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  • Title: Synthesis and antiviral activity of beta-carboline derivatives bearing a substituted carbohydrazide at C-3 against poliovirus and herpes simplex virus (HSV-1).
    Author: Nazari Formagio AS, Santos PR, Zanoli K, Ueda-Nakamura T, Düsman Tonin LT, Nakamura CV, Sarragiotto MH.
    Journal: Eur J Med Chem; 2009 Nov; 44(11):4695-701. PubMed ID: 19647908.
    Abstract:
    Several novel 1,3-disubstituted beta-carboline derivatives bearing a substituted carbohydrazide group at C-3 were synthesized and evaluated for their antiviral activity against vaccinal poliovirus (VP) and herpes simplex virus type 1 (HSV-1). The cytotoxicity and selectivity index of the active compounds were also evaluated. Among the synthesized derivatives, compounds 10 and 11 displayed potent activity against both vaccinal poliovirus and HSV-1 virus. Compound 10 presented the highest selectivity index (SI=2446.8) against HSV-1 virus and low cytotoxicity (CC(50)=1150.0+/-67.3 microM). The virus yield inhibition assay showed that compound 10 was able to inhibit HSV-1 plaque formation before and during the virus adsorption. The characteristic small plaque pattern observed in compound-treated cells suggested that compound 10 inhibited viral dissemination to neighboring cells. A computational study for prediction of ADME properties of the novel synthesized beta-carbolines derivatives was performed by determination of lipophilicity, topological polar surface area (TPSA), absorption (% ABS) and simple molecular descriptors, using Lipinski's rule.
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