Title:Dimeric Drugs
Volume: 29
Issue: 16
Author(s): Abraham Nudelman*
Affiliation:
- Chemistry Department, Bar Ilan University, Ramat Gan 52900, Israel
Keywords:
Monomeric drugs, dimeric drugs, symmetry linking bridges, synergy, biological activity, industrial medicinal chemists.
Abstract: This review intends to summarize the structures of an extensive number of
symmetrical-dimeric drugs, having two monomers, linked via a bridging entity emphasizing
the versatility of biologically active substances reported to possess dimeric structures.
The major number of these compounds consists of anticancer agents, antibiotics/
antimicrobials, and anti-AIDS drugs. Other symmetrical-dimeric drugs include antidiabetics,
antidepressants, analgesics, anti-inflammatories, drugs for the treatment of Alzheimer’s
disease, anticholesterolemics, estrogenics, antioxidants, enzyme inhibitors, anti-
Parkinsonians, laxatives, antiallergy compounds, cannabinoids, etc. Most of the articles
reviewed do not compare the activity/potency of the dimers to that of their corresponding
monomers. Only in limited cases, various suggestions have been made to justify the unexpectedly
higher activity of the dimers vs. that of the corresponding monomers. These
suggestions include statistical effects, the presence of dimeric receptors, binding of a dimer
to two receptors simultaneously, and others. It is virtually impossible to predict
which dimers will be preferable to their respective monomers, or which linking bridges
will lead to the most active compounds. It is expected that the extensive variety of substances
mentioned, and the assortment of their biological activities should be of interest to
academic and industrial medicinal chemists.
