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Journal articles on the topic 'Primary Moiety for The Synthesis of Anti-Inflammatory Agents'

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

Archana, Singh, Prasad Virendra, Rajkhowa Sanchayita, D. Tripathi Vishwa, and K. Tiwari Vinod. "Synthesis of glycosylated aminothiol from D-glucose as promising anti-tubercular agent." Journal of Indian Chemical Society Vol. 97, Feb 2020 (2020): 213–25. https://doi.org/10.5281/zenodo.5651696.

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Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi-221 005, Uttar Pradesh, India <em>E-mail</em>: tiwari_chem@yahoo.co.in, vinod.tiwari@bhu.ac.in Department of Chemistry, Gauhati University, Guwahati-781 014, Assam, India Department of Chemistry, M. K. College, L. N.Mithila University, Darbhanga-846 004, Bihar, India <em>Manuscript received online 29 September 2019, revised and accepted 18 January 2020</em> A facile method for a series of novel glycosylated β-aminothiols by employing TBAB/NEt<sub>3</sub> -catalyzed ring opening of thiirane ring of D-glucose-

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2

Sharkey, D. J., та S. A. Robertson. "229.Seminal plasma TGFβ activates pro-inflammatory cytokine synthesis in human cervical epithelial cells". Reproduction, Fertility and Development 16, № 9 (2004): 229. http://dx.doi.org/10.1071/srb04abs229.

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Exposure to semen at intercourse in women elicits an inflammation-like response characterised by recruitment of inflammatory cells and expression of pro-inflammatory cytokines including GM-CSF, interleukin-6 (IL-6) and IL-8 (1). Studies in animal models have implicated TGFβ as the major active moiety in seminal plasma, and we have shown previously that TGFβ1 and TGFβ3 are present in high concentrations in human seminal plasma (>100 ng/mL), while TGFβ2 is less abundant. To investigate the physiological significance of each of the three TGFβ isoforms as pro-inflammatory agents in human semina

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3

Pei, Shanshan, Kevin Callahan, Mohammad Minhajuddin, et al. "Targeting Redox Homeostasis As a Means to Selectively Eradicate Primary Human Leukemia Cells,." Blood 118, no. 21 (2011): 3506. http://dx.doi.org/10.1182/blood.v118.21.3506.3506.

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Abstract Abstract 3506 Many studies have indicated that induction of oxidative stress is one component of the mechanism by which anti-leukemia agents function. However, little is known about the differences between leukemic and normal redox homeostasis, and whether these agents achieve their selective toxicity to leukemia through specifically targeting leukemic redox homeostasis. Hence, the present study performed a detailed analysis of CD34+ cells derived from normal bone marrow (NBM) or primary acute myelogenous leukemia (AML) specimens. By evaluating the expression profiles of redox regulat

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4

Madadi, Nikhil R., Narsimha R. Penthala, Amit Ketkar, et al. "Synthesis and Evaluation of 2-Naphthaleno trans-Stilbenes and Cyanostilbenes as Anticancer Agents." Anti-Cancer Agents in Medicinal Chemistry 18, no. 4 (2018): 556–64. http://dx.doi.org/10.2174/1871521409666170412115703.

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Background: Naphthalene is a good structural replacement for the isovanillin moiety (i.e. the 3- hydroxy-4-methoxyphenyl unit) in the combretastatin A-4 molecule, a natural product structurally related to resveratrol, which consistently led to the generation of highly cytotoxic naphthalene analogues when combined with a 3,4,5-trimethoxyphenyl or related aromatic system. Also, the naphthalene ring system is present in many current drug molecules that are utilized for anti-tumor, anti-arrhythmia and antioxidant therapy. Objective: In our continuing quest to improve the potencies of naturally occ

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5

Allart-Simon, Ingrid, Aurélie Moniot, Nicolo Bisi, et al. "Pyridazinone derivatives as potential anti-inflammatory agents: synthesis and biological evaluation as PDE4 inhibitors." RSC Medicinal Chemistry 12, no. 4 (2021): 584–92. http://dx.doi.org/10.1039/d0md00423e.

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6

Mamatha, S. V., S. L. Belagali, and Mahesh Bhat. "Synthesis and SAR Evaluation of Mercaptotriazolo derivatives as anti-inflammatory agents." International Journal of ChemTech Research 13, no. 1 (2020): 187–98. http://dx.doi.org/10.20902/ijctr.2019.130123.

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A new series of benzothiazole appended triazole derivatives were synthesized. Characterization is done by FT-IR, Mass, 1H and 13C NMR spectroscopic techniques. The newly synthesized compounds were screened for antioxidant and anti inflammatory activities. Experimental data hypothesized compound 7b as highly potent cytotoxicant with lengthened activity. Structure–activity relation interrelates the biological activity and chemical moiety of the molecule. Structurally, 7b is a benzothiazolyltriazole having a pyrrolidine group (five membered ring) attached to two CH2 groups and methyl substituent

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7

R. Makwana, Hetal, and Atul H. Makwana. "SYNTHESIS AND CHARACTERIZATION OF 1-(BENZOYL)-4- (ARYLIDENE)-3-METHYL-1H-PYRAZOL-5(4H)-ONES DERIVATIVES AND THEIR BIOLOGICAL ACTIVITIES." RASAYAN Journal of Chemistry 17, no. 04 (2024): 2062–66. https://doi.org/10.31788/rjc.2024.1748574.

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Pyrazole and its derivatives are considered pharmacologically active and itgives various types of biological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as a potent anti-inflammatory, anti-microbial, andanalgesic, has proved the pharmacological potential of the pyrazole moiety.

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8

Sahoo, Biswa M., Bera Venkata V. Ravi Kumar, Bimal K. Banik, and Preetismita Borah. "Green Efficient Synthesis of Oxadiazole Derivatives as Analgesic and Antiinflammatory Agents." Current Green Chemistry 7, no. 2 (2020): 163–78. http://dx.doi.org/10.2174/2213346107999200427080057.

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Non-steroidal anti-inflammatory drugs (NSAIDs) act as a major class of therapeutic agents. The biological activity of NSAIDs is due to the suppression of prostaglandin biosynthesis by inhibiting cyclooxygenase (COX) enzyme. COX is an endogenous enzyme, which catalyzes the conversion of arachidonic acid into prostaglandins. But the significant side effect by NSAIDs is the formation of gastric ulcers, irritation and GI bleeding. Therefore, alternative drugs that can overcome these limitations are necessary. Towards the goal, oxadiazole derivatives are designed and synthesized following a green c

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9

Vlachou, Evangelia-Eirini N., and Konstantinos E. Litinas. "An Overview on Pyranocoumarins: Synthesis and Biological Activities." Current Organic Chemistry 23, no. 24 (2020): 2679–721. http://dx.doi.org/10.2174/1385272823666191025151236.

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Pyrano- and dipyranocoumarins are classes of naturally occurring organic compounds with very interesting biological activities. This review focuses on the synthetic strategies for the synthesis of pyranocoumarins and dipyranocoumarins and the biological properties of those compounds. The synthesis involves the formation of the pyran ring, at first, from a coumarin or the formation of pyranone moiety from an existing pyran. Pyranocoumarins and dipyranocoumarins present anti-HIV, anti-cancer, neuroprotective, antidiabetic, antibacterial, antifungal, anti-inflammatory activities. Especially khell

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10

Vashisht, Ketan, Pooja Sethi, Anshul Bansal, et al. "Path of Pyrazoles from Synthetic Factors to Anti-inflammatory Potential: A Review." Asian Journal of Chemistry 36, no. 6 (2024): 1217–31. http://dx.doi.org/10.14233/ajchem.2024.31652.

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Pyrazoles, a class of heterocyclic compounds, have garnered considerable attention in drug development due to their intriguing properties, particularly those containing a pyrazole moiety. Pyrazole, a pivotal chemical in the creation of potent bioactive agents, encompasses five heterocyclic members. The discovery of certain pyrazole compounds exhibiting robust biological activities has spurred interest in this field of inquiry. Heterocyclic compounds incorporating nitrogen and its derivatives have historically served as crucial sources of medicinal compounds. Given that the heterocyclic group c

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Benny, Anjitha Theres, Sonia D. Arikkatt, Cijo George Vazhappilly, et al. "Chromone, A Privileged Scaffold in Drug Discovery: Developments in the Synthesis and Bioactivity." Mini-Reviews in Medicinal Chemistry 22, no. 7 (2022): 1030–63. http://dx.doi.org/10.2174/1389557521666211124141859.

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: Chromones are the class of secondary metabolites that broadly occur in the plant kingdom in a noticeable quantity. This rigid bicyclic system has been categorized “as privileged scaffolds in compounds” in medicinal chemistry. Their wide biological responses have made them an important moiety in a drug discovery program. This review provides updates on the various methods of synthesis of chromones and biological applications in medicinal chemistry. Various synthetic strategies for the construction of chromones include readily available phenols, salicylic acid and its derivatives, ynones, chal

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Khalil, Omneya M. "Synthesis of Some Chalcones and Pyrazolines Carrying Morpholinophenyl Moiety as Potential Anti-Inflammatory Agents." Archiv der Pharmazie 344, no. 4 (2010): 242–47. http://dx.doi.org/10.1002/ardp.201000245.

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13

MISHRA, KHUSHBOO, S. K. Jain, and P. K. Singour. "Synthesis and Biological Evaluation of pyrazole derivatives containing ethanone skeleton as Anti-inflammatory agents." Journal of Drug Delivery and Therapeutics 9, no. 3 (2019): 40–47. http://dx.doi.org/10.22270/jddt.v9i3.2736.

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Current research had focused on the synthesis of the novel pyrazole ethanone linked compounds with improved biological activity. In this synthetic process 1st step was to synthesize the intermediate chalcone and 2nd step was the synthesis of final compound pyrazole derivative containing ethanone moiety. This procedure is the type of cyclization reaction using proton transfer mechanism. By using this method 8 derivatives synthesized. After synthesis these were subjected to identification tests by using various methods like melting point study, thin layer chromatography, solubility study and cha

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14

Markov, Andrey V., Aleksandra V. Sen’kova, Oksana V. Salomatina та ін. "Trioxolone Methyl, a Novel Cyano Enone-Bearing 18βH-Glycyrrhetinic Acid Derivative, Ameliorates Dextran Sulphate Sodium-Induced Colitis in Mice". Molecules 25, № 10 (2020): 2406. http://dx.doi.org/10.3390/molecules25102406.

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Semi-synthetic triterpenoids, bearing cyano enone functionality in ring A, are considered to be novel promising therapeutic agents with complex inhibitory effects on tissue damage, inflammation and tumor growth. Previously, we showed that the cyano enone-containing 18βH-glycyrrhetinic acid derivative soloxolone methyl (SM) effectively suppressed the inflammatory response of macrophages in vitro and the development of influenza A-induced pneumonia and phlogogen-stimulated paw edema in vivo. In this work, we reported the synthesis of a novel 18βH-glycyrrhetinic acid derivative trioxolone methyl

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15

Savjani, Jignasa, Bhavesh Variya, Snehal Patel, et al. "Drug Design, Synthesis and Biological Evaluation of Heterocyclic Molecules as Anti-Inflammatory Agents." Molecules 27, no. 4 (2022): 1262. http://dx.doi.org/10.3390/molecules27041262.

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Non-steroidal anti-inflammatory drugs (NSAIDs) are generally utilized for numerous inflammatory ailments. The long-term utilization of NSAIDs prompts adverse reactions such as gastrointestinal ulceration, renal dysfunction and hepatotoxicity; however, selective COX-2 inhibitors prevent these adverse events. Various scientific approaches have been employed to identify safer COX-2 inhibitors, as in any case, a large portion of particular COX-2 inhibitors have been retracted from the market because of severe cardiovascular events. This study aimed to develop and synthesize a novel series of indom

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16

V S, Anila Kumari, Dr Prasobh G R, and Sheeja Rekha A G. "A Brief Review on Isoxazole Derivatives as Antibacterial Agents." International Journal of Research and Review 9, no. 9 (2022): 321–33. http://dx.doi.org/10.52403/ijrr.20220935.

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Isoxazole compounds exhibit a wide spectrum of targets and broad biological activities. Isoxazole derivatives are still popular scaffolds for the development of new agents with variable biological activities such as antimicrobial, antiviral, anticancer, anti-inflammatory, immunomodulatory, anticonvulsant or antidiabetic properties. The key feature of these heterocycles is that they possess the typical properties of an aromatic system but contain a weak nitrogen-oxygen bond which under certain reaction conditions like reducing or basic conditions is a potential site of ring cleavage. Thus, isox

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17

Zheng, Xian-Jing, Chun-Shi Li, Ming-Yue Cui, et al. "Synthesis, biological evaluation of benzothiazole derivatives bearing a 1,3,4-oxadiazole moiety as potential anti-oxidant and anti-inflammatory agents." Bioorganic & Medicinal Chemistry Letters 30, no. 13 (2020): 127237. http://dx.doi.org/10.1016/j.bmcl.2020.127237.

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18

Lopes, Juliana Romano, Freddy Humberto Marin-Dett, Rita Alexandra Machado Silva, et al. "Design and Synthesis of Boronic Chalcones with Dual Anticancer and Anti-Inflammatory Activity." Molecules 30, no. 14 (2025): 3032. https://doi.org/10.3390/molecules30143032.

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Head and neck cancer (HNC) is a highly aggressive malignancy with limited treatment options and poor prognosis. Inflammation plays a critical role in HNC progression, with elevated levels of pro-inflammatory cytokines such as TNF, IL-6, IL-8, and IL-1β contributing to tumor development. In this study, a novel series of boronic chalcones was designed and synthesized as potential dual-action anticancer and anti-inflammatory agents. The most potent compounds were evaluated for their cytotoxicity against Squamous Cell Carcinoma (SCC-25), and their selectivity index (SI) was determined. Compound 5

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19

Ma, Yulu, Xi Zheng, Ping Zhu, et al. "Novel Resveratrol-chalcone Derivatives: Synthesis and Biological Evaluation." Mini-Reviews in Medicinal Chemistry 19, no. 5 (2019): 424–36. http://dx.doi.org/10.2174/1389557518666180727165358.

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Introduction: Resveratrol and chalcones are lead compounds with good biological activities. </P><P> Method: In this study, a series of novel derivatives (6-38) between resveratrol and chalcone possessing piperazine moiety have been synthesized, and in vitro anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and anti-proliferative effect on a panel of human tumor cell lines (Hela, A549 and SGC7901) by MTT assay were evaluated. </P><P> Result: The results demonstrated that the substituents of the NH group of piperazine ring had an obvi

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20

Maniewska, Jadwiga, Benita Wiatrak, Żaneta Czyżnikowska, and Berenika M. Szczęśniak-Sięga. "Synthesis of New Tricyclic 1,2-Thiazine Derivatives with Anti-Inflammatory Activity." International Journal of Molecular Sciences 22, no. 15 (2021): 7818. http://dx.doi.org/10.3390/ijms22157818.

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New, tricyclic compounds containing a sulfonyl moiety in their structure, as potential safer COX inhibitors, were designed and synthesized. New derivatives have three conjugated rings and a sulfonyl group. A third ring, i.e., an oxazine, oxazepine or oxazocin, has been added to the 1,2-benzothiazine skeleton. Their anti-COX-1/COX-2 and cytotoxic effects in vitro on NHDF cells, together with the ability to interact with model membranes and the influence on reactive oxygen species and nitric oxide, were studied. Additionally, a molecular docking study was performed to understand the binding inte

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21

Kalaivanan.R , S. Senthilkumar , V. Sughanya. "Synthesis, Characterization and In-Vitroanti-Tumor Activity of Some Novel Pyrazole Derivatives." Tuijin Jishu/Journal of Propulsion Technology 44, no. 4 (2023): 2046–54. http://dx.doi.org/10.52783/tjjpt.v44.i4.1179.

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Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as a potent anti-inflammatory, antipsychotic , anti-obesity drug, an analgesic, and anti-depressant agents have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This heterocyclic c

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22

Occhiuzzi, Maria Antonietta, Giuseppina Ioele, Michele De Luca, et al. "Dissecting CYP1A2 Activation by Arylalkanoic Acid Prodrugs toward the Development of Anti-Inflammatory Agents." International Journal of Molecular Sciences 25, no. 1 (2023): 435. http://dx.doi.org/10.3390/ijms25010435.

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Arylalkane-derived prodrugs of arylacetic acids are a small group of substances that have long been known for their anti-inflammatory action. Despite their ease of synthesis and good potential for the development of new potent and safe anti-inflammatory agents, this group of substances has not received much attention from researchers so far. Therefore, representative arylalkane derivatives were investigated through molecular docking techniques to verify the possible hepatic activation mode toward active metabolites by CYP1A2. In this regard, arylalkanoic acid prodrugs were docked with a crysta

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NASSAR, Ekhlass. "Synthesis of Diarylpyrazoles Containing a Phenylsulphone or Carbonitrile Moiety and their Chalcones as Possible Anti-Inflammatory Agents." Scientia Pharmaceutica 79, no. 3 (2011): 507–24. http://dx.doi.org/10.3797/scipharm.1105-14.

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Abdel-Aziz, Hatem A., Khalid A. Al-Rashood, Kamal Eldin H. ElTahir, and Ghada M. Suddek. "Synthesis of N-benzenesulfonamide-1H-pyrazoles bearing arylsulfonyl moiety: Novel celecoxib analogs as potent anti-inflammatory agents." European Journal of Medicinal Chemistry 80 (June 2014): 416–22. http://dx.doi.org/10.1016/j.ejmech.2014.04.065.

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25

Irfan, Ali, Sajjad Ahmad, Saddam Hussain, et al. "Recent Updates on the Synthesis of Bioactive Quinoxaline-Containing Sulfonamides." Applied Sciences 11, no. 12 (2021): 5702. http://dx.doi.org/10.3390/app11125702.

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Quinoxaline is a privileged pharmacophore that has broad-spectrum applications in the fields of medicine, pharmacology and pharmaceutics. Similarly, the sulfonamide moiety is of considerable interest in medicinal chemistry, as it exhibits a wide range of pharmacological activities. Therefore, the therapeutic potential and biomedical applications of quinoxalines have been enhanced by incorporation of the sulfonamide group into their chemical framework. The present review surveyed the literature on the preparation, biological activities and structure-activity relationship (SAR) of quinoxaline su

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26

Hayun, H., R. N. Fauzan, N. T. Wibowo, A. Asrianingtiyas, N. Afriliana, and T. Ananda. "Synthesis and Anti-inflammatory Activity of 2-Methoxy-4-(1-phenyl-3- methyl-1H-pyrazol-5-yl)phenol) and Its Aminomethyl Derivatives." Asian Journal of Chemistry 32, no. 3 (2020): 607–11. http://dx.doi.org/10.14233/ajchem.2020.22159.

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Using heat-induced protein denaturation technique, a series of novel synthesized 1,5-diarylpyrazole compounds, namely 2-methoxy-4-(1-phenyl-3-methyl-1H-pyrazol-5-yl)phenol (1) and its aminomethyl derivatives (2a-e) were evaluated for their anti-inflammatory potentiality. The structures of the synthesized compounds were elucidated using FTIR, NMR (1H & 13C) and mass spectral data. The study found that the activity of aminomethyl derivatives (2a-e) was higher than that of parent compound 1. In this series, aminomethyl derivatives bearing dimethylamino-methyl, diethylaminomethyl and pyrrolidi

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27

Redda, Kinfe Ken, Madhavi Gangapuram, Absera W. Haile, and Suresh Eyunni. "Abstract 5742: Synthesis of substituted benzimidazole tetrahydropyridines as anti-breast cancer agents." Cancer Research 85, no. 8_Supplement_1 (2025): 5742. https://doi.org/10.1158/1538-7445.am2025-5742.

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Abstract Breast cancer is the most common type of cancer worldwide. In 2023, the World Health Organization (WHO) reported that 2.3 million women were diagnosed with breast cancer, leading to 670, 000 deaths. Furthermore, the incidence rates of breast cancer have been rising at 3% each year. Overexpression of COX-2 in breast cancer tissues is associated with poor prognosis, including higher tumor grade, increased metastatic potential, and resistance to therapy. Selective COX-2 inhibitors have demonstrated potential in reducing tumor growth in preclinical and some clinical studies. These inhibit

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Xia, Yan, Xiliang Zheng, Erkang Wang, Dongfeng Li, Ruibin Hou, and Jin Wang. "Synthesis of adenosine analogues with indole moiety as human adenosine A 3 receptor ligands." Royal Society Open Science 5, no. 2 (2018): 171596. http://dx.doi.org/10.1098/rsos.171596.

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Adenosine is an endogenous modulator exerting its functions through the activation of four adenosine receptor (AR) subtypes, termed A 1 , A 2A , A 2B and A 3 , which belong to the G-protein-coupled receptor superfamily. The human A 3 AR (hA 3 AR) subtype is implicated in several cytoprotective functions. Therefore, hA 3 AR modulators, and in particular agonists, are sought for their potential application as anti-inflammatory, anti-cancer and cardioprotective agents. Here, we prepared novel adenosine derivatives with indole moiety as hA 3 AR ligands. According to the biological assay, we found

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Bano, Sameena, Kalim Javed, Shamim Ahmad, I. G. Rathish, Surender Singh, and M. S. Alam. "Synthesis and biological evaluation of some new 2-pyrazolines bearing benzene sulfonamide moiety as potential anti-inflammatory and anti-cancer agents." European Journal of Medicinal Chemistry 46, no. 12 (2011): 5763–68. http://dx.doi.org/10.1016/j.ejmech.2011.08.015.

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Tageldin, Gina N., Salwa M. Fahmy, Hayam M. Ashour, Mounir A. Khalil, Rasha A. Nassra, and Ibrahim M. Labouta. "Design, synthesis and evaluation of some pyrazolo[3,4-d]pyrimidine derivatives bearing thiazolidinone moiety as anti-inflammatory agents." Bioorganic Chemistry 80 (October 2018): 164–73. http://dx.doi.org/10.1016/j.bioorg.2018.06.013.

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Hassan, Ghaneya Sayed, Sahar Mahmoud Abou-Seri, Gehan Kamel, and Mamdouh Moawad Ali. "Celecoxib analogs bearing benzofuran moiety as cyclooxygenase-2 inhibitors: Design, synthesis and evaluation as potential anti-inflammatory agents." European Journal of Medicinal Chemistry 76 (April 2014): 482–93. http://dx.doi.org/10.1016/j.ejmech.2014.02.033.

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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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Barbarossa, Alexia, Jessica Ceramella, Alessia Carocci, et al. "Benzothiazole-Phthalimide Hybrids as Anti-Breast Cancer and Antimicrobial Agents." Antibiotics 12, no. 12 (2023): 1651. http://dx.doi.org/10.3390/antibiotics12121651.

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The benzothiazole nucleus is a major heterocyclic scaffold whose therapeutic potential has been thoroughly explored due to its structural simplicity and ease of synthesis. In fact, several benzothiazole derivatives have been synthesized over time, demonstrating numerous pharmacological properties such as anticancer, antimicrobial, anti-inflammatory, and antioxidant activities. Herein, we propose a new series of benzothiazole-phthalimide hybrids obtained by linking the phthalimide moiety to differently substituted benzothiazole nuclei through the N atom. These compounds have been screened for t

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Atiya, Rana N., Zahraa L. Razzaq, Widad I. Yahya, and Helen M. Neamah. "Synthesis, Characterization and Studying Biological Activity of Heterocyclic Compounds." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 13, no. 01 (2023): 205–11. http://dx.doi.org/10.25258/ijddt.13.1.31.

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Heterocyclic moiety was mentioned to present diverse biological activities such as inhibitors of protein glycation, antibacterial, antifungal, anticancer, antidepressant, anti-inflammatory, antituberculosis, antioxidant, and as antiviral agents, in addition to other biological activities; therefore, many medicines containing heterocyclic moiety have been observed. Due to the pharmacological importance of heterocyclic derivatives, the present work comes as attempt to synthesis of heterocyclic compound involved (tetrazole and pyrazole rings) by series of steps starting from pyrimidin-2-amine, wh

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Barbari, Riccardo, Vera Bruggink, Robert Klaus Hofstetter, et al. "Synthesis and Biological Activity Assessment of 2-Styrylbenzothiazoles as Potential Multifunctional Therapeutic Agents." Antioxidants 13, no. 10 (2024): 1196. http://dx.doi.org/10.3390/antiox13101196.

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A current trend in healthcare research is to discover multifunctional compounds, able to interact with multiple biological targets, in order to simplify multi-drug therapies and improve patient compliance. The aim of this work was to outline the growing demand for innovative multifunctional compounds, achieved through the synthesis, characterisation and SAR evaluation of a series of 2-styrylbenzothiazole derivatives. The six synthesised compounds were studied for their potential as photoprotective, antioxidant, antiproliferative, and anti-inflammatory agents. In order to profile antioxidant ac

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36

Ameziane El Hassani, Issam, Khouloud Rouzi, Hamza Assila, Khalid Karrouchi, and M’hammed Ansar. "Recent Advances in the Synthesis of Pyrazole Derivatives: A Review." Reactions 4, no. 3 (2023): 478–504. http://dx.doi.org/10.3390/reactions4030029.

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Pyrazole, characterized by a five-membered heterocyclic structure featuring two neighboring nitrogen atoms, serves as a core element. Pyrazoles hold a privileged status as versatile frameworks in various sectors of the chemical industry, including medicine and agriculture. Previous reviews have extensively highlighted the significance of pyrazoles and their diverse biological activities, encompassing roles such as antituberculosis, antimicrobial, antifungal, anti-inflammatory, anticancer, and antidiabetic agents. Consequently, they have garnered substantial interest from researchers. The aim o

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Burmistrov, Vladimir, Christophe Morisseau, Denis A. Babkov, et al. "Anti-Inflammatory Activity of Soluble Epoxide Hydrolase Inhibitors Based on Selenoureas Bearing an Adamantane Moiety." International Journal of Molecular Sciences 23, no. 18 (2022): 10710. http://dx.doi.org/10.3390/ijms231810710.

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The inhibitory potency of the series of inhibitors of the soluble epoxide hydrolase (sEH) based on the selenourea moiety and containing adamantane and aromatic lipophilic groups ranges from 34.3 nM to 1.2 μM. The most active compound 5d possesses aliphatic spacers between the selenourea group and lipophilic fragments. Synthesized compounds were tested against the LPS-induced activation of primary murine macrophages. The most prominent anti-inflammatory activity, defined as a suppression of nitric oxide synthesis by LPS-stimulated macrophages, was demonstrated for compounds 4a and 5b. The cytot

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Sharma, Aastha, Aakash Deep, Minakshi Gupta Marwaha, and Rakesh Kumar Marwaha. "Quinoxaline: A Chemical Moiety with Spectrum of Interesting Biological Activities." Mini-Reviews in Medicinal Chemistry 22, no. 6 (2022): 927–48. http://dx.doi.org/10.2174/1389557521666210927123831.

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Abstract: Quinoxaline (C8H6N2), commonly called 1,4-diazanaphthalene, 1,4-benzodiazine, or benzopyrazine, is a very potent nitrogenous heterocyclic moiety consisting of a benzene ring fused with the pyrazine ring. A number of different methods for the synthesis of quinoxaline derivatives have been reported in the literature, but the most effective method, commonly used for the synthesis of quinoxaline analogues involves the condensation of substituted o-phenylenediamines with 1, 2- dicarbonyl compounds in the presence of different catalyst(s). The presence of different types of catalysts and t

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Mateev, Emilio, Maya Georgieva, and Alexander Zlatkov. "Pyrrole as an Important Scaffold of Anticancer Drugs: Recent Advances." Journal of Pharmacy & Pharmaceutical Sciences 25 (January 4, 2022): 24–40. http://dx.doi.org/10.18433/jpps32417.

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With the significant increase of patients suffering from different types of cancer, it is evident that prompt measures in the development of novel and effective agents need to be taken. Pyrrole moiety has been found in various active compounds with anti-inflammatory, antiseptic, antibacterial, lipid-lowering and anticancer properties. Recent advances in the exploration of highly active and selective cytotoxic structures containing pyrrole motifs have shown promising data for future investigations. Accordingly, this review presents an overview of recent developments in the pyrrole derivatives a

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Chłoń-Rzepa, Grażyna, Agnieszka W. Jankowska, Małgorzata Zygmunt, Krzysztof Pociecha, and Elżbieta Wyska. "Synthesis of 8-alkoxy-1,3-dimethyl-2, 6-dioxopurin-7-yl-substituted acetohydrazides and butanehydrazides as analgesic and anti-inflammatory agents." Heterocyclic Communications 21, no. 5 (2015): 273–78. http://dx.doi.org/10.1515/hc-2015-0100.

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AbstractA series of new 8-alkoxy-1,3-dimethyl-2,6-dioxopurin-7-yl-substituted acetohydrazides and butanehydrazides 6–12 was synthesized and evaluated for the analgesic activity in two in vivo models: the writhing syndrome and the hot-plate tests. Among the investigated derivatives, compounds with N′-arylidenehydrazide moiety 9–12 show analgesic activity significantly higher than that of acetylsalicylic acid, which may indicate the importance of this structural element for analgesic properties. The lack of the activity in the hot-plate test may suggest that the analgesic activity of the newly s

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Tilvi, Supriya, Safia Khan та Mahesh S. Majik. "γ-Hydroxybutenolide Containing Marine Natural Products and Their Synthesis: A Review". Current Organic Chemistry 23, № 22 (2020): 2436–68. http://dx.doi.org/10.2174/1385272823666191021122810.

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: γ-Hydroxybutenolides (γ-HB) is an important structural core found in many bioactive marine natural products (MNPS). The γ-HB core containing NPS served as an inspiration to medicinal chemists to undertake designing of the new synthetic strategies to construct γ-HB core. Subsequently, it further results in the development of novel physiological and therapeutic agents. The most notable example includes manoalides, cacospongionolides, petrosaspongioide M and dysidiolide from marine sponges possessing anti-inflammatory properties. γ-HB containing MNPS were known to possess various pharmacologica

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Singh, Shiv Dev, Arvind Kumar, Firoz Babar, Neetu Sachan, and Arun Kumar Sharma. "Synthesis of Novel 3(N,N-dialkylamino)alkyl/phenyl Substituted Thieno [2,3-d]pyrimidinones as H1-Anti-Histaminic and Antimicrobial Agents." Current Bioactive Compounds 15, no. 1 (2019): 63–70. http://dx.doi.org/10.2174/1573407214666180226130957.

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Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial acti

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Surowiak, Alicja K., Lucyna Balcerzak, Stanisław Lochyński, and Daniel J. Strub. "Biological Activity of Selected Natural and Synthetic Terpenoid Lactones." International Journal of Molecular Sciences 22, no. 9 (2021): 5036. http://dx.doi.org/10.3390/ijms22095036.

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Terpenoids with lactone moieties have been indicated to possess high bioactivity. Certain terpenoid lactones exist in nature, in plants and animals, but they can also be obtained by chemical synthesis. Terpenoids possessing lactone moieties are known for their cytotoxic, anti-inflammatory, antimicrobial, anticancer, and antimalarial activities. Moreover, one terpenoid lactone, artemisinin, is used as a drug against malaria. Because of these abilities, there is constant interest in new terpenoid lactones that are both isolated and synthesized, and their biological activities have been verified.

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He, Meng, Mingjun Yu, Chao Li, et al. "Design, Synthesis and Bioactivity Evaluation of Novel Chalcone Derivatives Possessing Tryptophan Moiety with Dual Activities of Anti-cancer and Partially Restoring the Proliferation of Normal Kidney Cells Pre-treated with Cisplatin." Anti-Cancer Agents in Medicinal Chemistry 22, no. 10 (2022): 1945–61. http://dx.doi.org/10.2174/1871520621666211021134626.

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Background: Chalcone is a broad-spectrum natural product with anti-cancer and anti-inflammatory activities. However, low potency, low selectivity, and serious side effects limit its druggability. L-Tryptophan is an essential precursor molecule of an anti-cancer active substance. Also, the indole moiety inhibits the proliferation of tumor cells by binding to colchicine sites. A decrease in kidney cell activity caused by kidney inflammation is the primary side effect of cancer therapy. Objective: The purpose of this work was to design, synthesize, and perform bioactivity evaluation of novel chal

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Muscará, Marcelo N., and John L. Wallace. "V. Therapeutic potential of nitric oxide donors and inhibitors." American Journal of Physiology-Gastrointestinal and Liver Physiology 276, no. 6 (1999): G1313—G1316. http://dx.doi.org/10.1152/ajpgi.1999.276.6.g1313.

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Nitric oxide is a crucial mediator of gastrointestinal mucosal defense, but, paradoxically, it also contributes to mucosal injury in several situations. Inhibitors of nitric oxide synthesis and compounds that release nitric oxide have been useful pharmacological tools for evaluating the role of nitric oxide in gastrointestinal physiology and pathophysiology. Newer inhibitors with selectivity for one of the isoforms of nitric oxide synthase are even more powerful tools and may have utility as therapeutic agents. Also, agents that can scavenge nitric oxide or peroxynitrite are promising as drugs

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Babu, Aravinda, Kenchaiah Sunil, Ayyiliath Meleveetil Sajith, et al. "NMI-SO2Cl2-Mediated Amide Bond Formation: Facile Synthesis of Some Dihydrotriazolopyrimidine Amide Derivatives as Potential Anti-Inflammatory and Anti-Tubercular Agents." Pharmaceuticals 17, no. 5 (2024): 548. http://dx.doi.org/10.3390/ph17050548.

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Facile access to some novel biologically relevant dihydrotriazolopyrimidine carboxylic acid-derived amide analogues using NMI/SO2Cl2, and aromatic and aliphatic primary and secondary amines, is reported herein. The role of N-methylimidazole (NMI) as the base and sulfuryl chloride (SO2Cl2) as the coupling reagent has been effectively realized in accessing these molecules in good to excellent yields. The feasibility of the developed protocol has also been extended to the gram-scale synthesis of N-benzylbenzamide in a 75% yield from benzoic acid and benzyl amine. The newly synthesized compounds w

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ul-Malik, Mokhtar A. Abd, Aly Abdou, Mohamed R. Fouad, Ahmed S. N. Alkamali, and Shaban A. A. Abdel-Raheem. "Synthesis, spectral characterization and molecular docking studies of some thiocarbohydrazide-based Schiff bases with pyrazole moiety as potential anti-inflammatory agents." Current Chemistry Letters 13, no. 4 (2024): 683–94. http://dx.doi.org/10.5267/j.ccl.2024.5.002.

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A new series of Schiff bases derived from pyrazole-thiocarbohydrazide, namely (4a-d), were well-synthesized. The synthesis is carried out using monothiocarbohydrazone derivative (3), which was prepared via coupling of 5-chloro-pyrazole-4-carbaldehyde (1) with thiocarbohydrazide (2) in absolute ethanol that contains a catalytic quantity of acetic acid. The structures of newly synthesized compounds were fully clarified by various spectroscopic analyses (FT-IR, 1H-NMR, 13C-NMR, and mass spectra) and elemental analysis. Also, the molecular docking was performed to investigate the binding interacti

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Dinesha, Shivapura Viveka, Prasanna S. Khandige, and Gundibasappa K. Nagaraja. "Molecular properties prediction and synthesis of new oxadiazole derivatives possessing 3-fluoro-4-methoxyphenyl moiety as potent anti-inflammatory and analgesic agents." Monatshefte für Chemie - Chemical Monthly 147, no. 2 (2015): 435–43. http://dx.doi.org/10.1007/s00706-015-1528-2.

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Liu, Wukun, Jinpei Zhou, Tong Zhang, et al. "Design and synthesis of thiourea derivatives containing a benzo[5,6]cyclohepta[1,2-b]pyridine moiety as potential antitumor and anti-inflammatory agents." Bioorganic & Medicinal Chemistry Letters 22, no. 8 (2012): 2701–4. http://dx.doi.org/10.1016/j.bmcl.2012.03.002.

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Brunetti, Leonardo, Fabio Francavilla, Mauro Niso, et al. "Hydrogen Sulfide (H2S)-Donating Formyl Peptide Receptor 2 (FPR2) Agonists: Design, Synthesis, and Biological Evaluation in Primary Mouse Microglia Culture." Antioxidants 14, no. 7 (2025): 827. https://doi.org/10.3390/antiox14070827.

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Chronic neuroinflammation and oxidative stress play an important role in the onset and progression of neurodegenerative disorders, including Alzheimer’s disease, which can ultimately lead to neuronal damage and loss. The mechanisms of sustained neuroinflammation and the coordinated chain of events that initiate, modulate, and then lead to the resolution of inflammation are increasingly being elucidated, offering alternative approaches for treating pathologies with underlying chronic neuroinflammation. Here, we propose a new multitarget approach to address chronic neuroinflammation and oxidativ

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