Dimeric Drugs

Abstract

This review intends to summarize the structures of an extensive number of symmetrical-dimeric drugs, having two monomers linked via a bridging entity while emphasizing the large versatility of biologically active substances reported to possess dimeric structures. The largest number of classes of these compounds consist 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-Parkisonians, 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 unexpected higher activity of the dimers vs. 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 number of articles summarized, and the large variety of substances mentioned, which display various biological activities, should be of interest to many academic and industrial medicinal chemists.

New Coumarin Derivatives Accessible in Short and Eco-Friendly Conditions with Antifungal Activity

“…This action was taken in the context of multivalent active compounds that are structures bearing at least two identic or different motifs. Becoming frequent within the field of drug discovery area, they are conceived to gain in synergy in terms of biological activity [32]. The newly synthesized compounds were tested for in vitro antifungal activity against A. niger, using a growth radial method in agar medium [33].…”

Unexpected Intermolecular C–H···O Hydrogen Bonds and 1H NMR Chemical Shifts in a Key Linker for Fluorine-18 Labeling of Dimeric Drugs

“…Notably, the resulting dimers of biologically active molecules often exhibit increased activity compared to their monomeric counterparts, presenting a potential avenue to enhance drug effectiveness, broaden the biological spectrum, overcome resistance, and improve pharmacological profiles. − Employing a bivalent ligand approach, these dimeric structures can also bridge independent recognition sites on transporters and foster favorable binding interactions . This innovative strategy offers the potential for therapeutics with stronger responses than monomeric drugs, providing a novel direction in drug development. ,,− …”

“…The synthesis of dimeric molecules has garnered significant attention over the past 2 decades. , This process, which involves the combination of two identical molecules through a suitable linker, emerges as a promising strategy for developing effective drugs. Notably, the resulting dimers of biologically active molecules often exhibit increased activity compared to their monomeric counterparts, presenting a potential avenue to enhance drug effectiveness, broaden the biological spectrum, overcome resistance, and improve pharmacological profiles. − Employing a bivalent ligand approach, these dimeric structures can also bridge independent recognition sites on transporters and foster favorable binding interactions .…”