29816-01-1Relevant articles and documents
DIPEPTIDE LINKED MEDICINAL AGENTS
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Paragraph 0814, (2016/07/05)
A non-enzymatically self cleaving dipeptide element is provided that can be linked to known medicinal agents via an amide bond. The dipeptide will spontaneously be cleaved from the medicinal agent under physiological conditions through a reaction driven by chemical instability. Accordingly, the dipeptide element provides a means of linking various compounds to known medicinal agents wherein the compounds are subsequently released from the medicinal agent after a predetermined time of exposure to physiological conditions. For example, the dipeptide can be linked to an active site of a drug to form a prodrug and/or the dipeptide may comprise a depot polymer to sequester an injectable composition comprising the complex at the point of administration.
Synthesis and Activity of New Epipolythiopiperazine-2,5-dione Compounds. I
Jiang, Hui,Newcombe, Nicole,Sutton, Philip,Lin, Qing Hui,Muellbacher, Arno,Waring, Paul
, p. 1743 - 1754 (2007/10/02)
The new lipophilic epipolythiopiperazine-2,5-diones 1,4-dibutylepidithiopiperazine-2,5-dione, 1,4-dibenzylepidithiopiperazine-2,5-dione, 1-benzyl-4-methylepidithiopiperazine-2,5-dione and 3,3'-dithiobis(1,4-dimethylpiperazine-2,5-dione) were synthesized.Unlike the parent compound, the fungal toxin and immunomodulating agent gliotoxin, these compounds did not affect macrophage adherence and cell proliferation in vitro.Like the reduced form of gliotoxin and other simple analogues, these new compounds induce oxidative damage to naked DNA.We conclude that an increase in lipophilicity plays no part in the biological activity of these compounds and in fact abrogates almost all activity.We also synthesized an intermolecular disulfide analogue which also lacked activity.