Inhibition of human immunodeficiency virus replication by RD6-Y664, a novel benzylhydroxylamine derivative

M. Okamoto, M. Fujiwara, E. Kodama, O. Yamamoto, S. Shigeta, H. Mitsuya, K. Konno, T. Yokota, M. Baba

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8 Citations (Scopus)


We have examined novel benzylhydroxylamine derivatives for their inhibitory effects on the replication of human immunodeficiency virus (HIV) in cell cultures. Among the series, O-(2-chloro-6-fluorobenzyl)hydroxylamine (RD6-Y664) was found to be the most potent inhibitor of HIV-1. The EC50 for HIV-1 strain IIIB was 1.6 μg/ml with a selectivity index greater than 38 in MT-4 cells. It also inhibited the replication of other HIV strains including a non-nucleoside reverse transcriptase (RT) inhibitor-resistant mutant, a nucleoside RT inhibitor-resistant mutant and HIV-2, in acutely infected cells. However, the compound did not affect HIV-1 production in chronically infected cells. A time-of-addition experiment and detection of proviral DNA synthesis suggested that RD6-Y664 targeted an early step of the viral replication cycle, presumably a process prior to reverse transcription. In fact, an assay for HIV-1 RT revealed that the compound did not suppress enzyme activity. Furthermore, RD6-Y664 did not show any inhibition of gp120-CD4 interaction, or binding of anti-CXCR4 antibody to CXCR4.

Original languageEnglish
Pages (from-to)71-77
Number of pages7
JournalAntiviral Chemistry and Chemotherapy
Issue number2
Publication statusPublished - 1999 Mar


  • Anti-HIV-1 activity
  • Benzylhydroxylamine
  • Structure-activity relationship


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