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Journal articles on the topic 'Indazole derivatives'

Author: Grafiati

Published: 4 June 2025

Last updated: 1 August 2025

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1

Kousalya, Patil* Dr. Somashekhar M. Metri Divya Shirke. "Synthetic Strategy And Pharmacological Approaches Of Benzopyrazole: A Review." Int. J. in Pharm. Sci. 1, no. 7 (2023): 261–68. https://doi.org/10.5281/zenodo.8161568.

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Indazole-containing derivatives represent one of the most important heterocycles in drug molecules. The presence of two nitrogen sites located in adjacent positions in the molecular structure allows indazole, at low concentrations in mildly acid or basic media, to form 1H and 2H tautomers via acid-base interactions as well as symmetrical dimers by hydrogen bonding. Indazole is also known as 1H-Benzopyrazole, 2-Azaindole. Synonyms of indazoles are 1H-Indazole, 2H-indazole, Isoindazole1,2-Diazaindene and Benzopyrazole. The first compound known to contain the indazole ring system was indazole and

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2

Saketi, Jagan Mohana Rao, S. N. Murthy Boddapati, Raghuram M., et al. "Pd(PPh3)4 Catalyzed Synthesis of Indazole Derivatives as Potent Anticancer Drug." Applied Sciences 10, no. 11 (2020): 3792. http://dx.doi.org/10.3390/app10113792.

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A series of 3-aryl indazoles and 1-methyl-3-aryl indazole derivatives are prepared with exceptional yields by coupling with several arylboronic acids and methylation by two dissimilar approaches. The as-prepared indazole derivatives (3a–3j) and their N-methyl derivatives (5a–5j) are evaluated for in vitro anticancer activity against two cancer cell lines, HCT-116 and MDA-MB-231. The results reveal that the indazole derivatives tested display mild to moderate anticancer activities against the cell lines tested.

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3

S, Zine Babasaheb, Najan Sopan A, Dhonde Shrikant P, and Mazahar Farooqui. "Synthesis, Characterization and Biological Evaluation of Schiff's bases containing Indazole Moiety." Der Pharma Chemica 15, no. 3 (2023): 4. https://doi.org/10.5281/zenodo.13319875.

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Indazole containing derivatives represent one of the most important heterocycles in pharmaceuticals. Substituted indazole derivatives bear a variety of functional groups and display versatile biological activities. A series of new Indazolyl derivatives have been prepared from commercially available N-substituted-3-indazole carboxylic acid and methanol with sulphuric acid. Synthesis of these compounds proceeds through the formation of 1-ethyl-1H-indazole -3-carboxylate, by acidic esterification, then conveted in to 1-ethyl-1H-indazole -3-hydrazide using hyrdazine hydrate in ethanol at reflux te

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4

Babasaheb, S. Zine, A. Najan Sopan, and Farooqui Mazahar. "Synthesis, Characterization and Biological Evaluation of Schiff's bases containing Indazole Moiety." DER PHARMA CHEMICA 15, no. 3 (2023): 4. https://doi.org/10.4172/0975-413X.15.3.34-37.

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Indazole containing derivatives represent one of the most important heterocycles in pharmaceuticals. Substituted indazole derivatives bear a variety of functional groups and display versatile biological activities. A series of new Indazolyl derivatives have been prepared from commercially available N-substituted-3-indazole carboxylic acid and methanol with sulphuric acid. Synthesis of these compounds proceeds through the formation of 1-ethyl-1H-indazole -3-carboxylate, by acidic esterification, then conveted in to 1-ethyl-1H-indazole -3-hydrazide using hyrdazine hydrate in ethanol at reflux te

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5

S, Zine Babasaheb, Sopan A. Najan, Shrikant P. Dhonde, and Mazahar Farooqui. "Synthesis, Characterization and Biological Evaluation of Schiff's bases containing Indazole Moiety." Der Pharma Chemica 15, no. 3 (2023): 4. https://doi.org/10.5281/zenodo.10952012.

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Indazole containing derivatives represent one of the most important heterocycles in pharmaceuticals. Substituted indazole derivatives bear a variety of functional groups and display versatile biological activities. A series of new Indazolyl derivatives have been prepared from commercially available N-substituted-3-indazole carboxylic acid and methanol with sulphuric acid. Synthesis of these compounds proceeds through the formation of 1-ethyl-1H-indazole -3-carboxylate, by acidic esterification, then conveted in to 1-ethyl-1H-indazole -3-hydrazide using hyrdazine hydrate in ethanol at reflux te

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6

Alam, Ryan M., and John J. Keating. "Regioselective N-alkylation of the 1H-indazole scaffold; ring substituent and N-alkylating reagent effects on regioisomeric distribution." Beilstein Journal of Organic Chemistry 17 (August 2, 2021): 1939–51. http://dx.doi.org/10.3762/bjoc.17.127.

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The indazole scaffold represents a promising pharmacophore, commonly incorporated in a variety of therapeutic drugs. Although indazole-containing drugs are frequently marketed as the corresponding N-alkyl 1H- or 2H-indazole derivative, the efficient synthesis and isolation of the desired N-1 or N-2 alkylindazole regioisomer can often be challenging and adversely affect product yield. Thus, as part of a broader study focusing on the synthesis of bioactive indazole derivatives, we aimed to develop a regioselective protocol for the synthesis of N-1 alkylindazoles. Initial screening of various con

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7

Wan, Yichao, Shengzhuo He, Wei Li, and Zilong Tang. "Indazole Derivatives: Promising Anti-tumor Agents." Anti-Cancer Agents in Medicinal Chemistry 18, no. 9 (2019): 1228–34. http://dx.doi.org/10.2174/1871520618666180510113822.

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Background: Currently, cancer continues being a dramatically increasing and serious threat to public health. Although many anti-tumor agents have been developed in recent years, the survival rate of patients is not satisfactory. The poor prognosis of cancer patients is closely related to the occurrence of drug resistance. Therefore, it is urgent to develop new anti-tumor agents to make up for the deficiency. Indazoles is an important class of heterocyclic compounds possessing a variety of biological activities, such as anti-tumor, anti-bacterial, antiinflammatory, anti-depressant and anti-hype

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8

Bhattacharjee, Suvam, Sudip Laru, and Alakananda Hajra. "Remote difunctionalization of 2H-indazoles using Koser's reagents." Chemical Communications 58, no. 7 (2022): 981–84. http://dx.doi.org/10.1039/d1cc06129a.

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9

Saketi, Jaganmohana Rao, S. N. Murthy Boddapati, Raghuram M, Geetha Bhavani Koduru, and Haribabu Bollikolla. "Novel Substituted Indazoles towards Potential Antimicrobial Agents." Oriental Journal Of Chemistry 37, no. 2 (2021): 508–12. http://dx.doi.org/10.13005/ojc/370234.

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The in vitroantimicrobial properties of a series of N-methyl-3-aryl indazoles (5a-5j) were screened. In this present work, we describe our efforts towards the development of potent antimicrobial activity of synthesized indazole derivatives. The antimicrobial activities of the prepared compounds were investigated against four bacterial strains: Xanthomonas campestris, Escherichia coli, Bacillus cereus, Bacillus megaterium, and a fungal strain Candida albicans. The biological evaluation studies of these indazole derivatives revealed that some of these tested compounds have shown moderate to good

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10

Hariyanti, Hariyanti, Arry Yanuar, Kusmardi Kusmardi, and Hayun Hayun. "(7E)-3-(4-Methoxyphenyl)-7-[(4-methoxyphenyl)methylidene]-4,5,6,7-tetrahydro-3aH-indazole." Molbank 2020, no. 4 (2020): M1162. http://dx.doi.org/10.3390/m1162.

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Indazole derivatives are well known to have various pharmacological activities. We synthesized a novel derivative of indazole, namely (7E)-3-(4-methoxyphenyl)-7-[(4-methoxyphenyl)methylidene]-4,5,6,7-tetrahydro-3aH-indazole by condensation reaction between 3-(4-methoxyphenyl)-3,3a,4,5,6,7-hexahydro-2H-indazole and 4-methoxy-benzaldehyde in good yield (61%).

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11

Tellal, Sakina, Badr Jismy, Djamila Hikem-Oukacha, and Mohamed Abarbri. "Synthesis of Trifluoromethylated Pyrimido[1,2-b]indazole Derivatives through the Cyclocondensation of 3-Aminoindazoles with Ketoester and Their Functionalization via Suzuki-Miyaura Cross-Coupling and SNAr Reactions." Molecules 29, no. 1 (2023): 44. http://dx.doi.org/10.3390/molecules29010044.

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A new series of trifluoromethylated pyrimido[1,2-b]indazol-4(1H)-one derivatives was synthesized with good to excellent yields through a simple condensation of 3-aminoindazole derivatives with ethyl 4,4,4-trifluoro 3-oxobutanoate. The functionalization of the corresponding chlorinated fused tricyclic scaffolds via Suzuki-Miyaura and aromatic nucleophilic substitution reactions led to the synthesis of highly diverse trifluoromethylated pyrimido[1,2-b]indazole derivatives with good yields.

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12

Shiri, Pezhman, Atefeh Roosta, Wim Dehaen, and Ali Mohammad Amani. "Recent Strategies in Transition-Metal-Catalyzed Sequential C–H Activation/Annulation for One-Step Construction of Functionalized Indazole Derivatives." Molecules 27, no. 15 (2022): 4942. http://dx.doi.org/10.3390/molecules27154942.

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Designing new synthetic strategies for indazoles is a prominent topic in contemporary research. The transition-metal-catalyzed C–H activation/annulation sequence has arisen as a favorable tool to construct functionalized indazole derivatives with improved tolerance in medicinal applications, functional flexibility, and structural complexity. In the current review article, we aim to outline and summarize the most common synthetic protocols to use in the synthesis of target indazoles via a transition-metal-catalyzed C–H activation/annulation sequence for the one-step synthesis of functionalized

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13

Zhang, Shu-Guang, Chao-Gen Liang, and Wei-Hua Zhang. "Recent Advances in Indazole-Containing Derivatives: Synthesis and Biological Perspectives." Molecules 23, no. 11 (2018): 2783. http://dx.doi.org/10.3390/molecules23112783.

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Indazole-containing derivatives represent one of the most important heterocycles in drug molecules. Diversely substituted indazole derivatives bear a variety of functional groups and display versatile biological activities; hence, they have gained considerable attention in the field of medicinal chemistry. This review aims to summarize the recent advances in various methods for the synthesis of indazole derivatives. The current developments in the biological activities of indazole-based compounds are also presented.

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14

Pozo-Martínez, Josué, Vicente J. Arán, Matías Zúñiga-Bustos, et al. "In Vitro Evaluation of New 5-Nitroindazolin-3-one Derivatives as Promising Agents against Trypanosoma cruzi." International Journal of Molecular Sciences 25, no. 20 (2024): 11107. http://dx.doi.org/10.3390/ijms252011107.

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Chagas disease is a prevalent health problem in Latin America which has received insufficient attention worldwide. Current treatments for this disease, benznidazole and nifurtimox, have limited efficacy and may cause side effects. A recent study proposed investigating a wide range of nitroindazole and indazolone derivatives as feasible treatments. Therefore, it is proposed that adding a nitro group at the 5-position of the indazole and indazolone structure could enhance trypanocidal activity by inducing oxidative stress through activation of the nitro group by NTRs (nitroreductases). The study

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15

Boddapati, S. N. Murthy, Jagan Mohan Rao Saketi, Baby Ramana M, Maheswara Rao Gokada, Suri Babu Patchipala, and Hari Babu Bollikolla. "Synthesis of Pharmacologically Active Indazoles and Its Analogues: A Review." Caribbean Journal of Science and Technology 09, no. 01 (2021): 20–34. http://dx.doi.org/10.55434/cbi.2021.9107.

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Studies on heterocyclic compounds are an evergreen branch of organic chemistry and attract the attention of chemists working not only in the field of natural products but also in synthetic chemistry. Indazole and its derivatives are one of the most vital heterocycles in drug molecules. Diversely substituted indazole derivatives have gained considerable attention in the field of medicinal chemistry due to their versatile biological activities. This mini review aims to abridge the recent (2011-2021 till date) advances in various methods for the synthesis of indazole derivatives. Moreover, the cu

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16

Petko, Kirill I., and Andrey A. Filatov. "N-Difluoromethylindazoles." Journal of Organic and Pharmaceutical Chemistry 20, no. 3 (2022): 3–11. http://dx.doi.org/10.24959/ophcj.22.265823.

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Aim. To study the possibility of the N-difluoromethylation and separation of 1-difluoromethyl and 2-difluoromethyl isomers of C-substituted indazoles, as well as some possibilities of functionalization of such molecules.Results and discussion. The N-difluoromethylation of indazole derivatives containing bromine, iodine, and nitro groups in various positions of the heterocyclic ring was studied. In all cases, the conditions for the separation of isomers – N-difluoromethylation products – in positions 1 and 2 were found. The corresponding amines, esters of carboxylic and boric acids were obtaine

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17

Rodríguez-Villar, Karen, Lilián Yépez-Mulia, Miguel Cortés-Gines, et al. "Synthesis, Antiprotozoal Activity, and Cheminformatic Analysis of 2-Phenyl-2H-Indazole Derivatives." Molecules 26, no. 8 (2021): 2145. http://dx.doi.org/10.3390/molecules26082145.

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Indazole is an important scaffold in medicinal chemistry. At present, the progress on synthetic methodologies has allowed the preparation of several new indazole derivatives with interesting pharmacological properties. Particularly, the antiprotozoal activity of indazole derivatives have been recently reported. Herein, a series of 22 indazole derivatives was synthesized and studied as antiprotozoals. The 2-phenyl-2H-indazole scaffold was accessed by a one-pot procedure, which includes a combination of ultrasound synthesis under neat conditions as well as Cadogan’s cyclization. Moreover, some c

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18

Digambar, Dr Kokane Balaji. "Facile Synthesis Of 1H-Indazoles Through IodobenzeneCatalyzed C–H Amination Under Mild And Metal-Free Conditions." IOSR Journal of Applied Chemistry 18, no. 1 (2025): 01–03. https://doi.org/10.9790/5736-1801010103.

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The transition-metal- and halogen-free synthesis of N-aryl substituted 1H-indazole and derivatives was accomplished on the basis of the iodobenzene-catalyzed intramolecular C -H amination of hydrazones under mild conditions. Reactions of hydrazones derived from ketones and hydrazines with a catalytic amount of iodobenzene in the presence of Oxone as an oxidant in trifluoroacetic acid took place to afford 1H indazoles in moderate to good yields.

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19

Ren, Demin, Guoqiang Kuang, Xiaolian Hu, and Xiaofang Li. "Synthesis of novel dispiro[indazole-5,3′-pyrrolidine-2′,3″-indole] derivatives via 1,3-dipolar cycloaddition of azomethine ylide." Journal of Chemical Research 41, no. 7 (2017): 427–29. http://dx.doi.org/10.3184/174751917x14981229444848.

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The 1,3-dipolar cycloaddition of azomethine ylide, generated in situ from isatin and sarcosine, to 5-arylmethylidene-1-phenyl-6,7-dihydro-1 H-indazol-4(5 H)-ones afforded novel 1′-methyl-4′-aryl-1-phenyl-6,7-dihydrodispiro[indazole-5,3′-pyrrolidine-2′,3″-indole]-2″,4(1 H,1″ H)-diones in moderate yields. The structures of all the products were characterised thoroughly by NMR, IR, HRMS, together with X-ray crystallographic analysis.

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20

S. AL-Rawi, Muna, Huda A. Hassan, Dheefaf F. Hassan та Ismaeel Y. Majeed. "New Series of Substituted Heterocyclics Derived from α , β – Unsaturated Ketone and Their Cytotoxic Activity Tumor Cell Lines". Oriental Journal of Chemistry 34, № 6 (2018): 2826–31. http://dx.doi.org/10.13005/ojc/340620.

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The aldol condensation of 2-acetylnaphthalene with 9-anthracene carboxaldehyde afforded α, β-unsaturated keton (1) . New heterocyclic compounds containing: cyclohexenone[2], indazole[3], pyrimidinethion [4], thiazolo fused pyrimidine[5], isoxazoline[6], substituted pyrazoline[7]a-d and pyrimidinone[8] rings system were synthesized from α, β-unsaturated keton[1]. Cyclization of [1] with ethylacetoacetate gave the mentioned heterocycle cyclohexanone [2]. The cyclo condensation of [2] with hydrazine gave the new indazole derivative [3]. furthermore, the reation of [1]with thiourea gives thiopyrmi

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21

Yadav, Mithlesh, Balasubramanian Narasimhan, and Archana Kapoor. "Development of 2-dimensional and 3-dimensional QSAR models of Indazole derivatives as TTK inhibitors having Anticancer potential." Current Chemistry Letters 13, no. 1 (2024): 225–40. http://dx.doi.org/10.5267/j.ccl.2023.6.006.

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The study aimed to explore the anticancer efficacy of indazole pharmacophore by analyzing a series of 109 derivatives of indazole as Tyrosine Threonine Kinase (TTK) inhibitors through quantitative activity relationship analysis using 2D and 3D QSAR techniques. The best 2D-QSAR model was generated by the MLR method, showing a high correlation coefficient (r2) of 0.9512, and good internal (q2), and external (pred_r2) cross-validation regression coefficients of 0.8998, and 0.8661, respectively. The residual values were modest, indicating good agreement between the observed and predicted pIC50 val

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22

Karangiya, Krushnakumar L., Manoj F. Dhaduk, and Jatin J. Upadhyay. "Design, synthesis, characterization and antimicrobial screening of newly synthesized indazoles of vanillin analogues." Current Chemistry Letters 14, no. 1 (2025): 51–58. http://dx.doi.org/10.5267/j.ccl.2024.10.002.

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A series of 6-(Aryl)-4-[4-(2,4-dichlorophenylmethoxy)-3-methoxyphenyl]-2,3,4,5-tetrahydro-indazol-3-one derivatives (3a-3i) have been synthesized by refluxing of previously synthesized Ethyl-4-(aryl)-6-[4-(2,4-Dichlorophenylmethoxy)-3-methoxyphenyl]-2-oxo-cyclohex-3-eneoates (2a-2i) with hydrazine hydrate in methanol for 7-8 hours in presence of catalytic amount of glacial acetic acid. The analytical and physical data of all the synthesized compounds (2a-2i) and (3a-3i) were observed and reported. The structures of each newly synthesized Indazole derivative have been characterized by various m

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23

Raut, Santosh, Atul Tidke, Bharat Dhotre, and Pathan Mohd Arif. "Different Strategies to the Synthesis of Indazole and its Derivatives: A Review." Mini-Reviews in Organic Chemistry 17, no. 4 (2020): 363–404. http://dx.doi.org/10.2174/1570193x16666190430160324.

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In this review, works of various researchers working on the synthesis of indazole and their related compound are cited. The review comprises of methodologies for the synthesis of 1H and 2H indazole derivatives, along with some pharmacological activities. In this review, research papers published in various peer-reviewed journals between the year 2000 and year 2017 are enlisted in alphabetical order.

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24

Alaime, T., M. Daniel, M. A. Hiebel, E. Pasquinet, F. Suzenet, and G. Guillaumet. "Access to 1H-indazoles, 1H-benzoindazoles and 1H-azaindazoles from (het)aryl azides: a one-pot Staudinger-aza-Wittig reaction leading to N–N bond formation?" Chemical Communications 54, no. 60 (2018): 8411–14. http://dx.doi.org/10.1039/c8cc03612h.

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25

Chen, Dong-Mei, Jia-Yan Liu, Ming Wei, Bing-Wei Wang, Ruo-Han Chu, and Dong-Sheng Chen. "Synthesis of indazolo[5,4-b][1,6]naphthyridine and indazolo[6,7-b][1,6]naphthyridine derivatives." Heterocyclic Communications 25, no. 1 (2019): 15–21. http://dx.doi.org/10.1515/hc-2019-0006.

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AbstractA simple method for the synthesis of the title compounds by an efficient in-situ reduction and cyclization reactions of aromatic aldehydes, tert-butyl 2,4-dioxopiperidine-1-carboxylate and 5-nitro-1H-indazole or 6-nitro-1H-indazole was developed.

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26

Bui, Thi Thanh Cham, Hue Linh Luu, Thi Thanh Luong, et al. "An Alternative Method for Synthesizing N,2,3-Trimethyl-2H-indazol-6-amine as a Key Component in the Preparation of Pazopanib." Chemistry 6, no. 5 (2024): 1089–98. http://dx.doi.org/10.3390/chemistry6050063.

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Due to its application as an anti-cancer drug, pazopanib (1) has attracted the interest of many researchers, and several studies on pazopanib synthesis have been reported over the years. This paper provides a novel route for synthesizing N,2,3-trimethyl-2H-indazol-6-amine (5), which is a crucial building block in the synthesis of pazopanib from 3-methyl-6-nitro-1H-indazole (6). By alternating between the reduction and two methylation steps, compound 5 was obtained in a yield comparable (55%) to what has been reported (54%). It is noteworthy that the last step of N2-methylation also yielded N,N

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27

Wang, Guodong, Jian Sun, Kai Wang, et al. "Palladium-catalyzed direct C–H nitration and intramolecular C–H functionalization for the synthesis of 3-nitro-1-(phenylsulfonyl)-1H-indazole derivatives." Organic Chemistry Frontiers 6, no. 10 (2019): 1608–12. http://dx.doi.org/10.1039/c9qo00367c.

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28

Zaidi, Saiyid Aftab Ahmad, Shahjahan, and Khwaja Salahuddin Siddiqui. "Coordination properties of new indazole derivatives." Transition Metal Chemistry 18, no. 1 (1993): 51–54. http://dx.doi.org/10.1007/bf00136049.

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29

Ghosh, Sumit, Susmita Mondal, and Alakananda Hajra. "Direct Catalytic Functionalization of Indazole Derivatives." Advanced Synthesis & Catalysis 362, no. 18 (2020): 3768–94. http://dx.doi.org/10.1002/adsc.202000423.

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30

Wan, Hao, Dongting Li, Huadan Xia, et al. "Synthesis of 1H-indazoles by an electrochemical radical C_sp²–H/N–H cyclization of arylhydrazones." Chemical Communications 58, no. 5 (2022): 665–68. http://dx.doi.org/10.1039/d1cc04656j.

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Rodríguez-Villar, Karen, Alicia Hernández-Campos, Lilián Yépez-Mulia, et al. "Design, Synthesis and Anticandidal Evaluation of Indazole and Pyrazole Derivatives." Pharmaceuticals 14, no. 3 (2021): 176. http://dx.doi.org/10.3390/ph14030176.

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Candidiasis, caused by yeasts of the genus Candida, is the second cause of superficial and mucosal infections and the fourth cause of bloodstream infections. Although some antifungal drugs to treat candidiasis are available, resistant strains to current therapies are emerging. Therefore, the search for new candicidal compounds is certainly a priority. In this regard, a series of indazole and pyrazole derivatives were designed in this work, employing bioisosteric replacement, homologation, and molecular simplification as new anticandidal agents. Compounds were synthesized and evaluated against

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Jin, Tienan, Fan Yang, and Yoshinori Yamamoto. "Facile and efficient synthesis of indazole derivatives by 1,3-cycloaddition of arynes with diazo compounds and azomethine imides." Collection of Czechoslovak Chemical Communications 74, no. 6 (2009): 957–72. http://dx.doi.org/10.1135/cccc2009014.

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N-Unsubstituted indazoles 3 and 1-arylindazoles 4 are readily available in good to high yields through [3+2] cycloaddition of 2-(trimethylsilyl)aryl triflates 1 and diazo compounds in the presence of KF or CsF under mild reaction conditions. Furthermore, we found that azomethine imides also underwent cycloaddition reaction with 2-(trimethylsilyl)phenyl triflates (1a) in the presence of KF to afford indazolone derivatives 6 in moderate yields.

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33

Ramos Silva, Manuela, Vânia M. Moreira, Cláudia Cardoso, Ana Matos Beja та Jorge A. R. Salvador. "1H-Indazole and 2H-indazole derivatives of androsta-5,16-dien-3β-ol". Acta Crystallographica Section C Crystal Structure Communications 64, № 4 (2008): o217—o219. http://dx.doi.org/10.1107/s0108270108005842.

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34

Gopi, Bandaru, and Vijayaparthasarathi Vijayakumar. "An efficient and simple approach for synthesizing indazole compounds using palladium-catalyzed Suzuki–Miyaura cross-coupling." RSC Advances 14, no. 36 (2024): 26494–504. http://dx.doi.org/10.1039/d4ra04633a.

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35

Rajesham, Bandari, Vemula Arunkumar, Praveen Kumar Naikawadi, and K. Shiva Kumar. "Copper-catalyzed cascade C–N coupling/C–H amination: one pot synthesis of imidazo[1,2-b]indazole." New Journal of Chemistry 44, no. 37 (2020): 15816–20. http://dx.doi.org/10.1039/d0nj03022h.

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36

Mollineda-Diogo, Niurka, Sergio Sifontes-Rodríguez, María Magdalena Aguirre-García, et al. "3-Alkoxy-1-Benzyl-5-Nitroindazole Derivatives Are Potent Antileishmanial Compounds." International Journal of Molecular Sciences 25, no. 19 (2024): 10582. http://dx.doi.org/10.3390/ijms251910582.

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Indazoles have previously been identified as molecules with antiprotozoal activity. In this study, we evaluate the in vitro activity of thirteen 3-alkoxy-1-benzyl-5-nitroindazole derivatives (series D) against L. amazonensis, L. infantum, and L. mexicana. In vitro, cytotoxicity against mouse peritoneal macrophages and growth inhibitory activity in promastigotes were evaluated for all compounds, and those showing adequate activity and selectivity were tested against intracellular amastigotes. Transmission and scanning electron microscopy were employed to study the effects of 3-alkoxy-1-benzyl-5

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Zhou, Jian, Chuanliu Yin, Tianshuo Zhong, et al. "A direct synthesis method towards spirocyclic indazole derivatives via Rh(iii)-catalyzed C–H activation and spiroannulation." Organic Chemistry Frontiers 8, no. 18 (2021): 5024–31. http://dx.doi.org/10.1039/d1qo00805f.

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A rhodium(iii)-catalyzed [4 + 1] spiroannulation of N-aryl phthalazine-diones (pyridazine-diones) with diazo compounds to construct spirocyclic indazole derivatives with diverse structures is described.

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38

Gholamhosseyni, Maral, and Ebrahim Kianmehr. "A ruthenium-catalyzed alkenylation–annulation approach for the synthesis of indazole derivatives via C–H bond activation." Organic & Biomolecular Chemistry 16, no. 33 (2018): 5973–78. http://dx.doi.org/10.1039/c8ob00999f.

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39

Yin, Chuanliu, Tianshuo Zhong, Xiangyun Zheng, Lianghao Li, Jian Zhou, and Chuanming Yu. "Direct synthesis of indazole derivatives via Rh(iii)-catalyzed C–H activation of phthalazinones and allenes." Organic & Biomolecular Chemistry 19, no. 35 (2021): 7701–5. http://dx.doi.org/10.1039/d1ob01458g.

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An Rh(iii)-catalyzed annulation of phthalazinones and various allenes was developed, leading to the formation of indazole derivatives. This catalytic system exhibits excellent functional group tolerance and atom economy.

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40

Cerecetto, Hugo, Alejandra Gerpe, Mercedes Gonzalez, Vicente Aran, and Carmen de Ocariz. "Pharmacological Properties of Indazole Derivatives: Recent Developments." Mini-Reviews in Medicinal Chemistry 5, no. 10 (2005): 869–78. http://dx.doi.org/10.2174/138955705774329564.

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41

Katayama, Hajime, Yong-ming Zhu, Kimiyoshi Kaneko, et al. "Synthesis of Indolo[1,2-b]indazole Derivatives." HETEROCYCLES 61, no. 1 (2003): 147. http://dx.doi.org/10.3987/com-03-s9.

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42

Hassan, Alaa A., Yusria R. Ibrahim, and Ahmed M. Shawky. "Indazole, oxathiadiazole, and thiadiazine derivatives from thiosemicarbazides." Journal of Sulfur Chemistry 28, no. 2 (2007): 211–22. http://dx.doi.org/10.1080/17415990701230596.

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43

Lang, Florian, and Agnes Görlach. "Heterocyclic indazole derivatives as SGK1 inhibitors, WO2008138448." Expert Opinion on Therapeutic Patents 20, no. 1 (2009): 129–35. http://dx.doi.org/10.1517/13543770903365209.

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44

Claramunt, Rosa M., Concepción López, Ana López, et al. "Synthesis and biological evaluation of indazole derivatives." European Journal of Medicinal Chemistry 46, no. 4 (2011): 1439–47. http://dx.doi.org/10.1016/j.ejmech.2011.01.027.

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45

Pérez-Villanueva, Jaime, Félix Matadamas-Martínez, Lilián Yépez-Mulia, et al. "Synthesis and Cytotoxic Activity of Combretastatin A-4 and 2,3-Diphenyl-2H-indazole Hybrids." Pharmaceuticals 14, no. 8 (2021): 815. http://dx.doi.org/10.3390/ph14080815.

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Cancer is the second leading cause of death, after cardiovascular diseases. Different strategies have been developed to treat cancer; however, chemotherapy with cytotoxic agents is still the most widely used treatment approach. Nevertheless, drug resistance to available chemotherapeutic agents is still a serious problem, and the development of new active compounds remains a constant need. Taking advantage of the molecular hybridization approach, in the present work we designed, synthesized, and tested the cytotoxic activity of two hybrid compounds and seven derivatives based on the structure o

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46

Wei, Wei, Zhihao Liu, Xiuli Wu, et al. "Synthesis and biological evaluation of indazole derivatives as anti-cancer agents." RSC Advances 11, no. 26 (2021): 15675–87. http://dx.doi.org/10.1039/d1ra01147b.

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One of the synthesized indazole derivatives, 2f, displayed inhibitory activities against proliferation, migration and invasion of breast cancer cell line 4T1, with the potential of inducing cell apoptosis, and suppressing tumor growth in vivo.

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47

Liu, Li, Pengxing Jiang, Yongguo Liu, Hongguang Du, and Jiajing Tan. "Direct radical alkylation and acylation of 2H-indazoles using substituted Hantzsch esters as radical reservoirs." Organic Chemistry Frontiers 7, no. 16 (2020): 2278–83. http://dx.doi.org/10.1039/d0qo00507j.

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48

Lin, Shengsheng, Xiaomei Cheng, Balati Hasimujiang, Zhongnan Xu, Fengtan Li, and Zhixiong Ruan. "Electrochemical regioselective C–H selenylation of 2H-indazole derivatives." Organic & Biomolecular Chemistry 20, no. 1 (2022): 117–21. http://dx.doi.org/10.1039/d1ob02108g.

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A metal- and oxidant-free, electrochemical strategy for the regioselective selenylation of 2H-indazole derivatives has been developed, with broad substrate scope and moderate to good yields, under mild and environment-friendly reaction conditions.

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49

Farooqui, Mazahar, Nasir Ali Shafakat Ali, Zaheer Zaheer, Zia Ur Rahman, and Ashpaq Khan. "Synthesis, Anti-bacterial, Analgesic and Anti-inflammatory Activities of Some New Biologically Important Indazole Derivatives." International Journal of Drug Design and Discovery 1, no. 4 (2024): 314–24. https://doi.org/10.37285/ijddd.1.4.5.

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A series of new indazolyl derivatives (1.1A - 1.5E) have been prepared from commercially available N-methyl-3-indazole carboxylic acid and 7-amino cephalosporic acid. The synthesized compounds were evaluated for anti-bacterial, analgesic and in vivo anti-inflammatory activities using acetic acid writhing in mice and carrageenan paw oedema method in mice. The series of compounds have analgesic activity in the order 1.4D>1.3C>1.5E>1.2B >1.1A Compound 1.3C had maximum zone of inhibition for Bacillus thurengensis, Staphylococus aureus, Bacillus Subtilis and showed least zone of inhibit

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Nan'ya, Seiko, Kaname Katsuraya, Yoshie Itamoto, Eturǒ Maekawa, and Yoshio Ueno. "Condensation of 2H-indazole-4,7-dione derivatives with 2-aminophenol derivatives." Journal of Heterocyclic Chemistry 25, no. 5 (1988): 1373–74. http://dx.doi.org/10.1002/jhet.5570250519.

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