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Journal articles on the topic 'Indole Heterocyclic compounds'

Author: Grafiati

Published: 4 June 2021

Last updated: 17 February 2022

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1

Boraei, Ahmed T. A., Ahmed A. M. Sarhan, Sammer Yousuf, and Assem Barakat. "Synthesis of a New Series of Nitrogen/Sulfur Heterocycles by Linking Four Rings: Indole; 1,2,4-Triazole; Pyridazine; and Quinoxaline." Molecules 25, no. 3 (2020): 450. http://dx.doi.org/10.3390/molecules25030450.

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A new series of nitrogen and sulfur heterocyclic systems were efficiently synthesized by linking the following four rings: indole; 1,2,4-triazole; pyridazine; and quinoxaline hybrids. The strength of the acid that catalyzes the condensation of 4-amino-5-(1H-indol-2-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thione 1 with aromatic aldehydes controlled the final product. Reflux in glacial acetic acid yielded Schiff bases 2–6, whereas concentrated HCl in ethanol resulted in a cyclization product at C-3 of the indole ring to create indolo-triazolo-pyridazinethiones 7–16. This fascinating cyclization appr

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2

Mir, Reyaz Hassan, Roohi Mohi-ud-din, Taha Umair Wani, et al. "Indole: A Privileged Heterocyclic Moiety in the Management of Cancer." Current Organic Chemistry 25, no. 6 (2021): 724–36. http://dx.doi.org/10.2174/1385272825666210208142108.

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Heterocyclic are a class of compounds that are intricately entwined into life processes. Almost more than 90% of marketed drugs carry heterocycles. Synthetic chemistry, in turn, allocates a cornucopia of heterocycles. Among the heterocycles, indole, a bicyclic structure consisting of a six-membered benzene ring fused to a five-membered pyrrole ring with numerous pharmacophores that generate a library of various lead molecules. Due to its profound pharmacological profile, indole got wider attention around the globe to explore it fully in the interest of mankind. The current review covers recent

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3

Sonawane, Ratnamala P., and Rahul R. Tripathi. "The Chemistry and Synthesis of 1H-indole-2,3-dione (Isatin) and its Derivatives." International Letters of Chemistry, Physics and Astronomy 12 (September 2013): 30–36. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.12.30.

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Isatins are synthetically versatile substrates, where they can be used for the synthesis of a large variety of heterocyclic compounds. In this, a convenient method has been developed for the conversion of Indoles into Isatins and some heterocyclic derivative were synthesised such as 5- nitro-1H-indole-2,3-dione, 2-methylquinoline-4-carboxylic acid which may be used as raw material for drug synthesis. The general process utilizes the effective method for synthesis of Isatin from Indole is bromination and oxidation with an N-bromosuccinimide-dimethyl sulfoxide reagent. The nitration of Isatin at

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4

El-Sawy, Eslam, Fatma Bassyouni, Sherifa Abu-Bakr, Hanaa Rady, and Mohamed Abdlla. "Synthesis and biological activity of some new 1-benzyl and 1-benzoyl-3-heterocyclic indole derivatives." Acta Pharmaceutica 60, no. 1 (2010): 55–71. http://dx.doi.org/10.2478/v10007-010-0004-0.

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Synthesis and biological activity of some new 1-benzyl and 1-benzoyl-3-heterocyclic indole derivativesStarting from 1-benzyl- (2a) and 1-benzoyl-3-bromoacetyl indoles (2b) new heterocyclic, 2-thioxoimidazolidine (4a, b), imidazolidine-2,4-dione (5a, b), pyrano(2,3-d)imida-zole (8a, band9a, b), 2-substituted quinoxaline (11a, b-17a, b) and triazolo(4,3-a)quinoxaline derivatives (18a, band19a, b) were synthesized and evaluated for their antimicrobial and anticancer activities. Antimicrobial activity screening performed with concentrations of 0.88, 0.44 and 0.22 μg mm-2showed that 3-(1-substitute

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5

Sulthana, Shaheen, and P. Pandian. "A review on Indole and Benzothiazole derivatives its importance." Journal of Drug Delivery and Therapeutics 9, no. 1-s (2019): 505–9. http://dx.doi.org/10.22270/jddt.v9i1-s.2358.

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In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Indole, Benzothiazole and its analogs are versatile substrates, which can be used for the synthesis of numerous heterocyclic compounds. Indole, Benzothiazole and its derivatives are used in organic synthesis and they are used in evaluating new product that possesses different biological activities. Hence, their extensive structural modification has result in different analogues of Indole and Benzothiazole derivatives depicting wide range

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6

Guan, Zong, Jan C. Namyslo, Martin H. H. Drafz, Martin Nieger, and Andreas Schmidt. "Dimerisation, rhodium complex formation and rearrangements of N-heterocyclic carbenes of indazoles." Beilstein Journal of Organic Chemistry 10 (April 10, 2014): 832–40. http://dx.doi.org/10.3762/bjoc.10.79.

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Deprotonation of indazolium salts at low temperatures gives N-heterocyclic carbenes of indazoles (indazol-3-ylidenes) which can be trapped as rhodium complexes (X-ray analysis). In the absence of Rh, the indazol-3-ylidenes spontaneously dimerize under ring cleavage of one of the N,N-bonds and ring closure to an indazole–indole spiro compound which possesses an exocyclic imine group. The E/Z isomers of the imines can be separated by column chromatography when methanol is used as eluent. We present results of a single crystal X-ray analysis of one of the E-isomers, which equilibrate in solution

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7

Ali, Imran, Sofi Danish Mukhtar, Ming Fa Hsieh, Zeid A. Alothman, and Abdulrahman Alwarthan. "Facile synthesis of indole heterocyclic compounds based micellar nano anti-cancer drugs." RSC Advances 8, no. 66 (2018): 37905–14. http://dx.doi.org/10.1039/c8ra07060a.

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8

Ashram, Muhammad, Ahmed Al-Mustafa, Wael A. Al-Zereini, Firas F. Awwadi, and Islam Ashram. "A convenient one-pot approach to the synthesis of novel pyrazino[1,2-a]indoles fused to heterocyclic systems and evaluation of their biological activity as acetylcholinesterase inhibitors." Zeitschrift für Naturforschung B 76, no. 5 (2021): 303–12. http://dx.doi.org/10.1515/znb-2020-0205.

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Abstract Pyrazino[1,2-a]indoles fused with various heterocycles, such as oxazolidine, oxazinane, imidazolidine, hexahydropyrimidine and benzimidazole, were synthesized transition metal-free by domino reactions which involved the condensation of 1-(2-bromoethyl)-3-chloro-1H-indole-2-carbaldehydes 28–31 with various nucleophilic amines, resulting in the formation of two new interesting fused heterocycles. The anticholinesterase, antioxidant and antibacterial activities of the compounds were evaluated. Acetylcholinesterase (AChE) inhibitory activities were tested by Ellman’s assay, antioxidant ac

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9

Kumar, Devendra, Sahil Sharma, Sourav Kalra, Gurpreet Singh, Vikramdeep Monga, and Bhupinder Kumar. "Medicinal Perspective of Indole Derivatives: Recent Developments and Structure-Activity Relationship Studies." Current Drug Targets 21, no. 9 (2020): 864–91. http://dx.doi.org/10.2174/1389450121666200310115327.

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Heterocyclic compounds play a significant role in various biological processes of the human body and many of them are in clinical use due to their diverse, chemical and biological properties. Among these, indole is one of the most promising pharmacologically active molecules. Due to its chemical reactivity, indole has been willingly modified to obtain a variety of new lead molecules, which has been successfully utilized to obtained novel drug candidates for the treatment of different pharmacological diseases. Indole-based compounds such as vincristine (anticancer), reserpine (antihypertensive)

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10

Black, DS, N. Chaichit, BM Gatehouse, and GI Moss. "Unusual Formation of New Indole-Containing Heterocyclic Ring Systems." Australian Journal of Chemistry 40, no. 12 (1987): 1965. http://dx.doi.org/10.1071/ch9871965.

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The oxazinoindoletrione (3) underwent reaction with aqueous ammonia in methanol or ethanol to yield the polycyclic methyl or ethyl esters (4) and (5) respectively. Reaction of trione (3) with gaseous ammonia in dry ethanol gave the aminobenzodiazepinone (7). This compound lost ammonia on heating in toluene to give compound (11) and in the presence of methanol or ethanol gave the methyl or ethyl esters (9) and (10) respectively. The structures of compounds (4), (7) and (10) were all established by X-ray crystallography.

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11

Zapol’skii, Viktor A., Ursula Bilitewski, Sören R. Kupiec, Isabell Ramming, and Dieter E. Kaufmann. "Polyhalonitrobutadienes as Versatile Building Blocks for the Biotargeted Synthesis of Substituted N-Heterocyclic Compounds." Molecules 25, no. 12 (2020): 2863. http://dx.doi.org/10.3390/molecules25122863.

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Substituted nitrogen heterocycles are structural key units in many important pharmaceuticals. A new synthetic approach towards heterocyclic compounds displaying antibacterial activity against Staphylococcus aureus or cytotoxic activity has been developed. The selective synthesis of a series of 64 new N-heterocycles from the three nitrobutadienes 2-nitroperchloro-1,3-butadiene, 4-bromotetrachloro-2-nitro-1,3-butadiene and (Z)-1,1,4-trichloro-2,4-dinitrobuta-1,3-diene proved feasible. Their reactions with N-, O- and S-nucleophiles provide rapid access to push-pull substituted benzoxazolines, ben

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12

Varun, Varun, Sonam Sonam, and Rita Kakkar. "Isatin and its derivatives: a survey of recent syntheses, reactions, and applications." MedChemComm 10, no. 3 (2019): 351–68. http://dx.doi.org/10.1039/c8md00585k.

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13

Foldesi, Tamas, Balazs Volk, and Matyas Milen. "A Review of 2,3-Benzodiazepine-related Compounds: Diazepines and 1,2,5- Triazepines Fused with Five-membered Nitrogen Heterocycles." Current Organic Synthesis 15, no. 6 (2018): 729–54. http://dx.doi.org/10.2174/1570179415666180601101856.

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Background: 2,3-Benzodiazepines represent an important class of biologically active compounds, some members of this family have reached the human clinical stage. With formal bioisosteric replacement of the benzene ring to five-membered nitrogen heterocycles, several new diazepine and 1,2,5-triazepine derivatives have been synthesized in the past 30 years. Objective: Investigations in the field of heterocyclic chemistry is very important, because there could be several new medicines among the newly synthesized heterocyclic ring systems, which could be used against several diseases which have no

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14

Sayed, Mostafa, Adel Mohamed Kamal Eldean, Mostafa Mohamed Ahmed, and Reda Hassanien. "SYNTHESIS OF SOME NEW HETEROCYCLIC COMPOUNDS CONTAINING INDOLE MOEITY." European Chemical Bulletin 6, no. 4 (2017): 171. http://dx.doi.org/10.17628/ecb.2017.6.171-176.

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15

ATHENA, G. S., JAGADEESH KRISHNAN, ERINGATHODI SURESH, and RONY RAJAN PAUL. "Using Homoenolate Annulated Products for Synthesis of Indole Embedded Derivatives." Asian Journal of Chemistry 33, no. 2 (2021): 319–24. http://dx.doi.org/10.14233/ajchem.2021.22986.

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The facile transformation of the functionalized spiro-cyclopentanones obtained by N-heterocyclic carbenes (NHC) catalyzed homoenolate annulation strategy, leading to the synthesis of indole embedded compounds is described.

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16

Shelar, Santosh V., and Narshinha P. Argade. "Facile synthesis of indolizinoindolone, indolylepoxypyrrolooxazole, indolylpyrrolooxazolone and isoindolopyrazinoindolone heterocycles from indole and imide derivatives." Organic & Biomolecular Chemistry 19, no. 27 (2021): 6160–69. http://dx.doi.org/10.1039/d1ob00754h.

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Acid-induced and base-induced regioselective coupling reactions of indole with cyclic imide derived lactamols and N-(2-iodoethyl)imides are demonstrated to provide structurally interesting heterocyclic compounds.

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17

Venkov, Atanas, Stela Statkova-Abeghe, and Atanaska Donova. "Amidoalkylation of heteroaromatic compounds with adducts of acyl chlorides and 3,4-dihydroisoquinoline and isoquinoline." Open Chemistry 2, no. 1 (2004): 234–46. http://dx.doi.org/10.2478/bf02476193.

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AbstractThe N-acyliminium intermediates of 3,4-dihydroisoquinoline and salts of isoquinoline with acyl chlorides were successfully used as amidoalkylating reagents toward synthesis of heterocyclic aromatics as indole, pyrrole, thiophene and pyrazine.

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18

Li, Dongli, Panpan Wu, Ning Sun, et al. "The Diversity of Heterocyclic N-oxide Molecules: Highlights on their Potential in Organic Synthesis, Catalysis and Drug Applications." Current Organic Chemistry 23, no. 5 (2019): 616–27. http://dx.doi.org/10.2174/1385272823666190408095257.

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The synthesis and chemistry of heterocyclic N-oxide derivatives such as those from pyridine and indazole are very well-known due to their usefulness as versatile synthetic intermediates and their biological importance. These classes of organic compounds have been demonstrated in many interesting and amazing functionalities, particularly vital in the areas including metal complexes formation, catalysts design, asymmetric catalysis and synthesis, and medicinal applications (some potent N-oxide compounds with anticancer, antibacterial, anti-inflammatory activity, etc.). Therefore, the heterocycli

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19

Abdel-Rahman, Reda M., Mohammad Saleh I. T. Makki, and Wafa A. Baker Bawazir. "Synthesis of Fluorine Heterocyclic Nitrogen Systems Derived From Sulfa Drugs as PhotochemicalProbe Agents for Inhibition of Vitiligo Disease-Part II." E-Journal of Chemistry 7, s1 (2010): S93—S102. http://dx.doi.org/10.1155/2010/467564.

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Some more new bioactive fluorine heterocyclic systems containing sulfur and nitrogen as six-membered rings such as;N,Nʼ-disubstituted-thiobarbituric acid, 3-thioxo-1,2,4-triazino[5,6-b]indole, 3-sulfanilamido-1,2,4-triazino[5,6-b]indole and 2-trifluoromethyl-4-imino-6-(sulfamido)1,3,5-triazino [3,2-a]indole derivatives (2-13) have been synthetically derived from the interaction of sulfa drugs with fluorine organic compounds (aldehydes, ketones, anhydride) followed by ring closure reactions. Structures of the targets have been established from their elemental and spectral data. Compounds 3, 6,

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20

Lynch, Daniel E., Laura J. Nicholls, Graham Smith, Karl A. Byriel, and Colin H. L. Kennard. "Molecular co-crystals of 2-aminothiazole derivatives." Acta Crystallographica Section B Structural Science 55, no. 5 (1999): 758–66. http://dx.doi.org/10.1107/s0108768199003146.

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A series of molecular adducts of 2-aminothiazole derivatives – 2-aminothiazole, 2-amino-2-thiazoline and 2-aminobenzothiazole with the carboxylic-acid-substituted heterocyclics indole-2-carboxylic acid, N-methylpyrrole-2-carboxylic acid and thiophene-2-carboxylic acid – have been prepared and characterized using X-ray powder diffraction and in five cases by single-crystal X-ray diffraction methods. These five compounds are the adducts of 2-amino-2-thiazolium with indole-2-carboxylate [(C3H7N2S)+(C9H6NO2)−], and N-methylpyrrole-2-carboxylate [(C3H7N2S)+-(C6H6NO2)−], 2-aminobenzothiazolium with

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21

Golubeva, I. S., N. P. Yavorskaya, L. V. Ektova, et al. "ANTITUMOR ACTIVITY OF SOME DERIVATIVES OF INDOLO[2,3-A]CARBAZOLES N-GLYCOSIDES WITH XYLOSE CARBOHYDRATE RESIDUE." Russian Journal of Biotherapy 19, no. 4 (2020): 86–93. http://dx.doi.org/10.17650/1726-9784-2020-19-4-86-93.

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Introduction. The search for new antineoplastic agents in a series of indolo[2,3-a]-carbazole derivatives is an urgent and promising direction, since compounds with antitumor activity have been found in this class. In the chemical fusion laboratory, N.N. Blokhin National Medical Research Center оf the Ministry of Health of Russia has developed an original and effective method for the synthesis of glycosides of indolo[2,3-a]-pyrrolo[3,4-c]carbazoles, which makes it possible to synthesize derivatives of N-glycosides of indolo[2,3-a]carbazoles with different substituents in the heterocyclic parts

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22

Agasti, Soumitra, Aniruddha Dey, and Debabrata Maiti. "Palladium-catalyzed benzofuran and indole synthesis by multiple C–H functionalizations." Chemical Communications 53, no. 49 (2017): 6544–56. http://dx.doi.org/10.1039/c7cc02053h.

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Heterocyclic compounds are commonly found in the core structures of several pharmaceuticals, natural products, and agrochemicals, thus spurring intensive research for conducting their synthesis in a mild and simpler way.

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23

Lang, Damanpreet K., Rajwinder Kaur, Rashmi Arora, Balraj Saini, and Sandeep Arora. "Nitrogen-Containing Heterocycles as Anticancer Agents: An Overview." Anti-Cancer Agents in Medicinal Chemistry 20, no. 18 (2020): 2150–68. http://dx.doi.org/10.2174/1871520620666200705214917.

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Background: Cancer is spreading all over the world, and it is becoming the leading cause of major deaths. Today’s most difficult task for every researcher is to invent a new drug that can treat cancer with minimal side effects. Many factors, including pollution, modern lifestyle and food habits, exposure to oncogenic agents or radiations, enhanced industrialization, etc. can cause cancer. Treatment of cancer is done by various methods that include chemotherapy, radiotherapy, surgery and immunotherapy in combination or singly along with kinase inhibitors. Most of the anti-cancer drugs use the c

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24

Halawa, Ahmed H., Shimaa Mohamed Abd El-Gilil, Ahmed H. Bedair, et al. "Synthesis, biological activity and molecular modeling study of new Schiff bases incorporated with indole moiety." Zeitschrift für Naturforschung C 72, no. 11-12 (2017): 467–75. http://dx.doi.org/10.1515/znc-2017-0025.

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AbstractA new series of heterocyclic Schiff bases2–9containing indole moiety were synthesized by facile and efficient condensation of indole-3/2/5-carboxaldehyde (1a/1b/1c) with different aromatic and heterocyclic primary amines using conventional and/or microwave irradiation methods. The structures of the obtained compounds were assigned by sophisticated spectroscopic and spectrometric techniques (1D-NMR, 2D-NMR and MS). The synthesized compounds were screened for their cytotoxicity and antibacterial activities. In vitro cytotoxicity screening revealed that compound5exhibited moderate activit

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25

Li, Min-Xin, Xiao-Jia Pu, Xia Zhang, et al. "Synthesis and Biological Evaluation of Heterocyclic Substituted Bis(indolyl)methanes." Current Organic Synthesis 17, no. 2 (2020): 144–50. http://dx.doi.org/10.2174/1570179417666200124103400.

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Background: Bis(indolyl)methane derivatives are widely found in nature with a broad range of biological and pharmacological activities. The development of techniques for the synthesis and functionalization of bis(indolyl)methanes have attracted more and more attention in recent years. Objective: To study the synthesis and biological activity of heterocyclic substituted bis(indolyl)methanes. Materials and Methods: A series of heterocyclic substituted bis(indolyl)methanes (3a-3p) have been prepared by condensation reaction of indole and heterocyclic aldehydes catalyzed by boron trifluoride ether

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26

Sayed, Mostafa, Adel M. Kamal El-Dean, Mostafa Ahmed, and Reda Hassanien. "Synthesis of some heterocyclic compounds derived from indole as antimicrobial agents." Synthetic Communications 48, no. 4 (2018): 413–21. http://dx.doi.org/10.1080/00397911.2017.1403627.

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27

Eldehna, Wagdy M., Ghada S. Hassan, Sara T. Al-Rashood, Hamad M. Alkahtani, Abdulrahman A. Almehizia, and Ghada H. Al-Ansary. "Marine-Inspired Bis-indoles Possessing Antiproliferative Activity against Breast Cancer; Design, Synthesis, and Biological Evaluation." Marine Drugs 18, no. 4 (2020): 190. http://dx.doi.org/10.3390/md18040190.

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Diverse indoles and bis-indoles extracted from marine sources have been identified as promising anticancer leads. Herein, we designed and synthesized novel bis-indole series 7a–f and 9a–h as Topsentin and Nortopsentin analogs. Our design is based on replacing the heterocyclic spacer in the natural leads by a more flexible hydrazide linker while sparing the two peripheral indole rings. All the synthesized bis-indoles were examined for their antiproliferative action against human breast cancer (MCF-7 and MDA-MB-231) cell lines. The most potent congeners 7e and 9a against MCF-7 cells (IC50 = 0.44

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28

Bhardwaj, Niti, S. K. Saraf, Pankaj Sharma, and Pradeep Kumar. "Syntheses, Evaluation and Characterization of Some 1, 3, 4-Oxadiazoles as Antimicrobial Agents." E-Journal of Chemistry 6, no. 4 (2009): 1133–38. http://dx.doi.org/10.1155/2009/698023.

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1,3,4-Oxadiazoles show various biological activities and have been synthesized from different compounds. 1,3,4-oxadiazole is popularly known for its antimicrobial, anti-inflammatory, pesticidal and antihypertensive activitiesetc. It is well known that the synthesis of heterocyclic compounds tend to contain multi-structure in a molecule. The ring formation involves the condensation reaction. The challenge is to develop the ring system by incorporating the indole nucleus into it through the proposed reaction scheme. There are two free positions for the substitution in the oxadiazole ring system.

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29

Lynch, Daniel E., Tariq Latif, Graham Smith, Karl A. Byriel, Colin H. L. Kennard, and Simon Parsons. "Molecular Cocrystals of Carboxylic Acids. XXXI Adducts of 2-Aminopyrimidine and 3-Amino-1,2,4-triazole with Heterocyclic Carboxylic Acids." Australian Journal of Chemistry 51, no. 5 (1998): 403. http://dx.doi.org/10.1071/c97201.

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A series of molecular adducts of 2-aminopyrimidine and 3-amino-1,2,4-triazole with heterocyclic carboxylic acids have been prepared and characterized by using X-ray powder diffraction and in four cases by single-crystal X-ray diffraction methods. These four compounds are the (1 : 1) adducts of 2-aminopyrimidine with indole-3-acetic acid [(C4H5N3)(C10H9NO2)], N-methylpyrrole-2-carboxylic acid [(C4H5N3)(C6H7NO2)] and thiophen-2-carboxylic acid [(C4H5N3)(C5H4O2S)], and the (1 : 1) adduct of 3-amino-1,2,4-triazole with thiophen-2-carboxylic acid [(C2H4N4)(C5H4O2S)]. Other compounds described are t

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30

Montoya-Aguilera, Julia, Jeremy R. Horne, Mallory L. Hinks, et al. "Secondary organic aerosol from atmospheric photooxidation of indole." Atmospheric Chemistry and Physics 17, no. 18 (2017): 11605–21. http://dx.doi.org/10.5194/acp-17-11605-2017.

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Abstract. Indole is a heterocyclic compound emitted by various plant species under stressed conditions or during flowering events. The formation, optical properties, and chemical composition of secondary organic aerosol (SOA) formed by low-NOx photooxidation of indole were investigated. The SOA yield (1. 3 ± 0. 3) was estimated from measuring the particle mass concentration with a scanning mobility particle sizer (SMPS) and correcting it for wall loss effects. The high value of the SOA mass yield suggests that most oxidized indole products eventually end up in the particle phase. The SOA parti

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31

Hiwarkar, Ajay Devidas, Vimal Chandra Srivastava, and Indra Deo Mall. "Simultaneous adsorption of nitrogenous heterocyclic compounds by granular activated carbon: parameter optimization and multicomponent isotherm modeling." RSC Adv. 4, no. 75 (2014): 39732–42. http://dx.doi.org/10.1039/c4ra06395c.

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32

Sajiki, Hironao, Yasunari Monguchi, and Yoshinari Sawama. "Synthesis of Triazole, Indole, and Five or Six-Membered Saturated Heterocyclic Compounds." HETEROCYCLES 91, no. 2 (2015): 239. http://dx.doi.org/10.3987/rev-14-811.

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33

Higashio, Yasuhiko, and Takayuki Shoji. "Heterocyclic compounds such as pyrrole, pyridines, pyrrolidine, piperidine, indole, imidazol and pyrazines." Applied Catalysis A: General 260, no. 2 (2004): 251–59. http://dx.doi.org/10.1016/s0926-860x(03)00197-2.

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34

Shaik, Adamshafi, Allaka Tejeswara Rao, S. V. M. Mohan Rao, and Pilli V. V. N. Kishore. "Synthesis of Biologically Active Novel Indole Fused Heterocyclic Derivatives: Molecular Modeling Studies." Asian Journal of Chemistry 33, no. 7 (2021): 1677–84. http://dx.doi.org/10.14233/ajchem.2021.23179.

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A novel series of fluoro/methoxy indole analogues 6 was synthesized and the final targets were confirmed by IR, 1H & 13C NMR and mass spectral analysis. Novel 3-substituted indole derivatives estimate for their antibacterial, antioxidant activities particularly the parent core combined with benzamides ring significantly. From antibacterial activities, compounds 6c, 6e and 6b show the highest bacterial activity against S. epidermidis, S. aureus, E. coli, with zone of inhibition 34, 30, 28 mm, respectively. Novel fluoroindole derivatives 6c, 6b, 6i shows an excellent antioxidant activity wit

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35

Dixon, David P., Jonathan D. Sellars, and Robert Edwards. "The Arabidopsis phi class glutathione transferase AtGSTF2: binding and regulation by biologically active heterocyclic ligands." Biochemical Journal 438, no. 1 (2011): 63–70. http://dx.doi.org/10.1042/bj20101884.

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The plant-specific phi class of glutathione transferases (GSTFs) are often highly stress-inducible and expressed in a tissue-specific manner, suggestive of them having important protective roles. To date, these functions remain largely unknown, although activities associated with the binding and transport of reactive metabolites have been proposed. Using a sensitive and selective binding screen, we have probed the Arabidopsis thaliana GSTFs for natural product ligands from bacteria and plants. Uniquely, when overexpressed in bacteria, family members GSTF2 and GSTF3 bound a series of heterocycl

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36

Kaur, Kamalpreet, and Vikas Jaitak. "Recent Development in Indole Derivatives as Anticancer Agents for Breast Cancer." Anti-Cancer Agents in Medicinal Chemistry 19, no. 8 (2019): 962–83. http://dx.doi.org/10.2174/1871520619666190312125602.

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Background:Breast Cancer (BC) is the second most common cause of cancer related deaths in women. Due to severe side effects and multidrug resistance, current therapies like hormonal therapy, surgery, radiotherapy and chemotherapy become ineffective. Also, the existing drugs for BC treatment are associated with several drawbacks such as poor oral bioavailability, non-selectivity and poor pharmacodynamics properties. Therefore, there is an urgent need for the development of more effective and safer anti BC agents.Objective:This article explored in detail the possibilities of indole-based heteroc

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Syromolotov, Alexander V., Alexander A. Kimyashov, and Diana R. Khafizova. "Synthesis of 1-phenylindoles derivatives." Butlerov Communications 58, no. 4 (2019): 53–57. http://dx.doi.org/10.37952/roi-jbc-01/19-58-4-53.

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The growing needs of medicine and pharmacology induce synthetic organic chemistry to constantly be in the process of modernizing existing methods of synthesis and developing new ones. Since ancient times, the high physiological activity of indole derivatives has been widely known. Indole is a heterocyclic condensed aromatic compound that is part of the molecules of a multitude of compounds with biochemical and physiological value. A large number of drugs of the indole group obtained synthetically are derivatives of arylindols. One of the most common methods of obtaining arylindoles is the use

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Sharmila, N., T. V. Sundar, G. Satish, A. Ilangovan, and P. Venkatesan. "Two new isatin derivatives: 1-benzyl-4,5,6-trimethoxyindoline-2,3-dione and 1-benzyl-5-fluoroindoline-2,3-dione." Acta Crystallographica Section C Structural Chemistry 71, no. 11 (2015): 975–78. http://dx.doi.org/10.1107/s2053229615018422.

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Isatin (1H-indole-2,3-dione) derivatives represent synthetically useful substrates which can be used to prepare a broad range of heterocyclic compounds. In the title compounds, C18H17NO5, (I), and C15H10FNO2, (II), the isatin ring systems are planar and form a dihedral angle of 73.04 (7)° in (I) and 76.82 (11)° in (II) with the benzyl groups. The bicyclic scaffolds in both compounds are almost superimposable, with an r.m.s. deviation of 0.061 Å. The crystal structures of both derivatives are stabilized by C—H...O interactions. These contacts generate anR12(7) ring motif in (I) and aC(7) chain

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Karataş, Semra, İrfan Çapan, and Süleyman Servi. "Synthesis of Indole and Benzimidazole Substituted Novel 16-Arylidene Steroid Derivatives." Letters in Organic Chemistry 16, no. 11 (2019): 884–90. http://dx.doi.org/10.2174/1570178616666190305130217.

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Novel aza-heterocyclic substituted dehydroepiandrosterone derivatives were synthesized through a three-step reaction sequence. Some new O-alkylated 4-hydroxybenzaldehydes were synthesized from the reaction of substituted benzaldehydes with dihalogen compounds which have different chain lengths. 16-Arylidene steroids were synthesized from the base-catalyzed aldol condensation of O-alkylated 4-hydroxybenzaldehydes and dehydroepiandrosterone. New indolyl and benzimidazolyl substituted steroid derivatives as hybrid molecules were obtained from the reaction of 16-arylidene steroids with indole or b

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Walter, Tatjana, Kareen H. Veldmann, Susanne Götker, et al. "Physiological Response of Corynebacterium glutamicum to Indole." Microorganisms 8, no. 12 (2020): 1945. http://dx.doi.org/10.3390/microorganisms8121945.

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The aromatic heterocyclic compound indole is widely spread in nature. Due to its floral odor indole finds application in dairy, flavor, and fragrance products. Indole is an inter- and intracellular signaling molecule influencing cell division, sporulation, or virulence in some bacteria that synthesize it from tryptophan by tryptophanase. Corynebacterium glutamicum that is used for the industrial production of amino acids including tryptophan lacks tryptophanase. To test if indole is metabolized by C. glutamicum or has a regulatory role, the physiological response to indole by this bacterium wa

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Waltman, R. J., and J. Bargon. "Electrically conducting polymers: a review of the electropolymerization reaction, of the effects of chemical structure on polymer film properties, and of applications towards technology." Canadian Journal of Chemistry 64, no. 1 (1986): 76–95. http://dx.doi.org/10.1139/v86-015.

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The electrochemical oxidation of aromatic heterocyclic compounds thiophene, pyrrole, and indole and benzenoid and nonbenzenoid polycyclic hydrocarbons azulene, fluorene, and pyrene yield electrically conducting polymers with conductivities of 10−5–10 S/cm. The presence of substituents affects the electrical conductivity of these films and also their electroactive properties. Furthermore, substituents determine whether electropolymerization of these compounds can occur or whether soluble products are formed. The relative importance of these pathways is dependent on the stability of the intermed

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Meng, Liubei, Rui Shi, Qiong Wang, and Shu Wang. "Analysis of Floral Fragrance Compounds of Chimonanthus praecox with Different Floral Colors in Yunnan, China." Separations 8, no. 8 (2021): 122. http://dx.doi.org/10.3390/separations8080122.

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In order to better understand the floral fragrance compounds of Chimonanthus praecox belonging to genus Chimonanthus of Chimonanaceae in Yunnan, headspace solid-phase microextraction combined with gas chromatography-mass spectrometry was used to analyze these compounds from four C. praecox plants with different floral colors. Thirty-one types of floral fragrance compounds were identified, among which terpenes, alcohols, esters, phenols, and heterocyclic compounds were the main compounds. Interestingly, the floral fragrance compounds identified in the flowers of C. praecox var. concolor include

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Yang, Zuoyi, Junhui Zhou, Yanbin Xu, et al. "Analysis of the Metabolites of Indole Degraded by an Isolated Acinetobacter pittii L1." BioMed Research International 2017 (2017): 1–10. http://dx.doi.org/10.1155/2017/2564363.

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Indole and its derivatives are typical nitrogen heterocyclic compounds and have been of immense concern since they are known for the risk of their toxic, recalcitrant, and carcinogenic properties for human and ecological environment. In this study, a Gram-negative bacterial strain of eliminating indole was isolated from a coking wastewater. The strain was confirmed as Acinetobacter pittii L1 based on the physiological and biochemical characterization and 16S ribosomal DNA (rDNA) gene sequence homology. 400 mg/L indole could be completely removed within 48 h by the strain on the optimum conditi

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Baraldi, Pier G., Roberta Budriesi, Barbara Cacciari, et al. "Synthesis and Calcium Antagonist Activity of Dialkyl 1,4-Dihydro-2,6-dimethyl-4-(nitrogenous heteroaryl)-3,5-pyridine Dicarboxylates." Collection of Czechoslovak Chemical Communications 57, no. 1 (1992): 169–78. http://dx.doi.org/10.1135/cccc19920169.

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A new series of 4-(nitrogenous heteroaryl)-1,4-dihydropyridine antagonists II - XVI were synthesized and screened for inotropic, chronotropic and calcium antagonist properties, in order to evaluate the effect on pharmacological activity of replacement of the 4-aryl group of nifedipine-like drugs by heterocyclic moieties, such as quinoline, indole, carbazole and pyrazole. The most potent bradycardic compounds of the series (VIII - X, XII and XIII) elicited weak calcium antagonist activity and were stronger negative inotropic.

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Albino, Sonaly L., Jamire M. da Silva, Michelangela S. de C. Nobre, et al. "Bioprospecting of Nitrogenous Heterocyclic Scaffolds with Potential Action for Neglected Parasitosis: A Review." Current Pharmaceutical Design 26, no. 33 (2020): 4112–50. http://dx.doi.org/10.2174/1381612826666200701160904.

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Neglected parasitic diseases are a group of infections currently considered as a worldwide concern. This fact can be attributed to the migration of these diseases to developed and developing countries, associated with therapeutic insufficiency resulted from the low investment in the research and development of new drugs. In order to overcome this situation, bioprospecting supports medicinal chemistry in the identification of new scaffolds with therapeutically appropriate physicochemical and pharmacokinetic properties. Among them, we highlight the nitrogenous heterocyclic compounds, as they are

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Kamel, Mona M., Mohamed K. Abdel-hameid, Hala B. El-Nassan, and Eman A. El-Khouly. "Synthesis and Cytotoxicity Evaluation of Novel Indole Derivatives as Potential Anti-Cancer Agents." Medicinal Chemistry 15, no. 8 (2019): 873–82. http://dx.doi.org/10.2174/1573406415666190408125514.

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Background: Marine sponges and tunicates have been a wealthy source of cytotoxic compounds such as indole alkaloids. Most of the indole alkaloids show in vitro cytotoxic and antineoplastic activities against a wide range of cancer cell lines. Objective: Three series of bioisosteres of marine indole alkaloids (meridianins) were synthesized and the compounds were tested for their in vitro anti-proliferative activity against HCT-116 cellline. In the design of the targeted analogues, the 2-aminopyrimidine ring of merdianins was replaced with 5-aminopyrazole, pyrazolo[1,5-a]pyrimidine and pyrazolo[

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Abd El-Aal, Hassan A. K., and Ali A. Khalaf. "Friedel–Crafts Chemistry. Part 53. Divergent and Diversity-Oriented Synthesis of Condensed Indole Scaffolds via Friedel–Crafts Ring Closure Approach." Australian Journal of Chemistry 72, no. 4 (2019): 276. http://dx.doi.org/10.1071/ch18537.

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A series of indole-fused medium-sized N-heterocyclic systems 10a–h were prepared from laboratory-synthesized indole-based esters 9a–h via intramolecular Friedel–Crafts cyclizations induced by both trifluoromethanesulfonic acid and AlCl3/CH3NO2 catalysts under suitable conditions. The synthetic sequence to precursors 9a–h that started from simple N-methylindole-2-carboxylic acid involved conversion to aminoindoles 2a, b, reaction with α,β-unsaturated acid chlorides to yield acyclic amides 5a–d, ring closure to tricyclic lactams 6a–d, and carbonyl reduction to respective pyrido and azepino tricy

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Journal, Baghdad Science. "Synthesis and Evaluation Antibacterial Activity of Some New Substituted 5-Bromoisatin Containing Five, Six Heterocyclic Ring." Baghdad Science Journal 13, no. 2 (2016): 345–59. http://dx.doi.org/10.21123/bsj.13.2.345-359.

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This research includes the synthesis of some new different heterocyclic derivatives of 5-Bromoisatin. New sulfonylamide, diazine, oxazole, thiazole and 1,2,3-triazole derivatives of 5-Bromoisatin have been synthesized. The synthesis process started by the reaction of 5-Bromoisatin with different reagents to obtain schiff bases of 5-Bromoisatin intermediate compounds(1, 8, 19) by using glacial acetic acid as a catalyst in three routes. The first route, 5-Bromoisatin reacted with p-aminosulfonylchloride to product compound(1), then converted to sulfonyl amide derivatives(2-7) by the reaction of

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Čík, Gabriel, František Šeršeň, Anton Blažej, Viktor Hayden та Bohuslava Havlínová. "An investigation of the formation of molecular complexes of O-(3,5-dinitrobenzoyl)-O-acetylcellulose with n- and π-donors". Collection of Czechoslovak Chemical Communications 53, № 3 (1988): 581–87. http://dx.doi.org/10.1135/cccc19880581.

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Soluble O-(3,5-dinitrobenzoyl)-O-acetylcellulose was synthesized, and the formation of molecular complexes with n- and π-donors was investigated. The formation of complexes obeys the Langmuir adsorption isotherm adjusted for macromolecules. The formation of molecular complexes with low-molar mass compounds of the type of heterocyclic compounds, aromatic amines and condensed hydrocarbons was confirmed by electric resistance measurements. The largest decrease in the specific resistance by 2-3 orders of magnitude was observed with indole and phenothiazine, while the specific resistance of the oth

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A. Joule, John, Mercedes Alvarez, and Marisa Salas. "Marine, Nitrogen-containing Heterocyclic Natural Products — Structures and Syntheses of Compounds Containing Indole Units." HETEROCYCLES 32, no. 7 (1991): 1391. http://dx.doi.org/10.3987/rev-91-429.

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