Multicomponent Reactions with Heterocycles: A Source of Novel Scaffolds for Antiparasitic and Antiviral Agents †
Department of Pharmacology, Toxicology and Therapeutical Chemistry, Faculty of Pharmacy, University of Barcelona, Barcelona Science Park, Baldiri Reixac 10-12, 08028 Barcelona, Spain
†
Presented at the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain, 8 September 2017.
Proceedings 2017, 1(6), 666; https://doi.org/10.3390/proceedings1060666
Published: 19 October 2017
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
We disclose a reaction discovery approach, based on novel multicomponent reactions (MCRs) upon heterocyclic substrates, especially azines, that yields a variety of scaffolds amenable to straightforward diversification. In just one step, we could jump from one generation of compounds to the next one by mere modification of the reagents. This feature greatly helps in the tuning of the biological properties and has allowed the formation of two classes of anti-infectious agents: antiparasitic and antiviral compounds. First, the silyl-promoted addition of isocyanides to azines yields pyridoimidazolium salts which are potent anti-trypanosoma agents. Next, we discuss the multiple multicomponent reaction approach on diaminodiazines using the Groebke–Blackburn–Bienaymé MCR as a source of new antiviral compounds, also featuring specific DNA affinity.
Details on the chemistry and biology related to these processes will be discussed.
Acknowledgments
This work was supported by DGICYT—Spain (project CTQ2015-67870-P) and Generalitat de Catalunya (2014 SGR 137).
Conflicts of Interest
The authors declare no conflict of interest.
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. |
© 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
Share and Cite
MDPI and ACS Style
Lavilla, R. Multicomponent Reactions with Heterocycles: A Source of Novel Scaffolds for Antiparasitic and Antiviral Agents. Proceedings 2017, 1, 666. https://doi.org/10.3390/proceedings1060666
AMA Style
Lavilla R. Multicomponent Reactions with Heterocycles: A Source of Novel Scaffolds for Antiparasitic and Antiviral Agents. Proceedings. 2017; 1(6):666. https://doi.org/10.3390/proceedings1060666
Chicago/Turabian StyleLavilla, Rodolfo. 2017. "Multicomponent Reactions with Heterocycles: A Source of Novel Scaffolds for Antiparasitic and Antiviral Agents" Proceedings 1, no. 6: 666. https://doi.org/10.3390/proceedings1060666
