New indole derivatives: Synthesis and antibacterial activity

Chikvaidze, I. Sh.; Megrelishvili, N. Sh.; Samsoniya, Sh. A.; Суворов, Н. Н.; Gus'kova, T. A.; Radkevich, T. P.; Бакланова, О. В.

doi:10.1007/bf02464223

Cited by 4 publications

(2 citation statements)

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“…Second pharmacophore, the indole and its various conjugates present in many natural and synthetic molecules exhibit a wide range of significant biological activities, such as antidiabetic [21], anti-inflammatory [22], antimalarial [23], antibacterial [24], antifungal [25], antiviral [26] and anticancer [27]. This moiety is very important for its medicinal and biological aspects, thus attracting a lot of scientific attention.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of non‐toxic anticancer active forskolin‐indole‐triazole conjugates along with their in silico succinate dehydrogenase inhibition studies

Devendar

Arigari

Naga

et al. 2021

Journal of Heterocyclic Chem

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Biologically important three different pharmacophores, forskolin, indole and 1,2,3-triazoles are coupled to obtain a hybrid molecule. Here, we described the synthesis of novel series of forskolin-indole-triazole conjugates 5a-5l by using the Cu(I) catalyzed 1,3-dipolar cycloaddition reaction. Furthermore, the biological significance of the synthesized molecules was assessed by in silico and in vitro modes. All the synthesized compounds were evaluated for in vitro anticancer activity against PC-3, MCF-7, MDA-MB-231, COLO-205, HeLa, WRL-68, RAJI, CHANG and RAW-264.7 cell lines. Compound 5g was found to be the most potent in all the tested cell lines (IC 50 range 9.6-21.66 μg/ml, except COLO-205), 5a, 5b and 5k were observed to exert its effect only against WRL-68 (IC 50 range 27.69-48.18 μg/ml), when compared to parent 3 (IC 50 > 100 μg/ml, tested concentrations 10-50 μg/ml) and standard Doxorubicin (IC 50 range 0.42-3.16 μg/ml). The most potent compound 5g (MEF 50 0.57) was found non-toxic to human erythrocytes as compared to control (MEF 50 0.60) at tested concentration (50 μg/ml). In silico-based succinate dehydrogenase inhibition showed that the synthesized compounds were having potent binding affinity compared to forskolin. Predictive ADMET and toxicity risk assessment analysis revealed that most of the compounds were complying with the standard limit of Lipinski's rule of five for oral bioavailability.

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Section: Introductionmentioning

confidence: 99%

Synthesis of non‐toxic anticancer active forskolin‐indole‐triazole conjugates along with their in silico succinate dehydrogenase inhibition studies

Devendar

Arigari

Naga

et al. 2021

Journal of Heterocyclic Chem

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“…Pyrimido[4, 5-d] Perusal of literature revealed that the indole moiety is probably the most common and important feature of a variety of natural products and medicinal agents with significant biological activities including antimicrobial, 9,10 antiviral 11 and antitumour. 12 The presence of two or more different heterocyclic moieties in a single molecule often enhances the biocidal profile remarkably.…”

Section: Introductionmentioning

confidence: 99%

Eco-friendly Solventless Synthesis of 5-Indolylpyrimido[4,5-d]pyrimidinones and Their Antimicrobial Activity

Jain¹,

Joshi²,

Jain³

2011

Bulletin of the Korean Chemical Society

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A series of 5-indolylpyrimido [4,5-d]pyrimidinones (4a-h) were obtained by multi-component reaction of 3-formylindole (1), thiobarbituric acid/barbituric acid (2) and thiourea/urea (3) under microwave irradiation in dry media. Secondly, grinding together neat reactants also gave the titled compounds in good yields. All the synthesized compounds have been characterized on the basis of elemental analyses and spectral data (IR, 1 H NMR and Mass). Representative compounds were also evaluated for their antimicrobial activity against Rhizopus stolonifer, Fusarium oxysporum, Escherichia coli, and Pseudomonas aeruginosa at different concentrations. Some of the compounds showed promising activity.

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The Design and Synthesis of Novel 2,3-Dihydrobenzo[f]isoquinolin-4(1H)-ones via Sequential Ugi-Heck Reactions by Using an Efficient Heterogeneous Palladium Nanocatalyst

Rasouli

Miri

Ranjbar

2014

J. Heterocyclic Chem.

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A facile and efficient synthesis of N‐alkyl‐2‐(1, 2 dihydro‐1‐methylene‐4‐oxobenzo[f] isoquinoline‐3(4H)‐yl)‐2‐phenylacetamides is performed by the consecutive, two‐step procedure that consists of Ugi and Heck reactions. The Heck reaction was performed both by homogenous and a designed heterogeneous catalyst. The heterogeneous catalyst is a coordinated palladium to 1, 10‐phenanthroline attached to chitosan@Fe3O4 magnetite nanoparticles, which was shown to be more efficient than the homogenous Pd(OAc)2/PPh3 catalyst with good to excellent yields.

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New indole derivatives: Synthesis and antibacterial activity

Cited by 4 publications

References 0 publications

Synthesis of non‐toxic anticancer active forskolin‐indole‐triazole conjugates along with their in silico succinate dehydrogenase inhibition studies

Synthesis of non‐toxic anticancer active forskolin‐indole‐triazole conjugates along with their in silico succinate dehydrogenase inhibition studies

Eco-friendly Solventless Synthesis of 5-Indolylpyrimido[4,5-d]pyrimidinones and Their Antimicrobial Activity

The Design and Synthesis of Novel 2,3-Dihydrobenzo[f]isoquinolin-4(1H)-ones via Sequential Ugi-Heck Reactions by Using an Efficient Heterogeneous Palladium Nanocatalyst

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