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Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target-

Mechanism-

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication-

Inactive Indication

HIV Infections

Originator Organization

Rational Drug Design Laboratories

Active Organization-

Inactive Organization

Yamanouchi Pharmaceutical Co., Ltd.Rational Drug Design Laboratories

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

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-fluo-robenzyl)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 nonnucleoside 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.

100 Deals associated with RD6-Y664

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