2. Academic Validation
  3. Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2/P3 moieties

Synthesis and antiviral property of allophenylnorstatine-based HIV protease inhibitors incorporating D-cysteine derivatives as P2/P3 moieties

  • Bioorg Med Chem Lett. 2007 Aug 1;17(15):4213-7. doi: 10.1016/j.bmcl.2007.05.039.
Ei'ichi Ami 1,  Koichiro Nakahara,  Akihiko Sato,  Jeffrey-Tri Nguyen,  Koushi Hidaka,  Yoshio Hamada,  Shingo Nakatani,  Tooru Kimura,  Yoshio Hayashi,  Yoshiaki Kiso
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science and 21st Century COE Program, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.
PMID: 17537628 DOI: 10.1016/j.bmcl.2007.05.039
Abstract

We designed several HIV Protease Inhibitors with various d-cysteine derivatives as P(2)/P(3) moieties based on the structure of clinical drug candidate, KNI-764. Herein, we report their synthesis, HIV Protease inhibitory activity, HIV IIIB cell inhibitory activity, cellular toxicity, and inhibitory activity against drug-resistant HIV strains. KNI-1931 showed distinct selectivity against HIV proteases and high potency against drug-resistant strains, surpassing those of Ritonavir and Nelfinavir.

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