Publication: Synthesis and HIV-1 reverse transcriptase inhibitory activity of non-nucleoside phthalimide derivatives
Issued Date
2008-02-01
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ISSN
1001604X
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2-s2.0-39749086177
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Mahidol University
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SCOPUS
Bibliographic Citation
Chinese Journal of Chemistry. Vol.26, No.2 (2008), 379-387
Suggested Citation
Jiraporn Ungwitayatorn, Chanpen Wiwat, Chutima Matayatsuk, Jutarat Pimthon, Suratsawadee Piyaviriyakul Synthesis and HIV-1 reverse transcriptase inhibitory activity of non-nucleoside phthalimide derivatives. Chinese Journal of Chemistry. Vol.26, No.2 (2008), 379-387. doi:10.1002/cjoc.200890073 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/19092
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Title
Synthesis and HIV-1 reverse transcriptase inhibitory activity of non-nucleoside phthalimide derivatives
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Abstract
A new type of non-nucleoside HIV-1 reverse transcriptase inhibitors in phthalimide series has been synthesized from either the reaction of N-carboethoxyphthalimide with amines or phthalimide with appropriate alkyl halides. The in vitro inhibitory activity of the synthesized compounds was studied by a radiometric assay at a concentration of 200 μg/mL using poly(rA)·oligo(dT) as a template-primer and methyl-[3H]dTTP as a substrate. The three most potent compounds, N-(m,p-dihydroxybenayl) phihalimide (11), N-[2-(a-furyl)ethyl]phthalimide (29) and N-(5-methylpyrazin-2- ylmethyl)phthalimide (25) exhibited IC50 values of 60.90, 98.10 and 120.75 μ/mL, respectively, lower than IC50 of delavirdine (502.22 μg/mL, using poly(rA)·oligo(dT) as a template-primer and [ 3H]dTTP as a substrate). © 2008 SIOC, CAS, & Wiley-VCH Verlag GmbH & Co. KGaA.
