BMS-538203

BMS-538203 is a highly efficient HIV integrase inhibitor and antiviral agent.IC50 value:Target: HIV integraseIn the current study we demonstrate a hit-to-clinical candidate pathway that resulted in 50- and 2000-fold improvements in enzyme-inhibition and antiviral activity without an increase in molecular weight or change in molecular topology. The original hit , 1 (mw = 268) was optimized in a stepwise manner. Potential covalent protein-binding moieties were removed by reducing the number of the ketone groups. High enzyme inhibition activity was achieved by optimizing the aryl-portion of the molecule. Protein binding was reduced by replacing the standard amide by the corresponding methyl-hydroxamide. This eventually led to the discovery of BMS-538203 compound 2 (mw = 269) a highly efficient inhibitor and antiviral agent.

Signaling Pathways >> Metabolic Enzyme/Protease >> HIV Integrase

Signaling Pathways >> Anti-infection >> HIV

Research Areas >> Infection

[1]. Methods and compositions for treating hiv infection. RU patent 2367439.

[2]. Nowicka-Sans B, et al. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of theprodrug BMS-663068. Antimicrob Agents Chemother. 2012 Jul;56(7):3498-507.

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