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ChemInform Abstract: 5-Alkyl-2-[(methylthiomethyl)thio]-6-(benzyl)-pyrimidin-4-(1H)-ones as Potent Non-Nucleoside Reverse Transcriptase Inhibitors of S-DABO Series.

✍ Scribed by R. VIG; C. MAO; T. K. VENKATACHALAM; L. TUEL-AHLGREN; E. A. SUDBECK; F. M. UCKUN

Publisher: John Wiley and Sons
Year: 2010
Weight: 33 KB
Volume: 29
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.199840161

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✦ Synopsis

5-Alkyl-2-[(methylthiomethyl)thio]-6-(benzyl)-pyrimidin-4-(1H)-ones as Potent Non-Nucleoside Reverse Transcriptase Inhibitors of S-DABO Series.

-Novel pyrimidinone derivatives (VII) (S-DABO) are synthesized and tested for their reverse transcriptase inhibitory activity as well as their anti-HIV activity. The computational approach allows the identification of ligand derivatization sites for the generation of more potent S-DABO derivatives. The lead S-DABO compound (VIIc) elicits potent anti-HIV activity (¿ 4-fold more active than AZT) and shows no detectable cytotoxicity. -(VIG,

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