Synthesis and HIV-1 Reverse Transcriptase Inhibitory Activity of Non-Nucleoside Phthalimide Derivatives

Autor:	Jutarat Pimthon, Jiraporn Ungwitayatorn, Chutima Matayatsuk, Chanpen Wiwat, Suratsawadee Piyaviriyakul
Rok vydání:	2008
Předmět:	chemistry.chemical_classification Stereochemistry Substrate (chemistry) General Chemistry In vitro Reverse transcriptase Phthalimide chemistry.chemical_compound chemistry medicine Delavirdine Nucleoside IC50 Alkyl medicine.drug
Zdroj:	Chinese Journal of Chemistry. 26:379-387
ISSN:	1614-7065 1001-604X
DOI:	10.1002/cjoc.200890073
Popis:	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-dihydroxybenzyl)phthalimide (11), N-[2-(α-furyl)ethyl]phthalimide (29) and N-(5-methylpyrazin-2-ylmethyl)phthalimide (25) exhibited IC50 values of 60.90, 98.10 and 120.75 µg/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).
Databáze:	OpenAIRE
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