2. Academic Validation
  3. Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 13. Synthesis and profiling of a novel amminium prodrug of the HIV-1 attachment inhibitor BMS-585248

Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 13. Synthesis and profiling of a novel amminium prodrug of the HIV-1 attachment inhibitor BMS-585248

  • J Med Chem. 2013 Feb 28;56(4):1670-6. doi: 10.1021/jm301638a.
Alicia Regueiro-Ren 1,  Jean Simmermacher-Mayer,  Michael Sinz,  Kim A Johnson,  Xiaohua Stella Huang,  Susan Jenkins,  Dawn Parker,  Sandhya Rahematpura,  Ming Zheng,  Nicholas A Meanwell,  John F Kadow
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, Connecticut 06492, United States. alicia.regueiroren@bms.com
PMID: 23374053 DOI: 10.1021/jm301638a
Abstract

In vitro studies suggested that the ammonium salt 2 could be a viable prodrug of the HIV-1 attachment inhibitor 1. Increased systemic exposure of the parent drug 1 following oral administration of the amminium salt 2 when compared to similar studies using solution dosing of the parent compound was observed in the in vivo studies in both rats and dogs. At high doses, the improvement in oral exposure of the parent drug was even more evident, indicating that the increased solubility of the amminium salt 2 can overcome dissolution-limited absorption and demonstrating the potential utility of this compound as a prodrug of 1.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-13829
    HIV-1附着抑制剂
    HIV
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