Delving into the Latest Updates on KNI-102 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

KNI-102

Target

HIV-1 protease

Mechanism

HIV-1 protease inhibitors(HIV protease inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication-

Inactive Indication

HIV Infections

Originator Organization

Japan Energy, Inc.

Active Organization-

Inactive Organization

Japan Energy, Inc.

Drug Highest PhaseDiscontinuedDiscovery

First Approval Date-

Regulation-

Some dipeptide-type human immunodeficiency virus (HIV) protease inhibitors derived from KNI-102, with a N-carbomethoxycarbonylprolyl-phenylalanine benzyl ester (CPF) moiety as a binding site to gp120, were synthesized. Compounds 11a showed 7--100 times higher HIV protease-inhibitory activity (11a; IC50 = 0.90 microgram/ml, 1.1 microM) than the standard compound 3 or 4 (3; IC50 = 3.7 micrograms/ml, 7.7 microM, 4; IC50 = 75 micrograms/ml, 155 microM). Generally, the compounds substituted at the o-position of the phenoxyacetyl group 7a, 11a, 16a and 21a showed several times higher inhibitory activity than 3.

01 Jan 1991·Chemical & pharmaceutical bulletinQ4 · MEDICINE

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

Q4 · MEDICINE

Article

Author: Akaji, Kenichi ; Imai, Junya ; Tanaka, Shigeki ; Hattori, Naoko ; Mimoto, Tsutomu ; Kisanuki, Sumitsugu ; Kiso, Yoshiaki

HIV-1 protease inhibitors containing allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid]-Pro (syn diastereomer) as a transition-state mimic were established to be potent and highly selective. Z-Asn-Apns-Pro-NHBut (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.

100 Deals associated with KNI-102

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