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In psychology, concepts can be divided into two categories: natural and artificial. Natural concepts are formed through direct or indirect experiences. For example, consider the concept of snow. If you live in a place with regular snowfall, such as Essex Junction, Vermont, you know snow through direct experiences. You’ve seen it fall, touched it, shoveled it, and played in it. You recognize its texture, appearance, and even its smell. In contrast, if you live on an island like Saint...
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Implantation of the Syncardia Total Artificial Heart
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Artificial Macrocycles.

Eman M M Abdelraheem1,2, Shabnam Shaabani1, Alexander Dömling1

  • 1University of Groningen, Department of Drug Design, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands, a.s.s.domling@rug.nl.

Synlett : Accounts and Rapid Communications in Synthetic Organic Chemistry
|July 30, 2019
PubMed
Summary
This summary is machine-generated.

Artificial macrocycles offer improved drug-like properties and synthesizability compared to natural ones. Multicomponent reactions provide a versatile synthetic route to explore this novel chemical space for drug discovery.

Keywords:
bioactivitybioavailabilityconvergencedruglike propertiesmacrocyclemulticomponent reactionproperty spacesynthetic pathway

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Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis

Background:

  • Artificial macrocycles are emerging as a promising area in drug discovery.
  • They offer advantages over natural macrocycles, including enhanced synthesizability and tunable physicochemical properties for drug-like characteristics.
  • Accessing the diverse chemical space of large macrocycles efficiently remains a synthetic challenge.

Purpose of the Study:

  • To review multicomponent reactions (MCRs) as a key technology for synthesizing artificial macrocycles.
  • To highlight the application of MCRs in accessing diverse macrocyclic structures with potential biological activity.
  • To emphasize the importance of integrating structure-activity relationships into the design of synthetic macrocycles.

Main Methods:

  • Review of multicomponent reactions (MCRs) for macrocycle synthesis.
  • Focus on proprietary synthetic methodologies developed by the authors.
  • Analysis of structure-activity relationships in designed macrocycles.

Main Results:

  • MCRs enable convergent, rapid, and diverse access to artificial macrocycles.
  • Demonstration of MCRs' utility in generating novel macrocyclic scaffolds.
  • Exploration of the link between macrocycle structure and biological activity.

Conclusions:

  • Multicomponent reactions are a powerful tool for artificial macrocycle synthesis.
  • Synthetic chemists should prioritize structure-based design for optimized drug discovery outcomes.
  • Further exploration of MCRs will expand the accessible chemical space for novel therapeutics.