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Journal articles on the topic 'Triazolopyridine derivatives'

Author: Grafiati

Published: 5 June 2025

Last updated: 2 August 2025

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1

Flefel, Eman M., Walaa I. El-Sofany, Mahmoud El-Shahat, Arshi Naqvi, and Eman Assirey. "Synthesis, Molecular Docking and in Vitro Screening of Some Newly Synthesized Triazolopyridine, Pyridotriazine and Pyridine–Pyrazole Hybrid Derivatives." Molecules 23, no. 10 (2018): 2548. http://dx.doi.org/10.3390/molecules23102548.

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A series of novel pyridine and fused pyridine derivatives have been prepared starting from 6-(3,4-dimethylphenyl)-2-hydrazinyl-4-(thiophen-2-yl)-pyridine-3-carbonitrile 1 which on treatment with appropriate formic acid, acetic acid/ acetic anhydride, benzoyl chloride and/or carbon disulfide afforded the corresponding triazolopyridine derivatives 2–5. Also, treatment of hydrazide 1 with diethyloxalate, chloroacetyl chloride, chloroacetic acid and/or 1,2-dichloroethane yielded the corresponding pyridotriazine derivatives 7–10. Further transformation of compound 1 with a different active methylen

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2

Ryu, Hwani, Ky-Youb Nam, Hyo Jeong Kim, et al. "Discovery of a Novel Triazolopyridine Derivative as a Tankyrase Inhibitor." International Journal of Molecular Sciences 22, no. 14 (2021): 7330. http://dx.doi.org/10.3390/ijms22147330.

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More than 80% of colorectal cancer patients have adenomatous polyposis coli (APC) mutations, which induce abnormal WNT/β-catenin activation. Tankyrase (TNKS) mediates the release of active β-catenin, which occurs regardless of the ligand that translocates into the nucleus by AXIN degradation via the ubiquitin-proteasome pathway. Therefore, TNKS inhibition has emerged as an attractive strategy for cancer therapy. In this study, we identified pyridine derivatives by evaluating in vitro TNKS enzyme activity and investigated N-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-1-(2-cyanophenyl)piperidine-4-carb

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3

Shashi Nayana, M. Ravi, Y. Nataraja Sekhar, N. Siva Kumari, S. K. Mahmood, and Muttineni Ravikumar. "CoMFA and docking studies on triazolopyridine oxazole derivatives as p38 MAP kinase inhibitors." European Journal of Medicinal Chemistry 43, no. 6 (2008): 1261–69. http://dx.doi.org/10.1016/j.ejmech.2007.07.010.

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4

Liu, Jing-Ying, Hong-En Zhang, Cheng Wang, et al. "Design, synthesis, and antitumor evaluation of triazolopyridine derivatives as novel inhibitors for BRD4." European Journal of Medicinal Chemistry 285 (March 2025): 117272. https://doi.org/10.1016/j.ejmech.2025.117272.

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5

Juan, S. Gómez-Jeria, and J. Valenzuela-Hueichaqueo Nahuel. "The relationships between electronic structure and human A1 adenosine receptor binding affinity in a series of triazolopyridine derivatives." Chemistry Research Journal 5, no. 4 (2020): 226–36. https://doi.org/10.5281/zenodo.13142828.

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<strong>Abstract </strong>Some triazolopyridine derivatives present a good binding affinity for the human adenosine A<sub>1</sub> receptor. In this paper we present the results of the examination of the relationships between the electronic structure of these molecules and the A<sub>1</sub> receptor binding affinity. The Klopman-Peradejordi-Gómez method was employed. A statistically significant equation, involving four local atomic reactivity indices, was obtained. Starting from the QSAR results we built the 2D-pharemacophore including the suggested interactions with the binding site. On

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6

Bandaru, N. V. M. Rao, Ashna Fathima, Vandana Joshi, et al. "Design, synthesis, and biological evaluation of substituted benzyl-triazolopyridine derivatives as non-hydroxamate based HDAC8 inhibitors." European Journal of Medicinal Chemistry Reports 13 (April 2025): 100255. https://doi.org/10.1016/j.ejmcr.2025.100255.

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7

Guba, Wolfgang, Matthias Nettekoven, Bernd Püllmann, Claus Riemer, and Sébastien Schmitt. "Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities?" Bioorganic & Medicinal Chemistry Letters 14, no. 12 (2004): 3307–12. http://dx.doi.org/10.1016/j.bmcl.2004.03.104.

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8

Sachdeva, Tanisha, May Lee Low, Chun‐Wai Mai, Siew Lee Cheong, Yun Khoon Liew, and Marilyn Daisy Milton. "Design, Synthesis and Characterisation of Novel Phenothiazine‐Based Triazolopyridine Derivatives: Evaluation of Anti‐Breast Cancer Activity on Human Breast Carcinoma." ChemistrySelect 4, no. 43 (2019): 12701–7. http://dx.doi.org/10.1002/slct.201903203.

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9

Tian, Chenyu, Guo Zhang, Ziyi Xia, Nanjun Chen, Shengyong Yang, and Linli Li. "Identification of triazolopyridine derivatives as a new class of AhR agonists and evaluation of anti-psoriasis effect in a mouse model." European Journal of Medicinal Chemistry 231 (March 2022): 114122. http://dx.doi.org/10.1016/j.ejmech.2022.114122.

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10

Chiassai, Leonardo, Rafael Ballesteros-Garrido, Maria Paz Clares, Enrique García-España, Rafael Ballesteros, and Belén Abarca. "Combining Amines and 3-(2-Pyridyl)-[1,2,3]Triazolo[1,5-a]pyridine: An Easy Access to New Functional Polynitrogenated Ligands." Synthesis 51, no. 21 (2019): 4034–42. http://dx.doi.org/10.1055/s-0037-1611901.

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Triazolopyridine-pyridine amine ligands are easily obtained by means of either thermal- or copper(II)-mediated reactions. Starting from a readily accessible iodo derivative of triazolopyridine-pyridine and different amines, this new family of compounds combines aromatic and aliphatic nitrogen atoms with promising coordinating properties. Furthermore, chemical derivatization of a new triazolopyridine-pyridine diamine compound, N1-[6-([1,2,3]triazolo[1,5-a]pyridin-3-yl)pyridin-2-yl]ethan-1,2-diamine, allows the preparation of several remote-pyridine-containing ligands.

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11

Zanotti, L., P. Albertazzi, G. Bonac-corsi, F. Pansini, and G. Mollica. "Neurovegetative Symptoms and Menopause: The Ef-fect of a Triazolopyridine Derivative." Menopause 2, no. 4 (1995): 267. http://dx.doi.org/10.1097/00042192-199502040-00087.

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12

Juan, S. Gómez-Jeria, Robles-Navarro Andrés, and Jaramillo-Hormazábal Ignacio. "A DFT analysis of the relationships between electronic structure and activity at D2, 5-HT1A and 5-HT2A receptors in a series of Triazolopyridinone derivatives." Chemistry Research Journal 7, no. 2 (2022): 6–28. https://doi.org/10.5281/zenodo.11396906.

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<strong>Abstract </strong>The Klopman-Peradejordi-Gómez FQSAR method was applied to search for relationships between the electronic structures of a group of triazolopyridinone derivatives and their activities at the dopamine D<sub>2</sub> receptor and the serotonin 5-HT<sub>1A</sub> and 5-HT<sub>2A</sub> receptors. The electronic structure was calculated with Density Functional Theory at the B3LYP/6-31G(d,p) level after full geometry optimization. D-Cent-QSAR software was employed for obtaining all the local atomic reactivity indices. Statistically significant equations were found for t

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13

Ma, Hongxing, and Tiansheng Mei. "Electrochemical Rearrangement Cyclization Based on Alkyl Carboxylic Acids: Synthesis of Triazolopyridinone Derivatives." Chinese Journal of Organic Chemistry 40, no. 11 (2020): 3982. http://dx.doi.org/10.6023/cjoc202000079.

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14

Shi, Wenqiang, Yu Wang, Chunhui Wu, et al. "Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics." Bioorganic & Medicinal Chemistry Letters 30, no. 8 (2020): 127027. http://dx.doi.org/10.1016/j.bmcl.2020.127027.

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15

Ahmed, Eman M., Nadia A. Khalil, Azza T. Taher, Rana H. Refaey, and Yassin M. Nissan. "Triazolopyridazine derivatives: Synthesis, cytotoxic evaluation, c-Met kinase activity and molecular docking." Bioorganic Chemistry 92 (November 2019): 103272. http://dx.doi.org/10.1016/j.bioorg.2019.103272.

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16

Vetter, Walter, Walter Meister, and Gottfried Oesterhelt. "Triazolopyridine, a new derivative for the structural determination of fatty acids by gas chromatography/mass spectrometry." Organic Mass Spectrometry 23, no. 8 (1988): 566–72. http://dx.doi.org/10.1002/oms.1210230803.

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17

Dymińska, Lucyna, Jerzy Hanuza, Jan Janczak, Maciej Ptak, and Radosław Lisiecki. "The Structural and Optical Properties of 1,2,4-Triazolo[4,3-a]pyridine-3-amine." Molecules 27, no. 3 (2022): 721. http://dx.doi.org/10.3390/molecules27030721.

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The structural and spectroscopic properties of a new triazolopyridine derivative (1,2,4-triazolo[4,3-a]pyridin-3-amine) are described in this paper. Its FTIR spectrum was recorded in the 100–4000 cm−1 range and its FT-Raman spectrum in the range 80–4000 cm−1. The molecular structure and vibrational spectra were analyzed using the B3LYP/6-311G(2d,2p) approach and the GAUSSIAN 16W program. The assignment of the observed bands to the respective normal modes was proposed on the basis of PED calculations. XRD studies revealed that the studied compound crystallizes in the centrosymmetric monoclinic

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18

NAKAO, Tohru, Hiroshi TANAKA, Yasuto MORIMOTO, Shuzo TAKEHARA, Kenichi DEMIZU, and Tetsuya TAHARA. "Studies on the Synthesis of Condensed Pyridazine Derivatives. III. Synthesis and Benzodiazepine Receptor Binding Studies of Condensed Triazolopyridazine Derivatives." YAKUGAKU ZASSHI 110, no. 12 (1990): 922–31. http://dx.doi.org/10.1248/yakushi1947.110.12_922.

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19

Chiang, Kuo-Chen, Fung Fuh Wong, Chih-Shiang Chang, et al. "Synthesis and characterization of 1,3,4-oxadiazole-triazolopyridinone hybrid derivatives as new blue-greenish photoluminescent materials." Journal of Heterocyclic Chemistry 44, no. 3 (2007): 591–96. http://dx.doi.org/10.1002/jhet.5570440313.

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20

NAKAO, T., H. TANAKA, Y. MORIMOTO, S. TAKEHARA, K. DEMIZU, and T. TAHARA. "ChemInform Abstract: Studies on the Synthesis of Condensed Pyridazine Derivatives. Part 3. Synthesis and Benzodiazepine Receptor Binding Studies of Condensed Triazolopyridazine Derivatives." ChemInform 22, no. 48 (2010): no. http://dx.doi.org/10.1002/chin.199148193.

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21

Darehkordi, Ali, Maryam Hosseini, and Fariba Rahmani. "Convenient Synthesis of New Boric Acid Catalyzed 1,2,4‐Triazolopyridinone Derivatives and an Investigation of their Optical Properties." Journal of Heterocyclic Chemistry 56, no. 4 (2019): 1306–11. http://dx.doi.org/10.1002/jhet.3501.

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22

Shin, Ming-Hsiang, Fung Fuh Wong, Chun-Min Lin, Wen-Yi Chen, and Mou-Yung Yeh. "New synthesis of highly potential efficient bluish-green electroluminescent materials based on 1,3,4-oxadiazole–triazolopyridinone–carbazole derivatives for single-layer devices." Heteroatom Chemistry 17, no. 2 (2006): 160–65. http://dx.doi.org/10.1002/hc.20201.

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23

Briguglio, Irene, Erik Laurini, Maria Antonietta Pirisi, et al. "Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics." European Journal of Medicinal Chemistry 141 (December 2017): 460–72. http://dx.doi.org/10.1016/j.ejmech.2017.09.065.

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24

Abarca, Belén, Rafael Ballesteros, and Mostafá Elmasnaouy. "Triazolopyridines 21.1 The stereochemistry of 1-[1,2,3]triazolo[1,5-a] pyridin-7-yl-4-(2H-[1,2,3]triazol-4-yl)-1,3-butadienes and triazolo ring opening derivatives." Arkivoc 2002, no. 6 (2002): 145–51. http://dx.doi.org/10.3998/ark.5550190.0003.613.

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25

Sabnis, Ram W. "Novel Triazolopyridine Derivatives as DGAT2 Inhibitors for Treating Multiple Diseases." ACS Medicinal Chemistry Letters, August 20, 2024. http://dx.doi.org/10.1021/acsmedchemlett.4c00408.

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26

Dashyan, Sh Sh, A. S. Ayvazyan, and R. G. Paronikyan. "Synthesis, Neurotropic Study and SAR of New Derivatives of Triazolopyridine." Pharmaceutical Chemistry Journal, May 22, 2025. https://doi.org/10.1007/s11094-025-03362-8.

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27

Sabnis, Ram W. "Pyrazolopyridine and Triazolopyridine Derivatives as DGAT2 Inhibitors for Treating Multiple Diseases." ACS Medicinal Chemistry Letters, October 14, 2024. http://dx.doi.org/10.1021/acsmedchemlett.4c00485.

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28

Kargbo, Robert B. "Treatment of Metabolic Disorders Using Novel DGAT2 Inhibitors: Pyrazolopyridine and Triazolopyridine Derivatives." ACS Medicinal Chemistry Letters, July 25, 2024. http://dx.doi.org/10.1021/acsmedchemlett.4c00329.

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29

Nettekoven, Matthias, Bernd Puellmann, and Sebastien Schmitt. "Synthesis Access to 2-Amido-5-aryl-8-methoxy-triazolopyridine and 2-Amido-5-morpholino-8-methoxy-triazolopyridine Derivatives as Potential Inhibitors of the Adenosine Receptor Subtypes." ChemInform 34, no. 49 (2003). http://dx.doi.org/10.1002/chin.200349133.

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30

Xu, Zhengshui, Changchun Ye, Xingjie Wang, et al. "Design and synthesis of triazolopyridine derivatives as potent JAK/HDAC dual inhibitors with broad-spectrum antiproliferative activity." Journal of Enzyme Inhibition and Medicinal Chemistry 39, no. 1 (2024). http://dx.doi.org/10.1080/14756366.2024.2409771.

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31

Manaithiya, Ajay, Ozair Alam, Vrinda Sharma, et al. "Current status of novel pyridine fused derivatives as anticancer agents: An insight into future perspectives and structure activity relationship (SAR)." Current Topics in Medicinal Chemistry 21 (September 16, 2021). http://dx.doi.org/10.2174/1568026621666210916171015.

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: Cancer is a heterogeneous disease characterized by an abnormal and uncontrolled division of the cells leading to tumors that invade the adjacent normal tissues. After cardiovascular diseases, it is the second most prevalent disease accounting for one in every six deaths worldwide. This alarming rate thus, demands an urgent need to investigate more effective drugs to combat the said disease. Oxygen and nitrogen-based heterocyclic compounds have shown remarkable therapeutic activity towards several diseases, including cancer. In this review, we have attempted to summarize the work done in the

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32

Guba, Wolfgang, Matthias Nettekoven, Bernd Puellmann, Claus Riemer, and Sebastien Schmitt. "Comparison of Inhibitory Activity of Isomeric Triazolopyridine Derivatives Towards Adenosine Receptor Subtypes or Do Similar Structures Reveal Similar Bioactivities?" ChemInform 35, no. 40 (2004). http://dx.doi.org/10.1002/chin.200440150.

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33

Keesara, Srinivasa Reddy, Ratna Sekhar Bolla, H. BHARATHKUMAR, Sai Balaji Andugulapati, Sreedhar Gundekari, and Mohan Varkolu. "Synthesis, characterization and biological applications of tetramethyl piperidine-triazolopyridazine derivatives." Synlett, August 12, 2024. http://dx.doi.org/10.1055/a-2384-6983.

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In this article, we have synthesized the tetramethyl piperidinetriazolopyridazine derivatives and screened all the molecules for its biological activity against anti-cancer(NCI-H460) cell lines. Among all the tested molecules, the 2-(3-(2,2,6,6-tetramethylpiperidin-4-yl)-3H-[1,2,3]triazolo[4,5-c]pyridazin-6-yl)-5-(2H-1,2,3-triazol-2-yl)phenol (9a) compound significantly inhibitted the cell growth with an IC 50 value of 5.2 μM. We hope this study will help for the development of better lung cancer candidates for the treatment of lung cancer.

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34

Ye, Zenghui, Yanqi Wu, Na Chen, et al. "Enantiospecific electrochemical rearrangement for the synthesis of hindered triazolopyridinone derivatives." Nature Communications 11, no. 1 (2020). http://dx.doi.org/10.1038/s41467-020-17389-w.

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35

Karche, Ranjit S., Shubham R. Bankar, and Vrushali H. Jadhav. "Alternative synthetic route for the pharmacophore of anticancer agent: Triazolopyridazine derivative." Tetrahedron Letters, July 2024, 155193. http://dx.doi.org/10.1016/j.tetlet.2024.155193.

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36

Zhang, Qinghua, You Ran, Honglei Xia, Siwei Song, and Kangcai Wang. "Thermostable Insensitive Energetic Materials Based on a Triazolopyridine Fused Framework with Alternating Nitro and Amine Groups." Synlett, October 27, 2023. http://dx.doi.org/10.1055/s-0043-1763570.

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AbstractIn this work, we designed and synthesized a series of novel triazolopyridine fused-ring compounds with alternating nitro and amine groups. Three compounds showed remarkable thermal stability at 256, 310, and 294 °C, respectively, and a low mechanical sensitivity [impact sensitivity (IS) = 40 J, friction sensitivity (FS) = 324 N; IS = 35 J, FS = 240 N; and IS > 40 J, FS = 324 N, respectively]. Significantly, two of these compounds exhibited a better detonation performance [detonation velocity (D) = 8200 and 8335 m s–1, Detonation pressure (P) = 25.6 and 27.2 GPa, respectively] than t

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37

Chiang, Kuo-Chen, Fung Fuh Wong, Chih-Shiang Chang, et al. "Synthesis and Characterization of 1,3,4-Oxadiazole-triazolopyridinone Hybrid Derivatives as New Blue-Greenish Photoluminescent Materials." ChemInform 38, no. 39 (2007). http://dx.doi.org/10.1002/chin.200739140.

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38

Shin, Ming-Hsiang, Fung Fuh Wong, Chun-Min Lin, Wen-Yi Chen, and Mou-Yung Yeh. "New Synthesis of Highly Potential Efficient Bluish-Green Electroluminescent Materials Based on 1,3,4-Oxadiazole-triazolopyridinone-carbazole Derivatives for Single-Layer Devices." ChemInform 37, no. 31 (2006). http://dx.doi.org/10.1002/chin.200631133.

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