172256-31-4Relevant academic research and scientific papers
Nonnucleoside HIV-1 reverse-transcriptase inhibitors, part 5.1) synthesis and anti-HIV-1 activity of novel 6-naphthylthio HEPT analogues
Sun, Guang-Fu,Chen, Xu-Xiang,Chen, Fen-Er,Wang, Yue-Ping,De Clercq, Erik,Balzarini, Jan,Pannecouque, Christophe
, p. 886 - 892 (2005)
As part of a series of studies to discover new HIV reverse-transcriptase inhibitors, various novel 6 α- and 6 β-naphthylthio 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio) thymine (HEPT) derivatives were synthesized, and in vitro anti-HIV-1 activity was evaluated. The results revealed that most of 6α-naphthylthio HEPT derivatives (7a - w) showed good activity [for 7e, IC50 value of 0.048 μM and selectivity index (SI) value of 735; for 7h, IC50 value of 0.057 μM and SI value of 579; for 7k, IC50 value of 0.063 μM and SI value of 565], 6 β-naphthylthio HEPT derivatives (8a - f) showed low activity, but the introduction of α nitro group to the C-1 position of the 6 β-naphthyl ring in the 6 β-naphthylthio series (11a - c) resulted in a dramatic increase in anti-HIV-1 activity.
Pyrimidine acyclonucleoside derivatives
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, (2008/06/13)
The present invention relates to novel pyrimidine acyclonucleoside derivatives represented by the following general formula (I), antiviral agents containing the derivatives as the active ingredients and processes of preparation thereof. STR1 wherein Rsup
A New Route to the Improved Synthesis of 1-(Alkoxymethyl)-5-alkyl- 6-(arylselenenyl)uracils
Lee, Namkyu,Kim, Young-Woo,Kim, Key H.,Kim, Dae-Kee
, p. 659 - 663 (2007/10/03)
A new route to C-6-selenenyl analogs of compound 1a from 5-alkyl-6-chlorouracils 6a-b has been described. A mild and highly efficient synthesis of 1-(alkoxymethyl)-5-alkyl-6-(arylselenenyl)uracils 8a-e has been accomplished from 6a-b in good yields using a two step procedure. Silylation of 5-alkyl-6-chlorouracils 6a-b using N,O-bis(trimethylsilyl)acetamide followed by regioselective alkylation of the silylated intermediate with ethyl or benzyl chloromethyl ether in dichloromethane afforded the desired 1-(alkoxymethyl)-5-alkyl-6-chlorouracils 7a-d in 88-94% yields. Compounds 7a-d readily underwent addition-elimination reaction with an appropriate arylselenol in the presence of ethanolic sodium hyroxide to produce the corresponding 1-(alkoxymethyl)-5-alkyl-6-(arylselenenyl)uracils 8a-e in excellent yields (94-99%).
