Article
Combination of non-natural D-amino acid derivatives and allophenylnorstatine-dimethylthioproline scaffold in HIV protease inhibitors have high efficacy in mutant HIV.
Journal of medicinal chemistry - 22 May 2008
Nakatani Shingo, Hidaka Koushi, Ami Ei'ichi, Nakahara Koichiro, Sato Akihiko, Nguyen Jeffrey-Tri, Hamada Yoshio, Hori Yasuko, Ohnishi Nobuyuki, Nagai Akinori, Kimura Tooru, Hayashi Yoshio, Kiso Yoshiaki
Abstract excerpt
Several non-natural D-amino acid derivatives were introduced as P2/P3 residues in allophenylnorstatine-containing (Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid) HIV protease inhibitors. The synthetic analogues exhibited potent inhibitory activity against HIV-1 protease enzyme and HIV-1 replication in MT-4 cells. Structure-activity relationships revealed that D-cysteine or serine derivatives contributed to...
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