KNI-102, a novel tripeptide HIV protease inhibitor containing allophenylnorstatine as a transition-state mimic

Article abstract of DOI:10.1248/cpb.39.3088

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.

Full text of DOI:10.1248/cpb.39.3088

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