Analog Design

Cannon, Joseph G.

doi:10.1002/0471266949.bmc031

Cited by 4 publications

(1 citation statement)

References 56 publications

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“…Bioisosteres are defined as groups or molecules that have chemical and physical properties conferring broadly similar biological properties [38]. In this study, the bio-isosteric replacement of NH for O resulted in amide derivatives of BA and betulin.…”

Section: Bio-isosteric Substitution At C-3mentioning

confidence: 99%

The discovery of a class of novel HIV-1 maturation inhibitors and their potential in the therapy of HIV

Yu¹,

Wild²,

Martin

et al. 2005

Expert Opinion on Investigational Drugs

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Although HIV infection is now primarily treated with reverse transcriptase and protease inhibitors, HIV therapy must look toward new drugs with novel mechanism(s) of action to both improve efficacy and address the growing problem of drug resistance. Using natural products as a source of biologically active compounds, our drug discovery program has successfully optimised the natural product betulinic acid to the first-in-class maturation inhibitor 3-O-(3',3'-dimethylsuccinyl)-betulinic acid (DSB). DSB's unique viral target has been identified as a late step in Gag processing. Specifically, it inhibits the cleavage of the capsid precursor, CA-SP1, resulting in a block to the processing of mature capsid protein leading to a defect in viral core condensation. DSB represents a unique class of anti-HIV compounds that inhibit virus maturation and provide additional opportunities for anti-HIV therapy. In this review, the discovery of DSB and its mode of action are summarised. Anti-AIDS Agents part 64. For part 63 in the series, see YU D, LEE KH: Recent progress and prospects on plant-derived anti-HIV agents and analogs. In: Medicinal Chemistry of Bioactive Natural Products. XT Liang, WS Fang (Eds), Wiley, New York, USA (2005) (In Press).

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Section: Bio-isosteric Substitution At C-3mentioning

confidence: 99%