2. Academic Validation
  3. Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions

Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions

  • J Med Chem. 2003 Sep 25;46(20):4236-9. doi: 10.1021/jm034082o.
Tao Wang 1,  Zhongxing Zhang,  Owen B Wallace,  Milind Deshpande,  Haiquan Fang,  Zheng Yang,  Lisa M Zadjura,  Donald L Tweedie,  Stella Huang,  Fang Zhao,  Sunanda Ranadive,  Brett S Robinson,  Yi-Fei Gong,  Keith Ricarrdi,  Timothy P Spicer,  Carol Deminie,  Ronald Rose,  Hwei-Gene Heidi Wang,  Wade S Blair,  Pei-Yong Shi,  Pin-Fang Lin,  Richard J Colonno,  Nicholas A Meanwell
Affiliations

Affiliation

  • 1 Department of Discovery Chemistry, The Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA.
PMID: 13678401 DOI: 10.1021/jm034082o
Abstract

Indole derivative 1 interferes with the interaction of the HIV surface protein gp120 with the host cell receptor CD4. The 4-fluoro derivative 2 exhibited markedly enhanced potency and was bioavailable in the rat, dog, and cynomolgus monkey when administered orally as a solution formulation. However, aqueous suspensions of 2 were poorly bioavailable, indicative of dissolution-limited absorption. The 7-azaindole derivative 3, BMS-378806, exhibited improved pharmaceutical properties while retaining the HIV-1 inhibitory profile of 2.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-14134
    98.94%, HIV抑制剂
    HIV
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