Macrocyclic Polyamines

Developments in functionalization of macrocyclic polyamines

Pure and Applied Chemistry ◽

10.1351/pac198961050823 ◽

1989 ◽

Vol 61 (5) ◽

pp. 823-828 ◽

Cited By ~ 40

Author(s):

E. Kimura

Keyword(s):

Macrocyclic Polyamines

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Effective and reversible DNA condensation induced by bifunctional molecules containing macrocyclic polyamines and naphthyl moieties

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2011.11.069 ◽

2012 ◽

Vol 20 (2) ◽

pp. 801-808 ◽

Cited By ~ 21

Author(s):

Hao Yan ◽

Zhi-Fen Li ◽

Zhi-Fo Guo ◽

Zhong-Lin Lu ◽

Feng Wang ◽

...

Keyword(s):

Dna Condensation ◽

Bifunctional Molecules ◽

Macrocyclic Polyamines

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Dimeric Macrocyclic Polyamines with Potent Inhibitory Activity against Human Immunodeficiency Virus

Antiviral Chemistry and Chemotherapy ◽

10.1177/095632029500600508 ◽

1995 ◽

Vol 6 (5) ◽

pp. 337-344 ◽

Cited By ~ 20

Author(s):

Y. Inouye ◽

T. Kanamori ◽

M. Sugiyama ◽

T. Yoshida ◽

T. Koike ◽

...

Keyword(s):

Human Immunodeficiency Virus ◽

Cytopathic Effect ◽

Syncytium Formation ◽

Physiological Conditions ◽

Structure Activity ◽

Immunodeficiency Virus ◽

Macrocyclic Polyamines ◽

Anti Hiv ◽

Viral Cytopathic Effect ◽

Potent Inhibitory Activity

The structure-activity relationships of monomeric and dimeric macrocyclic polyamines were studied in an attempt to find potent inhibitors of human immunodeficiency virus (HIV) types 1 and 2. In general, dimeric polyamines are superior as HIV inhibitors to their monomeric counterparts, and the activity of a dimer is proportional to that of its constituent monomers. For the monomeric compounds, the amount of positive charge on the monomer rings under physiological conditions was more important for anti-HIV activity than the ring size. On the basis of these findings, the 14-membered tetraamine cyclam was selected as the component of dimeric compounds with potentially high activity. Of the series of newly synthesized bicyclams, in which the monomeric cyclams were linked at each C-6 position, a compound with an aIkyI chain bridge three carbons in length was found to exhibit the maximum anti-HIV activity. For one particular strain (HIV-2GH-1), syncytium formation was inhibited by the bicyclams at a similar concentration to that required to inhibit the viral cytopathic effect.

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