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Journal articles on the topic 'Privileged scaffold'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

Shinde, Rani A., Vasanti M. Suvarna, and Arundhati N. Abhyankar. "AN INSIGHT INTO PRIVILEGED SCAFFOLDS IN TUBERCULOSIS: DEVELOPMENTAL ASPECTS AND IMPLICATIONS IN DRUG DESIGN." Indian Drugs 59, no. 01 (2022): 7–22. http://dx.doi.org/10.53879/id.59.01.13140.

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Tuberculosis remains a major threat to mankind, becoming more deadly due to COVID-19 pandemic. The worldwide scenario is daunted by additional factors such as drug resistance, non-adherence and complexity of the treatment. To overcome these obstacles, there is a constant need for novel drug development. However, drug development is an extensive process in itself requiring enormous financial investment and is time-consuming with a low success rate. A viable alternative to circumvent these complications is to explore ‘privileged scaffold/s’. Further logical approaches would be to study the privi

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2

Tomassoli, Isabelle, and Daniela Gündisch. "Bispidine as a Privileged Scaffold." Current Topics in Medicinal Chemistry 16, no. 11 (2016): 1314–42. http://dx.doi.org/10.2174/1568026615666150915111434.

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3

N, Ramalakshmi, Amuthalakshmi S, Yamuna R, A. Smith Anton, and Arunkumar S. "Indolizine- A Privileged Biological Scaffold." Der Pharma Chemica 13, no. 2 (2021): 10. https://doi.org/10.5281/zenodo.14718468.

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Indolizine derivatives own cherished biological activities and have been studied for their hypoglycemic, antimicrobial, anti-inflammatory& analgesic, anti-tumour activities. Indolizine scaffold has fascinated speculation and continuing interest and has become an important parent system for the development of potent new drug candidates. The conjugated planar electronic structure exhibits strong fluorescence properties which serve as a valuable tool for DNA interaction and spectroscopic sensitizer studies. Thus, the chemistry, synthesis and properties of this merged system and its derivative

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4

Cesarini, Silvia, Ilaria Vicenti, Federica Poggialini, et al. "Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy." Molecules 29, no. 7 (2024): 1452. http://dx.doi.org/10.3390/molecules29071452.

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The use of privileged scaffolds as a starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development. Scaffold decoration, morphing and hopping are additional techniques that enable the modification of the chosen privileged framework and better explore the chemical space around it. In this study, two series of highly functionalized pyrimidine and pyridine derivatives were synthesized using a scaffold morphing approach consisting of triazine compounds obtained previously as antiviral agents. Newly synthesized azines were evalua

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5

Chaudhary, Ashu, and Anshul Singh. "NANOPARTICLES: PRIVILEGED SCAFFOLD FOR CANCER TREATMENT." International Journal of Advanced Research 4, no. 10 (2016): 1–10. http://dx.doi.org/10.21474/ijar01/2047.

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6

Saha, Debasmita, Garima Jain, and Anuj Sharma. "Benzothiazepines: chemistry of a privileged scaffold." RSC Advances 5, no. 86 (2015): 70619–39. http://dx.doi.org/10.1039/c5ra12422k.

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Benzothiazepines being an integral part of the major cardiovascular drugs in market ascertain their biological importance. This review presents a comprehensive vision of the various synthetic tactics adopted till now to afford these frameworks.

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7

Rakesh, K. P., C. S. Shantharam, M. B. Sridhara, H. M. Manukumar, and Hua-Li Qin. "Benzisoxazole: a privileged scaffold for medicinal chemistry." MedChemComm 8, no. 11 (2017): 2023–39. http://dx.doi.org/10.1039/c7md00449d.

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8

Roelfes, Gerard. "LmrR: A Privileged Scaffold for Artificial Metalloenzymes." Accounts of Chemical Research 52, no. 3 (2019): 545–56. http://dx.doi.org/10.1021/acs.accounts.9b00004.

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9

Chao, Bo, Bingbing X. Li, and Xiangshu Xiao. "The chemistry and pharmacology of privileged pyrroloquinazolines." MedChemComm 6, no. 4 (2015): 510–20. http://dx.doi.org/10.1039/c4md00485j.

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10

Xiong, Donglu, Wenxi Zhou, Zhiwu Lu, Suping Zeng, and Jun (Joelle) Wang. "A highly enantioselective access to chiral chromanones and thiochromanones via copper-catalyzed asymmetric conjugated reduction of chromones and thiochromones." Chemical Communications 53, no. 51 (2017): 6844–47. http://dx.doi.org/10.1039/c7cc03939e.

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11

Pedroso de Lima, Fábio, Marta Costa, Ana Sousa, and Maria Fernanda Proença. "The Chromenopyridine Scaffold: A Privileged Platform in Drug Design." Molecules 29, no. 13 (2024): 3004. http://dx.doi.org/10.3390/molecules29133004.

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The chromenopyridine scaffold represents an important class of heterocyclic compounds exhibiting a broad spectrum of biological properties. This review describes novel and efficient procedures for the synthesis of this scaffold. Herein, several methods were detailed and grouped according to their starting material (e.g., salicylaldehydes, chromones, chromanones and coumarins) and respective biological activity, when reported. This review highlights the potential of the reported synthetic strategies for preparing chromenopyridine derivatives with promising biological activity, paving the way fo

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12

Tomasic, T., and L. Masic. "Rhodanine as a Privileged Scaffold in Drug Discovery." Current Medicinal Chemistry 16, no. 13 (2009): 1596–629. http://dx.doi.org/10.2174/092986709788186200.

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13

Malki, Yohan, Jean Martinez, and Nicolas Masurier. "1,3‐Diazepine: A privileged scaffold in medicinal chemistry." Medicinal Research Reviews 41, no. 4 (2021): 2247–315. http://dx.doi.org/10.1002/med.21795.

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14

Xia, Li-Wen, Meng-Yu Ba, Wei Liu, et al. "Triazol: a privileged scaffold for proteolysis targeting chimeras." Future Medicinal Chemistry 11, no. 22 (2019): 2919–73. http://dx.doi.org/10.4155/fmc-2019-0159.

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Current traditional drugs such as enzyme inhibitors and receptor agonists/antagonists present inherent limitations due to occupancy-driven pharmacology as the mode of action. Proteolysis targeting chimeras (PROTACs) are composed of an E3 ligand, a connecting linker and a target protein ligand, and are an attractive approach to specifically knockdown-targeted proteins utilizing an event-driven mode of action. The length, hydrophilicity and rigidity of connecting linkers play important role in creating a successful PROTAC. Some PROTACs with a triazole linker have displayed promising anticancer a

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15

Farmer, Luke A., Evan A. Haidasz, Markus Griesser, and Derek A. Pratt. "Phenoxazine: A Privileged Scaffold for Radical-Trapping Antioxidants." Journal of Organic Chemistry 82, no. 19 (2017): 10523–36. http://dx.doi.org/10.1021/acs.joc.7b02025.

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16

Saha, Debasmita, Garima Jain, and Anuj Sharma. "ChemInform Abstract: Benzothiazepines: Chemistry of a Privileged Scaffold." ChemInform 46, no. 43 (2015): no. http://dx.doi.org/10.1002/chin.201543233.

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17

Zhu, Rongfeng, Guangqian Jiang, Wanyu Tang, et al. "Aporphines: A privileged scaffold in CNS drug discovery." European Journal of Medicinal Chemistry 256 (August 2023): 115414. http://dx.doi.org/10.1016/j.ejmech.2023.115414.

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18

Niwetmarin, Worawat, Hugo Rego Campello, Hazel A. Sparkes, Varinder K. Aggarwal, and Timothy Gallagher. "(−)-Cytisine: Access to a stereochemically defined and functionally flexible piperidine scaffold." Organic & Biomolecular Chemistry 16, no. 32 (2018): 5823–32. http://dx.doi.org/10.1039/c8ob01456f.

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19

Chapman, Michael R., Maria H. T. Kwan, Georgina E. King, et al. "Rapid, metal-free and aqueous synthesis of imidazo[1,2-a]pyridine under ambient conditions." Green Chemistry 18, no. 17 (2016): 4623–27. http://dx.doi.org/10.1039/c6gc01601d.

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20

Wang, Feng, Yongfang Yao, Hai-liang Zhu, and Yinghui Zhang. "Nitrogen-containing Heterocycle: A Privileged Scaffold for Marketed Drugs." Current Topics in Medicinal Chemistry 21, no. 6 (2021): 439–41. http://dx.doi.org/10.2174/156802662106210304105631.

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21

Zhan, Peng, Dongyue Li, Junyi Li, Xuwang Chen, and Xinyong Liu. "Benzimidazole Heterocycle as a Privileged Scaffold in Antiviral Agents." Mini-Reviews in Organic Chemistry 9, no. 4 (2012): 397–410. http://dx.doi.org/10.2174/157019312804699456.

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22

Weekes, A., and A. Westwell. "2-Arylbenzothiazole as a Privileged Scaffold in Drug Discovery." Current Medicinal Chemistry 16, no. 19 (2009): 2430–40. http://dx.doi.org/10.2174/092986709788682137.

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23

R. Solomon, V., and H. Lee. "Quinoline as a Privileged Scaffold in Cancer Drug Discovery." Current Medicinal Chemistry 18, no. 10 (2011): 1488–508. http://dx.doi.org/10.2174/092986711795328382.

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24

Berthet, Mathéo, Thomas Cheviet, Gilles Dujardin, Isabelle Parrot, and Jean Martinez. "Isoxazolidine: A Privileged Scaffold for Organic and Medicinal Chemistry." Chemical Reviews 116, no. 24 (2016): 15235–83. http://dx.doi.org/10.1021/acs.chemrev.6b00543.

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25

Grover, Jagdeep, and Sanjay M. Jachak. "Coumarins as privileged scaffold for anti-inflammatory drug development." RSC Advances 5, no. 49 (2015): 38892–905. http://dx.doi.org/10.1039/c5ra05643h.

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26

Blanco-Ania, Daniel, René W. M. Aben, Leon W. A. van Berkom, Hans W. Scheeren, and Floris P. J. T. Rutjes. "High-Pressure-Mediated Extension of the Privileged Steroid Scaffold." European Journal of Organic Chemistry 2014, no. 7 (2013): 1438–44. http://dx.doi.org/10.1002/ejoc.201301511.

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27

Barresi, Elisabetta, Marco Robello, Emma Baglini, et al. "Indol-3-ylglyoxylamide as Privileged Scaffold in Medicinal Chemistry." Pharmaceuticals 16, no. 7 (2023): 997. http://dx.doi.org/10.3390/ph16070997.

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In recent years, indolylglyoxylamide-based derivatives have received much attention due to their application in drug design and discovery, leading to the development of a wide array of compounds that have shown a variety of pharmacological activities. Combining the indole nucleus, already validated as a “privileged structure,” with the glyoxylamide function allowed for an excellent template to be obtained that is suitable to a great number of structural modifications aimed at permitting interaction with specific molecular targets and producing desirable therapeutic effects. The present review

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28

Mathur, Ritu, Khushal Singh Negi, Rahul Shrivastava, and Rashmy Nair. "Recent developments in the nanomaterial-catalyzed green synthesis of structurally diverse 1,4-dihydropyridines." RSC Advances 11, no. 3 (2021): 1376–93. http://dx.doi.org/10.1039/d0ra07807g.

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Single pot multicomponent approaches using different nanomaterials as green catalysts for synthesis of 1,4-dihydropyridine (1,4-DHP), a privileged heterocyclic scaffold with vital biological and therapeutic applications are reviewed.

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29

Baillache, Daniel J., and Asier Unciti-Broceta. "Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold." RSC Medicinal Chemistry 11, no. 10 (2020): 1112–35. http://dx.doi.org/10.1039/d0md00227e.

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Pyrazolo[3,4-d]pyrimidines have become of significant interest for the medicinal chemistry community as a privileged scaffold for the development of kinase inhibitors to treat a range of diseases, including cancer.

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30

Yoon, Jeong A., and Young Taek Han. "Efficient Synthesis of Pyrido[3,2-c]coumarins via Silver Nitrate Catalyzed Cycloisomerization and Application to the First Synthesis of Polyneomarline C." Synthesis 51, no. 24 (2019): 4611–18. http://dx.doi.org/10.1055/s-0037-1610730.

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Herein, we report an efficient method for the synthesis of the pyrido[3,2-c]coumarin scaffold, one of the privileged heterocycle-fused coumarin scaffolds, via a AgNO3-catalyzed cycloisomerization of 4-(propynylamino)coumarins obtained from diverse 4-hydroxycoumarins. This concise method affords pyrido[3,2-c]coumarin analogues bearing diverse substituents on the benzene or pyridine ring in moderate to good yields. Moreover, this methodology was extended to the facile synthesis of polyneomarline C, a natural pyrido[3,2-c]coumarin derivative isolated from the Chinese herbal medicine Polyalthia ne

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31

Vinogradova, Lyubov, Kristina Komarova, Alexey Lukin, et al. "You Win Some, You Lose Some: Modifying the Molecular Periphery of Nitrofuran-Tagged Diazaspirooctane Reshapes Its Antibacterial Activity Profile." International Journal of Molecular Sciences 26, no. 1 (2024): 207. https://doi.org/10.3390/ijms26010207.

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The use of the concept of privileged structures significantly accelerates the search for new leads and their optimization. 6-(methylsulfonyl)-8-(4-methyl-4H-1,2,4-triazol-3-yl)-2-(5-nitro-2-furoyl)-2,6-diazaspiro[3.4]octane 1 has been identified as a lead, with MICs of 0.0124–0.0441 μg/mL against MTb multiresistant strains. Several series of structural analogues have been synthesized, including variations in the periphery and simplifications of their scaffolds. All synthesized compounds were tested against the MTb H37Rv strain and ESKAPE panel of pathogens using serial broth dilutions. However

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32

Paz, Bruno Matos, Yang Li, Mathias Kirk Thøgersen, and Karl Anker Jørgensen. "Enantioselective synthesis of cyclopenta[b]benzofurans via an organocatalytic intramolecular double cyclization." Chemical Science 8, no. 12 (2017): 8086–93. http://dx.doi.org/10.1039/c7sc03006a.

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An enantioselective organocatalytic strategy, combining Brønsted base and N-heterocyclic carbene catalysis in a unique manner, is demonstrated for a concise construction of the privileged cyclopenta[b]benzofuran scaffold, present in many bioactive compounds having both academic and commercial interests.

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33

Duan, Yongtao, and Hai-liang Zhu. "Privileged Scaffold for Drug Design and Activity Improvement - Part V." Current Topics in Medicinal Chemistry 22, no. 7 (2022): 549. http://dx.doi.org/10.2174/156802662207220503005804.

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34

Wang, Yingge, Yongfang Yao, Hai-Liang Zhu, and Yongtao Duan. "Butterfly Structure: A Privileged Scaffold Targeting Tubulin-Colchicine Binding Site." Current Topics in Medicinal Chemistry 20, no. 17 (2020): 1505–8. http://dx.doi.org/10.2174/1568026620999200616132924.

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: Butterfly-shaped structure, as a novel scaffold with an attractive and certain shape, has been widely used in new drug discovery. Tubulin, composing of α- and β-tubulin heterodimers, plays a key role in mitosis and cell division which are regarded as an excellent target for cancer therapy. Currently, a series of butterfly shape diaryl heterocyclic compounds have been reported with strong potential against the tubulin-colchicine binding site. It is with one ring buried in the β subunit, another ring interacts with the α subunit and the main body is located in the flat pocket. Here, we firstly

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35

Duan, Yongtao, and Hai-liang Zhu. "Privileged Scaffold for Drug Design and Activity Improvement - Part III." Current Topics in Medicinal Chemistry 21, no. 28 (2021): 2513. http://dx.doi.org/10.2174/156802662128211125124443.

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36

Han, Xu, Yun Long Yu, Yang Sheng Hu, and Xin Hua Liu. "1,3,4-thiadiazole: A Privileged Scaffold for Drug Design and Development." Current Topics in Medicinal Chemistry 21, no. 28 (2021): 2546–73. http://dx.doi.org/10.2174/1568026621666211111154342.

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1,3,4-thiadiazole is a five-membered aromatic heterocycle containing two nitrogen atoms and one sulfur atom. As a privileged scaffold, it has its unique chemical properties and biological characteristics. In the design of drugs, they are widely and flexibly applied by medicinal chemists, and many candidates with therapeutic prospects have been developed. In this review, we focus on 1,3,4-thiadiazole derivatives and their various biological activities reported in the past five years (from 2015 to early 2020), such as anticancer, antibacterial, antifungal, anti-tuberculosis, antiinflammatory, an

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37

Gharat, Ruchita, Arati Prabhu, and Mihir P. Khambete. "Potential of triazines in Alzheimer's disease: A versatile privileged scaffold." Archiv der Pharmazie 355, no. 4 (2022): 2100388. http://dx.doi.org/10.1002/ardp.202100388.

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38

Duan, Yongtao, and Hai-liang Zhu. "Privileged Scaffold for Drug Design and Activity Improvement - Part IV." Current Topics in Medicinal Chemistry 22, no. 4 (2022): 268. http://dx.doi.org/10.2174/156802662204220210163610.

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39

Polanski, J., A. Kurczyk, A. Bak, and R. Musiol. "Privileged Structures - Dream or Reality: Preferential Organization of Azanaphthalene Scaffold." Current Medicinal Chemistry 19, no. 13 (2012): 1921–45. http://dx.doi.org/10.2174/092986712800167356.

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40

Secci, Daniela, Erica Sanna, Simona Distinto, et al. "Privileged Scaffold Hybridization in the Design of Carbonic Anhydrase Inhibitors." Molecules 29, no. 18 (2024): 4444. http://dx.doi.org/10.3390/molecules29184444.

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Human Carbonic Anhydrases (hCA) are enzymes that contribute to cancer’s development and progression. Isoforms IX and XII have been identified as potential anticancer targets, and, more specifically, hCA IX is overexpressed in hypoxic tumor cells, where it plays an important role in reprogramming the metabolism. With the aim to find new inhibitors towards IX and XII isoforms, the hybridization of the privileged scaffolds isatin, dihydrothiazole, and benzenesulfonamide was investigated in order to explore how it may affect the activity and selectivity of the hCA isoforms. In this respect, a seri

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41

Silva, Carlos F. M., Vasco F. Batista, Diana C. G. A. Pinto, and Artur M. S. Silva. "Challenges with chromone as a privileged scaffold in drug discovery." Expert Opinion on Drug Discovery 13, no. 9 (2018): 795–98. http://dx.doi.org/10.1080/17460441.2018.1494720.

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42

Reis, Joana, Alexandra Gaspar, Nuno Milhazes, and Fernanda Borges. "Chromone as a Privileged Scaffold in Drug Discovery: Recent Advances." Journal of Medicinal Chemistry 60, no. 19 (2017): 7941–57. http://dx.doi.org/10.1021/acs.jmedchem.6b01720.

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43

Chen, Tao, Hao Xiong, Jing-Fang Yang, Xiao-Lei Zhu, Ren-Yu Qu, and Guang-Fu Yang. "Diaryl Ether: A Privileged Scaffold for Drug and Agrochemical Discovery." Journal of Agricultural and Food Chemistry 68, no. 37 (2020): 9839–77. http://dx.doi.org/10.1021/acs.jafc.0c03369.

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44

Benito Scarim, Cauê, and Chung Man Chin. "Nitroheterocyclic derivatives: privileged scaffold for drug development against Chagas disease." Medicinal Chemistry Research 28, no. 12 (2019): 2099–108. http://dx.doi.org/10.1007/s00044-019-02453-y.

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45

Noreen, Tayyaba, Muhammad Taha, Syahrul Imran, et al. "Synthesis of alpha amylase inhibitors based on privileged indole scaffold." Bioorganic Chemistry 72 (June 2017): 248–55. http://dx.doi.org/10.1016/j.bioorg.2017.04.010.

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46

Boniface, Pone K., and Ferreira I. Elizabeth. "Flavones as a Privileged Scaffold in Drug Discovery: Current Developments." Current Organic Synthesis 16, no. 7 (2019): 968–1001. http://dx.doi.org/10.2174/1570179416666190719125730.

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Background: Flavones are one of the main subclasses of flavonoids with diverse pharmacological properties. They have been reported to possess antimalarial, antimicrobial, anti-tuberculosis, anti-allergic, antioxidant, anti-inflammatory activities, among others. Objective: The present review summarizes the recent information on the pharmacological properties of naturally occurring and synthetic flavones. Method: Scientific publications referring to natural and synthetic flavones in relation to their biological activities were hand-searched in databases such as SciFinder, PubMed (National Librar

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47

Xiao, You‐Cai, and Fen‐Er Chen. "Chloramphenicol Base: A New Privileged Chiral Scaffold in Asymmetric Catalysis." ChemCatChem 11, no. 8 (2019): 2043–53. http://dx.doi.org/10.1002/cctc.201900150.

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48

Keri, Rangappa S., Srinivasa Budagumpi, Ranjith Krishna Pai, and R. Geetha Balakrishna. "Chromones as a privileged scaffold in drug discovery: A review." European Journal of Medicinal Chemistry 78 (May 2014): 340–74. http://dx.doi.org/10.1016/j.ejmech.2014.03.047.

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49

Zhu, Wei, Bao Wang, Shengbin Zhou, and Hong Liu. "The facile construction of the phthalazin-1(2H)-one scaffold via copper-mediated C–H(sp2)/C–H(sp) coupling under mild conditions." Beilstein Journal of Organic Chemistry 11 (September 14, 2015): 1624–31. http://dx.doi.org/10.3762/bjoc.11.177.

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A novel strategy for the construction of the phthalazin-1(2H)-one scaffold has been developed by means of a copper-mediated cascade C–H/C–H coupling and intramolecular annulations and a subsequent facile hydrazinolysis. This C–H activation transformation proceeds smoothly with wide generality, good functional tolerance and high stereo- and regioselectivity under mild conditions. Through the removal of the directing group, the resulting moiety could easily be transformed into the phthalazin-1(2H)-one scaffold, which is known to be a privileged moiety and a bioactive nucleus in pharmaceuticals.

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50

Pasricha, Sharda, and Pragya Gahlot. "Synthetic Strategies and Biological Potential of Coumarin-Chalcone Hybrids: A New Dimension to Drug Design." Current Organic Chemistry 24, no. 4 (2020): 402–38. http://dx.doi.org/10.2174/1385272824666200219091830.

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Privileged scaffolds are ubiquitous as effective templates in drug discovery regime. Natural and synthetically derived hybrid molecules are one such attractive scaffold for therapeutic agent development due to their dual or multiple modes of action, minimum or no side effects, favourable pharmacokinetics and other advantages. Coumarins and chalcone are two important classes of natural products affording diverse pharmacological activities which make them ideal templates for building coumarin-chalcone hybrids as effective biological scaffold for drug discovery research. Provoked by the promising

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