Five groups of lexitropsin oligopeptides have been synthesized that are structurally related to the natural antiviral agents netropsin and distamycin and bearing two such moieties joined by flexible or rigid linkers. Inhibitory activity of these types of agents against murine leukemia retrovirus (MuLV) led to an evaluation of their inhibition of HIV-I in cell culture. The antiretroviral activity of the five different classes of lexitropsins is discussed in terms of their structural differences.
Intramolecular end-to-end excimer formation of bis[(1-pyrenylmethoxy)carbonyl]alkanes. A study of end-to-end collisional frequency on a chain molecule
作者:T. Kanaya、K. Goshiki、M. Yamamoto、Y. Nishijima
DOI:10.1021/ja00377a007
日期:1982.6
Template-controlled oligomerization support studies. Template synthesis and functionalization
作者:Ken S. Feldman、John S. Bobo、Susan M. Ensel、Yoon B. Lee、Paul H. Weinreb
DOI:10.1021/jo00289a019
日期:1990.1
US5616606A
申请人:——
公开号:US5616606A
公开(公告)日:1997-04-01
[EN] OLIGOPEPTIDE ANTIRETROVIRAL AGENTS
申请人:SYNPHAR LABORATORIES, INC.
公开号:WO1992013838A1
公开(公告)日:1992-08-20
(EN) Oligopeptide antiretroviral agents are represented by formula (I), wherein A is a moiety bearing a positive charge and of a size which avoids steric inhibition of binding of said compound to nucleic acid sequences associated with the cellular activity of retroviruses; R1 is a moiety derived from a dicarboxylic acid; Het is a five-membered heterocyclic moiety; y and z are independently 0, 1, 2 or 3; and x is 0 or 1. These compounds exhibit antiretroviral activity, especially against Human Immunodeficiency Virus (HIV).(FR) Cette invention concerne des agents antirétroviraux oligopeptidiques représentés par la formule (I), dans laquelle A représente une fraction portant une charge positive dont la taille permet d'éviter l'inhibition stérique de liaison dudit composé à des séquences d'acides nucléiques associées à l'activité cellulaire de rétrovirus; R1 représente une fraction dérivée d'un acide dicarboxylique; y et z représentent indépendamment 0, 1, 2, ou 3; et x est égal à 0 ou 1. Les composés présentent une activité antirétrovirale, plus particulièrement contre le virus de l'immunodéficience humaine (VIH).