4H-1,2,4-triazole-3-thiol) were treated with chloroacetyl chloride to produce final products (2a-c). To confirm the structure of the generated compounds, FT-IR, 1H-NMR, and mass spectroscopy were used to characterize all derivatives

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16

Al-Masoudi, Najim A., Nadhir N. A. Jafar, Layla J. Abbas, Sadiq J. Baqir, and Christophe Pannecouque. "Synthesis and anti-HIV Activity of New Benzimidazole, Benzothiazole and Carbohyrazide Derivatives of the anti-Inflammatory Drug Indomethacin." Zeitschrift für Naturforschung B 66, no. 9 (2011): 953–60. http://dx.doi.org/10.1515/znb-2011-0914.

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There is an urgent need for the design and development of new and safer drugs for the treatment of HIV infection, active against the currently resistant viral strains. New derivatives of the non-steroidal anti-inflammatory drug indomethacin bearing benzimidazoles, benzothiazole, purine and pyridine residues 8 - 13 were synthesized with the aim of developing new non-nucleoside reverse transcriptase inhibitors (NNRTIs).Alternatively, new imine analogs 16 - 20 were synthesized from condensation of indomethacinyl hydrazide 15, prepared from the ester 14, with various ketone precursors. Treatment o

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17

Hamed, Amany M., Souhaila S. Enaili, Walaa I. Mohammed, et al. "Novel Benzenesulfonamide Derivatives of 5′-Aminospirotriazolotriazine Exhibit Anti-Inflammatory Activity by Suppressing Pro-Inflammatory Mediators: In Vitro and In Vivo Evaluation Using a Rat Model of Carrageenan-Induced Paw Edema." Biomedicines 13, no. 7 (2025): 1732. https://doi.org/10.3390/biomedicines13071732.

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Background/Objectives: Inflammation is a crucial and complex mechanism that protects the body against infections. In our study, we propose to provide scientific evidence for the anti-inflammatory properties of 1,3,5-triazine derivatives. Methods: Initially, we ensured the safety of the three synthesized derivatives by administering graded doses of up to 2000 mg/kg intraperitoneally in Wistar rats. Thus, the three derivatives were considered generally safe. We also evaluated their ability to reduce carrageenan-induced rat paw edema. Results: Compounds 1, 2, and 3 demonstrated stronger anti-infl

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Mohamed, Mosaad S., Aymn E. Rashad, Mostafa Adbel-Monem, and Samar S. Fatahalla. "New Anti-Inflammatory Agents." Zeitschrift für Naturforschung C 62, no. 1-2 (2007): 27–31. http://dx.doi.org/10.1515/znc-2007-1-205.

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The pyrrole derivatives 1a, b and 2a, b were used as precursors for the preparation of N-substituted pyrrole derivatives 3a, b-9a, b and pyrrolo[2,3-d]pyrimidines 13-16. Also, all the newly prepared products were tested for anti-inflammatory activity as analogues to fenamates, and some of them revealed moderate anti-inflammatory activity compared to the standard drug indomethacin.

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19

Brousseau, Danica, Jean-François Desjardins, Gaëtan Jasmin, and Louis Dumont. "Altered coronary and cardiac adrenergic response in the failing hamster heart: role of cyclooxygenase derivatives." Canadian Journal of Physiology and Pharmacology 80, no. 3 (2002): 218–25. http://dx.doi.org/10.1139/y02-042.

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Although the influence of the adrenergic system has been studied in the presence of heart failure, controversies still exist. Since cyclooxygenase derivatives appear to modulate coronary and cardiac adaptation in the failing heart, we hypothesized that cyclooxygenase derivatives may participate in the altered adrenergic responses in this situation. Isolated hearts from cardiomyopathic (UM-X7.1 subline) and normal hamsters, aged >240 days, were utilized. Coronary and cardiac response to α1-, β1-, and β2-adrenergic stimulations was observed before and after pretreatment with indomethacin, a c

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Andreani, Aldo, Alberto Leoni, Alessandra Locatelli, et al. "Ring-Opened Analogs of Indomethacin Affecting Human Neutrophil Functions." Collection of Czechoslovak Chemical Communications 64, no. 2 (1999): 299–312. http://dx.doi.org/10.1135/cccc19990299.

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A series of ring-opened analogs of indomethacin was synthesized and tested in vitro (at concentrations ranging from 10-9 to 10-5 mol/l) on human neutrophil functions. Two compounds lacking the carboxylic group were subjected to the same tests and one of these showed unexpected activity. Among the acidic derivatives, compound 12 bearing the same substituents as indomethacin 10 (methoxy and 4-chlorobenzoyl groups) was the most active: it significantly lowered neutrophil responses in all five bioassays and at the three concentrations considered.

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21

Kassab, Asmaa E., and Ehab M. Gedawy. "Repurposing of Indomethacin and Naproxen as anticancer agents: progress from 2017 to present." RSC Advances 14, no. 54 (2024): 40031–57. https://doi.org/10.1039/d4ra07581a.

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To aid in potential future repositioning of NSAIDs for cancer treatment, we summarize work from 2017–2024 on the antiproliferative activity of derivatives of indomethacin and naproxen, their mechanism of action and structure–activity relationships.

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22

Pop, Raluca, and Dušanka Janežič. "Interactions of Indomethacin with Functionalized Rhombellanes – a Molecular Docking Study." Croatica chemica acta 92, no. 4 (2020): 503–9. http://dx.doi.org/10.5562/cca3591.

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The specific properties of carbon-based nanomaterials like fullerenes and graphenes have attracted a continuous interest for their possible use as drug carriers. The functionalization of these nanomaterials can lead to the variation or improvement of the required properties, in order to lead to the design of the most suitable compounds within a specific field. In this regard, the possible use of a new class of nanostructures -the rhombellanes- as nanocarriers is investigated. The aim of the paper is to study the interactions of indomethacin and four analogues with anti-inflammatory activity on

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23

OBATA, TOHRU, SARA SHIRATANI, TOMOMI NADA, et al. "Structure-activity Relationship of Indomethacin Derivatives as IDO1 Inhibitors." Anticancer Research 41, no. 5 (2021): 2287–96. http://dx.doi.org/10.21873/anticanres.15004.

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24

Moth, Christopher W., Jeffrey J. Prusakiewicz, Larry J. Marnett, and Terry P. Lybrand. "Stereoselective Binding of Indomethacin Ethanolamide Derivatives to Cyclooxygenase-1." Journal of Medicinal Chemistry 48, no. 10 (2005): 3613–20. http://dx.doi.org/10.1021/jm0494164.

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25

Tok, Fatih, and Bedia Koçyiğit-Kaymakçıoğlu. "Design, Synthesis and Biological Screening of Novel 1,5-Diphenyl-3-(4-(trifluoromethyl)phenyl)-2-pyrazoline Derivatives." Acta Chimica Slovenica 67, no. 4 (2020): 1139–47. http://dx.doi.org/10.17344/acsi.2020.6028.

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1-Phenyl-5-substituted-3-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-pyrazole derivatives were synthesized from chalcone derivatives. The structures of compounds were characterized by IR, 1H NMR spectroscopic methods and elemental analysis. All compounds were evaluated for their in vitro antioxidant activity using DPPH and ABTS methods, anti-inflammatory activity using lipoxygenase inhibitory method and antidiabetic activity using the α-glucosidase inhibitory method. Especially, pyrazoline derivatives exhibited stronger anti-inflammatory activity than the reference drug indomethacin (IC50: 50.4

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Hall, Iris H., Bruce S. Burnham, Shang Y. Chen, Anup Sood, Bernard F. Spielvogel, and Karen W. Morse. "The Anti-Inflammatory Activity of Boron Derivatives in Rodents." Metal-Based Drugs 2, no. 1 (1995): 1–12. http://dx.doi.org/10.1155/mbd.1995.1.

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Acyclic amine-carboxyboranes were effective anti-inflammatory agents in mice at 8 mg/kg x 2. These amine-carboxyboranes were more effective than the standard indomethacin at 8 mg/kg x 2, pentoxifylline at 50 mg/kg x 2, and phenylbutazone at 50 mg/kg x 2. The heterocyclic amine derivatives as well as amine-carbamoylboranes, carboalkoxyboranes, and cyanoboranes were generally less active. However, selected aminomethyl-phosphonate-N-cyanoboranes demonstrated greater than 60% reduction of induced inflammation. The boron compounds were also active in the rat induced edema, chronic arthritis, and pl

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27

Mazzoni, MR, and A. Lucacchini. "Evidence for the Existence of A Specific Binding Site for Indomethacin on Bovine Vesicular Gland Microsomes." Biotechnology and Applied Biochemistry 9, no. 4 (1987): 339–45. http://dx.doi.org/10.1111/j.1470-8744.1987.tb00482.x.

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Using bovine vesicular gland microsomes and [14C]indomethacin we demonstrated the presence of a specific binding site for nonsteroidal anti‐inflammatory drugs. Specific binding of [14C]indomethacin to microsomes was rapid, with most of the ligand bound by 2 min at 4 degrees C. In routine binding assays the incubation temperature was maintained at 4 degrees C, because the maximal specific binding was obtained. Specific [14C]indomethacin binding appeared to increase linearly with increasing protein concentration over the range of 0.1‐1.0 mg of microsomal protein. Specific binding was saturable a

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El-Ossaily, Yasser A., Nuha M. M. Alanazi, Ibrahim O. Althobaiti, et al. "Multicomponent approach to the synthesis and spectral characterization of some 3,5-pyrazolididione derivatives and evaluation as anti-inflammatory agents." Current Chemistry Letters 13, no. 1 (2024): 127–40. http://dx.doi.org/10.5267/j.ccl.2023.8.003.

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Pyrazolones are a class of heterocyclic compounds that contain a pyrazole ring fused to a ketone group. Recent scientific research has focused extensively on the potential anti-inflammatory properties of pyrazolone compounds due to their diverse pharmacological effects in alleviating inflammation and reducing fever. This motivated us to focus on the preparation of these derivatives in a simple and eco-friendly manner. A convenient new green methodology was modified for the preparation of 1-phenyl-3,5-pyrazolidinedione by the sonicated MCR of diethyl malonate, phenylhydrazine, and a catalytic a

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Wells, Isabelle, and Lawrence J. Marnett. "Inactivation of prostaglandin endoperoxide synthase by acylating derivatives of indomethacin." Biochemistry 32, no. 10 (1993): 2710–16. http://dx.doi.org/10.1021/bi00061a032.

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Chennamaneni, Snigdha, Chunfang Gan, Rati Lama, Bo Zhong, and Bin Su. "Indomethacin derivatives as tubulin stabilizers to inhibit cancer cell proliferation." Bioorganic & Medicinal Chemistry 24, no. 2 (2016): 277–85. http://dx.doi.org/10.1016/j.bmc.2015.12.016.

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Zhou, Yuxiang, Chenglong Li, Xiaoyan Yuan, Feiyan Zhang, Xiaozu Liu та Peijun Liu. "Cobalt-catalyzed C2α-acyloxylation of 2-substituted indoles with tert-butyl peresters". Organic & Biomolecular Chemistry 17, № 13 (2019): 3343–47. http://dx.doi.org/10.1039/c9ob00159j.

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An efficient cobalt-catalyzed C2α selective C(sp<sup>3</sup>)–H acyloxylation of 2-substituted indoles with tert-butyl peresters to synthesize diverse 2α-acyloxylated indole derivatives is described. This developed method exhibits mild conditions, low-cost catalyst, and high functional group compatibility. The effectiveness of this chemistry is illuminated by a late-stage modification of methylated indomethacin.

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Amrita, Dwivedi, and K. Srivastava A. "Modeling of inhibitory activity of indomethacin derivatives as COX-2 inhibitors through QSAR analysis." Journal of Indian Chemical Society 93, Jul 2016 (2016): 795–98. https://doi.org/10.5281/zenodo.5638006.

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QSAR Laboratory, Department of Chemistry, University of Allahabad, Allahabad-211 002, Uttar Pradesh, India <em>E-mail</em> : srivastavaak50@gmail.com Quantitative structure-activity relationships (QSAR) study has been performed on a series of indomethacin derivatives using topological and physicochemical parameters. Several QSAR equations were formulated through regression analysis by grouping these descriptors. It has been demonstrated that empirical parameters such as D, St, IOR along with indicator parameter have considerable effect on the inhibitory activity of these derivatives towards CO

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Ermekova, Dinara, and Isabek Ismailov. "CONTENT-ANALYSIS OF THE PHARMACEUTICAL MARKET OF NONSTEROIDAL ANTI-INFLAMMATORY DRUGS IN GROUPS OF ACETIC ACID DERIVATIVES IN THE KYRGYZ REPUBLIC." Avicenna Bulletin 22, no. 1 (2020): 74–81. http://dx.doi.org/10.25005/2074-0581-2020-22-1-74-81.

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Objective: To segment the pharmaceutical market of non-steroidal anti-inflammatory drugs (NSAIDs) of the derivatives groups of acetic acid in the Kyrgyz Republic. Methods: The database of the State Registry of Medicines registered and approved for Medical use in Kyrgyzstan, the Department of Drugs Security and Medical Engineering of the Ministry of Health of the Kyrgyz Republic is used for analysis. Results: Analysis showed that the leaders of the pharmaceutical market in Kyrgyzstan the number of registered medicines (M) under the trade names are Medical Drugs (MD) with international generic n

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Xavier, Fabiano E., Javier Blanco-Rivero, Esther Sastre, Lina Badimón, and Gloria Balfagón. "Simultaneous inhibition of TXA2 and PGI2 synthesis increases NO release in mesenteric resistance arteries from cirrhotic rats." Clinical Science 119, no. 7 (2010): 283–92. http://dx.doi.org/10.1042/cs20090536.

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Our present study examines, in mesenteric resistance arteries, possible vasodilation alterations, and the role of NO and COX (cyclo-oxygenase) derivatives, in cirrhosis. The vasodilator response to acetylcholine was analysed in segments from control and cirrhotic rats. The effects of the non-specific COX inhibitor indomethacin, the specific COX-1 inhibitor SC-560 and the specific COX-2 inhibitor NS-398 were analysed in segments from both groups of rats. NO release was measured, and eNOS [endothelial NOS (NO synthase)], phospho-eNOS, iNOS (inducible NOS), COX-1 and COX-2 protein expression was

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Kant, Geeta, Anupama Parate, and SC Chaturvedi. "2D-QSAR study of indomethacin ester derivatives as cyclooxygenase-2- inhibitors." Indian Journal of Pharmaceutical Sciences 68, no. 6 (2006): 826. http://dx.doi.org/10.4103/0250-474x.31029.

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Amin, Mohamed M., Mohamed R. Shaaban, Nadia T. Al-Qurashi, Huda K. Mahmoud, and Thoraya A. Farghaly. "Indomethacin Analogs: Synthesis, Anti-inflammatory and Analgesic Activities of Indoline Derivatives." Mini-Reviews in Medicinal Chemistry 18, no. 16 (2018): 1409–21. http://dx.doi.org/10.2174/1389557518666180330101447.

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Zhang, Jiquan, Jianta Wang, Haoshu Wu, et al. "Design, synthesis and insulin-sensitizing activity of indomethacin and diclofenac derivatives." Bioorganic & Medicinal Chemistry Letters 19, no. 12 (2009): 3324–27. http://dx.doi.org/10.1016/j.bmcl.2009.04.050.

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Scholz, Matthias, Anna L. Blobaum, Lawrence J. Marnett, and Evamarie Hey-Hawkins. "Synthesis and evaluation of carbaborane derivatives of indomethacin as cyclooxygenase inhibitors." Bioorganic & Medicinal Chemistry 19, no. 10 (2011): 3242–48. http://dx.doi.org/10.1016/j.bmc.2011.03.054.

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Scholz, Matthias, Anna L. Blobaum, Lawrence J. Marnett, and Evamarie Hey-Hawkins. "ortho-Carbaborane derivatives of indomethacin as cyclooxygenase (COX)-2 selective inhibitors." Bioorganic & Medicinal Chemistry 20, no. 15 (2012): 4830–37. http://dx.doi.org/10.1016/j.bmc.2012.05.063.

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Amir, Mohd, and Shikha Kumar. "Anti-inflammatory and Gastro Sparing Activity of Some New Indomethacin Derivatives." Archiv der Pharmazie 338, no. 1 (2005): 24–31. http://dx.doi.org/10.1002/ardp.200400891.

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Camacho-Camacho, Carlos, Irma Rojas-Oviedo, M. Angeles Paz-Sandoval, et al. "Synthesis, structural characterization and cytotoxic activity of organotin derivatives of indomethacin." Applied Organometallic Chemistry 22, no. 3 (2008): 171–76. http://dx.doi.org/10.1002/aoc.1366.

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42

Bafail, Rawan S. M., and Waad A. Samman. "Anti-parkinsonian, anti-inflammatory, anti-microbial, analgesic, anti-hyperglycemic and anticancer activities of poly-fused ring pyrimidine derivatives." Tropical Journal of Pharmaceutical Research 23, no. 1 (2024): 67–75. http://dx.doi.org/10.4314/tjpr.v23i1.9.

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Purpose: To investigate the anti-inflammatory, anti-cancer, anti-parkinsonian, anti-microbial, analgesic, and anti-hyperglycemic properties of a variety of poly-fused pyrimidine derivatives. Methods: A novel series of fused pyrimidine derivatives 1-6 were synthesized by reacting amino pyrazole derivatives with active methylene derivatives to give the corresponding compounds 1-6. Anti-parkinsonian activity was investigated with benzotropene as a reference drug, anti-inflammatory effect in mice was evaluated using carrageenan in paw edema with indomethacin as reference drug, anti-microbial

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Lee, Bong-Seop, Xiangpeng Yuan, Qijin Xu, et al. "Nanoprodrugs of NSAIDs Inhibit the Growth of U87-MG Glioma Cells." Journal of Nanomaterials 2010 (2010): 1–10. http://dx.doi.org/10.1155/2010/583970.

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Several recent reports have demonstrated that nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit the growth of various malignant cells suggesting their application as anticancer agents. In this study, we prepared six nanometer-sized prodrugs (nanoprodrugs) of NSAIDs, ibuprofen, indomethacin, and naproxen through the spontaneous emulsification mechanism using monomeric and dimeric derivatives of the NSAIDs. We evaluated their effect on the proliferation of U87-MG glioma cells by cell counting, WST-1 cell proliferation reagent, and propidium iodide incorporation. The two ibuprofen nanoprodrug

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Menshawy, A. Mohamed* Adnan A. Beckeit Adel S. El-Azab Ghada F. Mohamed Sami G. Abdel-Hamid and Maged S. Abdel-Kader. "SYNTHESIS AND EVALUATION OF SOME UMBELLIFERONE DERIVATIVES AS ANTI-INFLAMMATORY AGENTS." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES 05, no. 12 (2018): 16165–77. https://doi.org/10.5281/zenodo.2268635.

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<em>S</em><em>eventeen 7-hydroxy coumarin (umbelliferone) derivatives were synthesized in an almost quantitative yield via reaction with the corresponding ethylchloroacetate, p-substituted benzyl chloride, 2-bromoacetophenone or 2-chloroacetanilide in the presence of anhydrous potassium carbonate in dry acetone.  The compounds were tested for their anti-inflammatory activity using cotton pellet implantation test and carrageenan-induced rat paw edema. The ulcerogenic effect of the compounds was also studied comparing with the NSAID indomethacin.</em> <strong>Keywords : </strong><em>7-Hydro

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Stadlbauer, Sven, René Frank, Matthias Scholz, et al. "Imitation and modification of bioactive lead structures via integration of boron clusters." Pure and Applied Chemistry 84, no. 11 (2012): 2289–98. http://dx.doi.org/10.1351/pac-con-11-11-02.

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In medicinal chemistry, carbaboranes can be employed either as boron carriers for boron neutron capture therapy (BNCT) or as scaffolds for radiodiagnostic or therapeutic agents. We have developed a suitable synthesis employing the phosphoramidite method to connect meta-carbaboranyl bis-phosphonites with the 6'-OH group of isopropylidene-protected galactose, followed by oxidation or sulfurization to give the corresponding bis-phosphonates. Deprotection yielded water-soluble compounds. The corresponding disodium salts exhibit especially low cytotoxicity. Preliminary results on the in vivo toxici

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Felts, Andrew S., Chuan Ji, Jennifer B. Stafford, et al. "Desmethyl Derivatives of Indomethacin and Sulindac as Probes for Cyclooxygenase-Dependent Biology." ACS Chemical Biology 2, no. 7 (2007): 479–83. http://dx.doi.org/10.1021/cb700077z.

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De Caprariis, Paolo, Francesco Palagiano, Franco Bonina, Lucia Montenegro, Michele D'Amico, and Francesco Rossi. "Synthesis and Pharmacological Evaluation of Oligoethylene Ester Derivatives as Indomethacin Oral Prodrugs." Journal of Pharmaceutical Sciences 83, no. 11 (1994): 1578–81. http://dx.doi.org/10.1002/jps.2600831112.

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Hegab, Mohamed, Nabil Yousef, Hany Nour, Mohey Ellithey, and Mahmoud Arbid. "Synthesis and pharmacological activities of some condensed 4-chloro-2,2-dialkyl chromene-3-carbaldehyde derivatives." Acta Pharmaceutica 58, no. 1 (2008): 15–27. http://dx.doi.org/10.2478/v10007-007-0042-4.

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Synthesis and pharmacological activities of some condensed 4-chloro-2,2-dialkyl chromene-3-carbaldehyde derivativesSome new hydrazono5a,b, thiosemicarbazono6a-c, and oximo chromenes7a-cwere preparedviathe reaction of the corresponding β-chlorocarbaldehyde3with hydrazine, aromatic hydrazine, thiosemicarbazide and hydroxylamine hydrochloride, respectively. In addition, ether derivatives8a-hwere prepared from the corresponding aldoximes7a-c. The new products were tested for anti-inflammatory and ulcerogenic score activities compared to indomethacin.

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Knight, John, Andrew F. Rowley, Mizue Yamazaki, and Anthony S. Clare. "Eicosanoids are modulators of larval settlement in the barnacle, Balanus amphitrite." Journal of the Marine Biological Association of the United Kingdom 80, no. 1 (1999): 113–17. http://dx.doi.org/10.1017/s0025315499001629.

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Eicosanoids are oxygenated derivatives of C20 polyunsaturated fatty acids known to play key roles in many physiological events in both invertebrates and vertebrates. The eicosanoid generating capacity of cypris larvae of the barnacle, Balanus amphitrite, was examined using enzyme immunoassay and high-performance liquid chromatography. These larvae generated the lipoxygenase products, 12-hydroxyeicosapentaenoic acid (HEPE), 8-HEPE and 8,15-diHEPE, together with the cyclooxygenase products, prostaglandin (PG) E, PGF and thromboxane (TX) B. Indomethacin, a selective cyclooxygenase inhibitor, caus

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Venugopala, Katharigatta N., Sandeep Chandrashekharappa, Christophe Tratrat, et al. "Crystallography, Molecular Modeling, and COX-2 Inhibition Studies on Indolizine Derivatives." Molecules 26, no. 12 (2021): 3550. http://dx.doi.org/10.3390/molecules26123550.

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The cyclooxygenase-2 (COX-2) enzyme is an important target for drug discovery and development of novel anti-inflammatory agents. Selective COX-2 inhibitors have the advantage of reduced side-effects, which result from COX-1 inhibition that is usually observed with nonselective COX inhibitors. In this study, the design and synthesis of a new series of 7-methoxy indolizines as bioisostere indomethacin analogues (5a–e) were carried out and evaluated for COX-2 enzyme inhibition. All the compounds showed activity in micromolar ranges, and the compound diethyl 3-(4-cyanobenzoyl)-7-methoxyindolizine-

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