Chemical Information

Biological Activity of BMS-538203

BMS-538203 is a  highly efficient HIV integrase inhibitor and antiviral agent.
IC50 value:
Target: HIV integrase
In 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.

References on BMS-538203

[1]. Methods and compositions for treating hiv infection. RU patent 2367439.
[2]. Optimization of compound efficiency in the context of discovering an amide ketoacid based HIV-integrase inhibitor with oral antiviral activity