Synthesis, Antibacterial, Antifungal and Anti-HIV Evaluation of Schiff and Mannich Bases of Isatin and its Derivatives with Triazole

“…The 2-oxoindole derivatives SU-5416 (semaxanib) and SU-11248 (sunitinib) reportedly have tyrosine kinase inhibitory and anti-angiogenic properties [15]. Schiff and Mannich bases of isatin are reported to exhibit broad antimicrobial properties, including antiviral [16], anti-mycobacterial [17], antifungal, and antibacterial activities [18]. A recent report by our group described the synthesis of 3-methylene-substituted indolinones and their antimalarial activities.…”

Section: A C C E P T E D Accepted Manuscriptmentioning

confidence: 99%

Azide-alkyne cycloaddition en route to 1 H -1,2,3-triazole-tethered 7-chloroquinoline-isatin chimeras: Synthesis and antimalarial evaluation

Raj

Singh

et al. 2013

European Journal of Medicinal Chemistry

126

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Please cite this article as: R. Raj, P. Singh, P. Singh, J. Gut, P.J. Rosenthal, V. Kumar, Azidealkyne cycloaddition en route to 1H-1,2,3-Triazole-tethered 7-chloroquinoline-isatin chimeras: Synthesis and antimalarial evaluation, European Journal of Medicinal Chemistry (2013), doi: 10.1016/ j.ejmech.2013 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. M A N U S C R I P T A C C E P T E D ACCEPTED MANUSCRIPTAzide-alkyne cycloaddition en route to 1H-1,2,3-Triazole-tethered The compound 8h with an optimum combination of longer alkyl chain length and chloro substitutent at C-5 position of isatin ring displayed the best activity among the test compounds. M A N U S C R I P T A C C E P T E D ACCEPTED MANUSCRIPT Abstract:We describe the synthesis and antimalarial activities of 1H-1,2,3-triazole tethered 7-chloroquinolineisatin hybrids. Activity against cultured parasites was dependent on the C-5 substituent of the isatin ring as well as the alkyl chain length between the isatin and 7-chloroquinoline moieties. Compound 8h, with an optimum alkyl chain length (n=3) and a chloro substitutent at the C-5 position of the isatin ring, displayed the best activity among the test compounds, with IC 50 value of 1.21 µM against cultured W2-strain Plasmodium falciparum.

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“…Their important biological activities include antifungal, [1][2][3][4][5][6] antibacterial, 7 anticancer 8 and antiviral, [9][10][11] H1/H2 histamine receptor blockers, cholinesterase active agents, central nervous system (CNS) stimulants, antianxiety and sedatives. [12][13] Antimycotic, fluconazole, itraconazole, ravuconazole and variconazole are therapeutically interesting drug candidates, including 1,2,4-triazole nucleus.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, in vitro Antiproliferative Activity, Binding Modeling of 1,2,4,-Triazoles as New Anti-Breast Cancer Agents

Genç¹,

Genç²,

Tekin³

et al. 2016

ACSi

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This article demonstrates the synthesis of 1,2,4-triazole derivatives and their applications in medicine particularly as anti-breast cancer agents which is a major issue of the present. The synthesized compounds were characterized by elemental analysis, FT-IR and NMR. DFT was used to study the quantum chemical calculations of geometries and vibrational wave numbers of 3-hydroxynaphthyl and p-tolyl substituted 1,2,4-triazoles in the ground state. The scaled harmonic vibrational frequencies obtained from the DFT method were compared with those of the FT-IR spectra and found good agreement. The synthesized 1,2,4-triazole-naphthyl hybrids were screened for the anticancer activity against MCF-7 breast cancer lines. Among them compounds 3 and 7 showed broad spectrum anticancer activity with IC 50 values 9.7 μM and 7.10 μM, respectively and their activity is comparable to that of the standard drugs. The molecular model for binding between the compounds (1-8) and the active site of BRCA2 was obtained on the basis of the computational docking results and the structure-activity relationship.

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Synthesis, Antibacterial, Antifungal and Anti-HIV Evaluation of Schiff and Mannich Bases of Isatin and its Derivatives with Triazole

Cited by 98 publications

References 6 publications

Microwave Assisted Synthesis and Spectral Analysis of Schiff Bases Derived from 2-Amino-5-Aryl-1,3,4-Oxadiazoles

Microwave Assisted Synthesis and Spectral Analysis of Schiff Bases Derived from 2-Amino-5-Aryl-1,3,4-Oxadiazoles

Azide-alkyne cycloaddition en route to 1 H -1,2,3-triazole-tethered 7-chloroquinoline-isatin chimeras: Synthesis and antimalarial evaluation

Design, Synthesis, in vitro Antiproliferative Activity, Binding Modeling of 1,2,4,-Triazoles as New Anti-Breast Cancer Agents

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