ChemInform Abstract: Synthesis and Antinociceptive Activity of 9‐Phenyloxy or 9‐Acyloxy Derivatives of Xanthene, Thioxanthene and Acridine.

Llama, E. F.; Campo, Carlos; Capo, Miguel Andrés; Anadón, M.J.

doi:10.1002/chin.198951313

Cited by 14 publications

(16 citation statements)

References 1 publication

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“…The intercalative property was referred to the planar aromatic system of the acridine moiety. In the same context, acridines have gained strong ground for various biological activities like antimicrobial, 1 antioxidant, 2 anticancer, [3][4][5] antimalarial, 6 analgesic, 7 antileishmanial, 8 antinociceptive, 9 acetyl cholinesterase inhibitors 10 and antiherpes 11 etc. Amsacrine is the best known compound of 9-anilinoacridines series.…”

Section: Introductionmentioning

confidence: 99%

Molecular Docking studies and in-silico ADMET Screening of Some novel Oxazine substituted 9-Anilinoacridines as Topoisomerase II Inhibitors

Rajagopal¹,

Sankar²,

Selvaraj³

et al. 2017

IJPER

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Introduction:In general, 9-aminoacridine derivatives are inhibiting DNA topoisomerase II (topoII) because of their strong activity due to the ability of acridine nucleus to intercalate into DNA base pair. To get insight of the intermolecular interactions, the molecular docking studies are performed at active site of topoisomerase II. Aim: In this study, an attempt is made for identification of potential ligands from oxazine substituted 9-anilino acridines targeted against topoisomerase-II (1ZXM) using molecular modelling and docking studies by using Schrodinger suit-2012 Maestro 9.3 version. Insilco ADMET screening also performed by qikprop module of Schrodinger suit. Results: The relative binding affinity of the designed compounds towards topoisomerase-II (1ZXM) was selected on the basis of docking score, GLIDE score and interaction patterns. Several compounds showed strong hydrogen bonding interactions with amino acid residues and their hydrophobic interactions and other parameters could also explain their potency to inhibit topoisomerase-II (1ZXM). The oxazine substituted 9-anilino acridine derivatives 1a-1k have good binding affinity with Glide score in the range of -5.7 to -8.06 when compared with the standard ledacrine (-5.24). The ADMET screening of the designed compounds have almost all the properties of the compounds are within the recommended values. Conclusion: Hence, this study provides evidence for consideration of valuable ligands in oxazine substituted 9-anilino acridine derivatives as potential topoisomerase-II inhibitor and further in vitro and in vivo investigations may prove its therapeutic potential

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Section: Introductionmentioning

confidence: 99%

Molecular Docking studies and in-silico ADMET Screening of Some novel Oxazine substituted 9-Anilinoacridines as Topoisomerase II Inhibitors

Rajagopal¹,

Sankar²,

Selvaraj³

et al. 2017

IJPER

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“…Among them, acridine and its derivatives containing a 1,4-dihydropyridine moiety are under constant investigation in view of their profound range of biological activities such as antitumor, 2 antibacterial, 3 antimalarial 4 and antinociceptive activities. 5 The 1,4-naphthoquinone structure is common in numerous natural products associated with antifungal, 6 antibacterial 7 and antiviral activities. 8 A number of 1,4-naphthoquinones containing a nitrogen atom have been shown to possess anticancer activity.…”

Section: Introductionmentioning

confidence: 99%

One‐pot Synthesis of 14‐Aryl‐1,6,7,14‐tetrahydrodibenzo‐[a,i]acridine‐1,6‐dione in Ionic Liquid

Shi

et al. 2009

Chin. J. Chem.

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“…In the same context, acridines have gained strong ground for various biological activities like antimicrobial [1], antioxidant [2], anticancer [3][4][5][6][7], antimalarial [8,9], anti-inflammatory [10], analgesic [11], antileishmanial [12], antinociceptive [13], acetyl cholinesterase inhibitors [14] and antiherpes [15] etc. Acriflavine and Ethacridine are the known antibacterial agents with acridine moiety.…”

Section: Introductionmentioning

confidence: 99%

Microwave Irradated Synthesis, Characterization and Evaluation for their Antibacterial and Larvicidal Activities of some Novel Chalcone and Isoxazole Substituted 9-Anilino Acridines

Rajagopal¹

2015

Open J Chem

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Introduction: Chalcone, isoxazole and acridines have diverse biological activities. A series of novel chalcone and isoxazole substituted 9-anilinoacridines were synthesized for their antibacterial, larvicidal, activities. Methods:A series of novel chalcone and isoxazole substituted 9-anilinoacridines (3a-h and 4a-h) were synthesized from 9-chloroacridine by microwave irradiation method. The antibacterial evaluation was performed by cup-plate method and screened for their larvicidal activity by larval bioassay method. Result:The compounds 3d, 3e, 3f, 3h, 4d, 4f have significant antibacterial activity against Gram +ve bacteria like Staphylococcus aureus, Bacillus megaterium, and Gram -ve Escherichia coli, Klebsiella pneumoniae at 25µg/ml. Compounds 3c, 3f, 4a, 4f have significant larvicidal activity against culex and anopheles species at LC 50 value of 17-36ppm. Conclusion:Many of the compounds have significant antibacterial and larvicidal activities, which are used for further refinement.activity against culex and anopheles species are described. As a part of our ongoing research on searching new potent antimicrobial and larvicidal agents, we have synthesized 9-anilinoacridine analogues bearing the isoxazole residue on anilino rings for antimicrobial and larvicidal evaluation. The results revealed that the newly synthesized derivatives exhibited significant biological activities. Materials and MethodsMelting points were obtained on Veego VMP-1 apparatus in open capillary tubes and are uncorrected. The reactions were monitored by TLC on silica gel thin layer plates. Compounds were analyzed for C, H, N and analytical results obtained for these elements were within ±0.5% of the calculated values for the formula shown. IR spectra were obtained using a Perkin Elmer spectrum-2 FT-IR spectrometer. 1 HNMR and 13 C NMR were recorded on Bruker A VIII 500 MHz Spectrometer. Chemical shifts are in parts per million (ppm). Mass spectra of the final compounds were recorded on a JEOL GC mate Mass Spectrometer. Microwave irradiation was carried out in cata scientific microwave synthesis system 2400 MHZ, catalyst systems, India. Synthesis and characterisation of the compoundsThe compounds were synthesized by microwave irradiation (MW) methods and schematized in scheme 1. The yield and reaction time were summarized (Table 1).

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ChemInform Abstract: Synthesis and Antinociceptive Activity of 9‐Phenyloxy or 9‐Acyloxy Derivatives of Xanthene, Thioxanthene and Acridine.

Cited by 14 publications

References 1 publication

Molecular Docking studies and in-silico ADMET Screening of Some novel Oxazine substituted 9-Anilinoacridines as Topoisomerase II Inhibitors

Molecular Docking studies and in-silico ADMET Screening of Some novel Oxazine substituted 9-Anilinoacridines as Topoisomerase II Inhibitors

One‐pot Synthesis of 14‐Aryl‐1,6,7,14‐tetrahydrodibenzo‐[a,i]acridine‐1,6‐dione in Ionic Liquid

Microwave Irradated Synthesis, Characterization and Evaluation for their Antibacterial and Larvicidal Activities of some Novel Chalcone and Isoxazole Substituted 9-Anilino Acridines

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