Academic literature on the topic 'Indomethacin derivatives'

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Journal articles on the topic "Indomethacin derivatives"

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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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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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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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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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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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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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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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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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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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Book chapters on the topic "Indomethacin derivatives"

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KAHÁNNÉ-LÁSZLÓ, ILONA, I. LEPRÁN, M. KOLTAI, and L. SZEKERES. "EFFECT OF IS, A WATER SOLUBLE DERIVATIVE OF INDOMETHACIN, ON THE OUTCOME OF THE VERY EARLY PHASE OF EXPERIMENTAL MYOCARDIAL INFARCTION IN CONSCIOUS RATS." In Advances in Pharmacological Research and Practice. Elsevier, 1986. http://dx.doi.org/10.1016/b978-0-08-034190-3.50028-2.

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Conference papers on the topic "Indomethacin derivatives"

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Zakai, Uzma I., Stephen Gately, and Robert West. "Abstract C50: Novel silicon derivatives of indomethacin: Generation of potent COX‐2 selective agents with improved anticancer activity." In Abstracts: First AACR International Conference on Frontiers in Basic Cancer Research--Oct 8–11, 2009; Boston MA. American Association for Cancer Research, 2009. http://dx.doi.org/10.1158/0008-5472.fbcr09-c50.

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Zakai, Uzma I., Stephen Gately, and Robert West. "Abstract 668: Second generation silicon derivatives of indomethacin: Synthesis of potent COX-2 selective agents with improved anticancer activity." In Proceedings: AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-668.

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