Towards the Design and Development of Agents with Broad Spectrum Chemotherapeutic Properties for the Effective Treatment of HIV / AIDS

Sriram, Dharmarajan; Yogeeswari, Perumal

doi:10.2174/0929867033457142

Cited by 28 publications

(11 citation statements)

References 55 publications

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“…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

122

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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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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

122

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“…Some of these compounds are also known for their applications as anti-verus of human imminidéficience (VIH) and antituberculosis,[192021222324] antimalaria,[25262728] antifungal,[2930] antiflaviviridae,[31] and spermicidal[32] agents.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, hematological, biochemical, and neurotoxicity screening of some Mannich base hydrochlorides

et al. 2013

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Background:Mannich bases are an important class of compounds in medicinal chemistry with a wide spectrum of biological activities, however, knowledge on their toxicity is limited.Materials and Methods:Two Mannich base hydrochlorides 1a (2-thienyl-β-dimethylaminoethyl ketone hydrochloride) and 1b (β-dimethylaminopropiophenone hydrochloride) were synthesized and characterized on the basis of their infrared and nuclear magnetic resonance spectral data. The potential effects of the synthesized compounds (5 mg/kg, i.p, during 30 days) on relative weight, hematological parameters, biochemical parameters, and neurotoxicity were tested using male Wistar rat.Results:The results showed that compound 1b alters body weight on the first 10 days (182%, P < 0.01) and on the last 10 days (107%, P < 0.01) of treatment. The same treatment decreases food intake (P < 0.01) and increases water intake (P < 0.05). Both compounds induced a deficit on rotarod test manifested by a decrease of grasping time (1a: 65.33%, P < 0.01; 1b: 60.55%, P < 0.01) and fall time (1a: 59.75%, P < 0.01; 1b: 56.81%, P < 0.01) only on the last day of training. Moreover, Mannich base 1b decreases the liver relative weight (22.24%, P < 0.01). It was also observed that both products decrease the total serum cholesterol (Ch) levels (1a: 52.87%, P < 0.01; 1b: 64.70%, P < 0.01). Interestingly, compounds 1a and 1b affect hematological parameters manifested by an increase of the number of white blood cells (1a: 32.29%, P < 0.05; 1b: 20.64%, P < 0.05) and red blood cells (RBCs) (1a: 12.57%, P < 0.05; 1b: 20.11%, P < 0.05), an increase of red cell hemoglobin concentration (1a: 10.48%, P < 0.05; 1b: 16.12%, P < 0.05) and of the volume occupied by RBCs or hematocrit (1a: 18.28%, P < 0.05; 1b: 15.56%, P < 0.05), and an increase of the number of platelets (1a: 16.80%, P < 0.05; 1b: 39.96%, P < 0.05) accompanied by a decrease in hemoglobin level only with the compound 1a (7.41%, P < 0.05).Conclusion:These results show that both compounds 1a and 1b induced a hypoxia status associated to low level of Ch and liver toxicity. The deficit observed by rotarod could be explained by the myorelaxant effect of the used products.

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“…In addition, isatin and N-alkylisatin derivatives show a wide range of biological effects, including anticancer, antiviral, tuberculostatic, anticonvulsant, immunosuppressive, anti-HIV, anti-SARS, and antithrombotic activities [6][7][8]. Since many isatin-based organic syntheses utilize nonpolar solvents, an understanding of isatin redox properties in organic solvents becomes particularly important.…”

Section: Introductionmentioning

confidence: 99%

Substituent and solvent dependence of the one-electron reduction of 5-substituted-N-methylisatins in aprotic solvents

Yeagley

Weigand-Heller

Hinds

et al. 2011

Journal of Electroanalytical Chemistry

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Towards the Design and Development of Agents with Broad Spectrum Chemotherapeutic Properties for the Effective Treatment of HIV / AIDS

Cited by 28 publications

References 55 publications

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

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

Synthesis, hematological, biochemical, and neurotoxicity screening of some Mannich base hydrochlorides

Substituent and solvent dependence of the one-electron reduction of 5-substituted-N-methylisatins in aprotic solvents

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