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. 1999 Jun;43(6):1487-90.
doi: 10.1128/AAC.43.6.1487.

In vitro anti-human immunodeficiency virus activities of Z- and E-methylenecyclopropane nucleoside analogues and their phosphoro-L-alaninate diesters

H Uchida  1 , E N Kodama, K Yoshimura, Y Maeda, P Kosalaraksa, V Maroun, Y L Qiu, J Zemlicka, H Mitsuya
Affiliations

In vitro anti-human immunodeficiency virus activities of Z- and E-methylenecyclopropane nucleoside analogues and their phosphoro-L-alaninate diesters

H Uchida et al. Antimicrob Agents Chemother. 1999 Jun.

Abstract

Nucleoside analogues with a Z- or an E-methylenecyclopropane moiety were synthesized and examined for activity against human immunodeficiency virus type 1 (HIV-1) in vitro. The addition of a methyl phenyl phosphoro-L-alaninate moiety to modestly active analogues resulted in potentiation of their anti-HIV-1 activity. Two such compounds, designated QYL-685 (with 2,6-diaminopurine) and QYL-609 (with adenine), were most potent against HIV-1 in vitro, with 50% inhibitory concentrations of 0.034 and 0.0026 microM, respectively, in MT-2 cell-based assays. Both compounds were active against zidovudine-resistant, didanosine-resistant, and multi-dideoxynucleoside-resistant infectious clones in vitro. Further development of these analogues as potential therapies for HIV-1 infection is warranted.

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Figures

FIG. 1
FIG. 1
Structures of various QYL compounds with or without the PPA moiety.
See this image and copyright information in PMC

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