Advances in Spiro Compounds

Dear Colleagues,

Spiro compounds (also named as spiranes following the suggestion of Adolf von Baeyer as early as 1900) are ubiquitous molecules, which contain a fused bicyclic system that share a single atom. A search for the key term “spiro” in the SciFinder database at the beginning of April 2017 resulted in more than 147,000 hits including 5000–6000 publications per annum after 2010. This enormous research activity encompasses a large number of fields in chemistry (especially organic and medicinal chemistry—with an emphasis on heterocyclic systems), but also includes pharmacology, crystallography, materials science, physics, biochemistry, molecular biology, engineering, energy and fuels, just to mention the most active areas. The immense interest in spirocycles, besides their unique features related to isolation from natural sources, synthesis and stereochemistry, is fuelled by an extremely wide range of useful properties, that comprise among others anti-cancer, antibacterial, antifungal, anti-diabetic, anti-HIV, cytotoxic, diuretic, spasmolytic, antiphlogistic, anti-hypertensive, anti-depressant, anxiolytic, anti-fouling, anti-feedant, herbicidal, plant growth regulatory effects; photochromism; and hole-transporting ability.

These properties have been translated into several practical applications which include marketed drugs; ophtalmic lenses and sunscreening (for instance in sunglasses); auxiliary compounds in stereoselective syntheses; electronic displays and optical data storage devices, etc. In addition, many other utilizations, such as new medications, chemical biosensing, controlled release drug delivery, molecular switches, and solar cells, are in a developmental phase.

With regard to pharmaceutical applications, it should also be mentioned that at the current time, driven by the ever-increasing pace of drug discovery, medicinal chemists are turning to new unexplored regions of chemical space in the quest to find more potent medicines. Thus, unusual strained spirocyclic bioisosteres are important targets, as they show diverse new biological activities. Moreover, besides potentially modulating binding potency and specificity, spirocyclic scaffolds may also improve bioavailability and metabolic stability, key issues when developing new pharmacological entities.

This forthcoming Special Issue of Molecules entitled “Advances in Spiro Compounds“ will be devoted to this amazing class of compounds, covering recent key findings in any of the above research fields.

Prof. Dr. László Somsák
Prof. Dr. Anthony J. Burke
Guest Editors

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