Chemical and Pharmaceutical Bulletin p. 3088 - 3088 (1991)
Update date:2022-08-17
Topics:
Mimoto
Imai
Tanaka
Hattori
Kisanuki
Akaji
Kiso
HIV-1 protease inhibitors containing allophenylnorstatine (Apns; (2S,3S)-3-amino-2-hydroxy-4-phenyl-butyric acid]-Pro (syn distereomer) as a transition-state mimic were established to be potent and highly selective. Z-Asn-Apns-Pro-NHBu(t) (KNI-102) is the only tripeptide exhibiting substantial anti-HIV activity and may be of minimum size for potent, selective inhibition of HIV protease. Ready availability due to its simple chemical structure and stability should make it valuable for studies of the development of metabolically stable anti-AIDS drugs.
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(1950)