Mimoto T, Imai J, Kisanuki S, Enomoto H, Hattori N, Akaji K, Kiso Y
Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Japan.
Chem Pharm Bull (Tokyo). 1992 Aug;40(8):2251-3. doi: 10.1248/cpb.40.2251.
Selective and potent HIV protease inhibitors containing allophenylnorstatine [Apns; (2S, 3S)-3-amino-2-hydroxy-4-phenylbutyric acid] as a transition-state mimic were designed and synthesized. Among them, conformationally constrained tripeptide derivatives, kynostatin (KNI)-227 and -272 (Fig. 1), exhibited highly potent antiviral activities against a wide spectrum of HIV isolates. Ready availability due to the simple synthetic procedure and the excellent antiviral properties indicate that KNI-227 and KNI-272 are promising candidates as selective anti-AIDS drugs.
设计并合成了含有别苯基去甲他汀[Apns；(2S, 3S)-3-氨基-2-羟基-4-苯基丁酸]作为过渡态模拟物的选择性强效HIV蛋白酶抑制剂。其中，构象受限的三肽衍生物，抑抑素（KNI）-227和-272（图1），对多种HIV分离株表现出高效的抗病毒活性。由于合成步骤简单且具有出色的抗病毒特性，KNI-227和KNI-272易于获得，这表明它们是有前景的选择性抗艾滋病药物候选物。
