Beyond Peptides and Peptidomimetics: Natural Heteroaromatic Amino Acids in the Synthesis of Fused Heterocyclic Frameworks for Bioactive Agents

Heterocycle cores are widely used in medicinal chemistry for developing bioactive compounds. In this scenario, using cheap and accessible starting material to build these heterocycles is desirable to obtain new drug candidates for cost-efficient processes. One easily accessible source of starting ma...

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Main Authors: Isis Apolo Silveira de Borba, Jamile Buligon Peripolli, Angélica Rocha Joaquim, Fernando Fumagalli
Format: Article
Language:English
Published: MDPI AG 2025-05-01
Series:Organics
Subjects:
Online Access:https://www.mdpi.com/2673-401X/6/2/23
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author Isis Apolo Silveira de Borba
Jamile Buligon Peripolli
Angélica Rocha Joaquim
Fernando Fumagalli
author_facet Isis Apolo Silveira de Borba
Jamile Buligon Peripolli
Angélica Rocha Joaquim
Fernando Fumagalli
author_sort Isis Apolo Silveira de Borba
collection DOAJ
description Heterocycle cores are widely used in medicinal chemistry for developing bioactive compounds. In this scenario, using cheap and accessible starting material to build these heterocycles is desirable to obtain new drug candidates for cost-efficient processes. One easily accessible source of starting material are amino acids. Usually, these compounds are employed in peptide synthesis, but their use for building heterocycle frameworks presents another appealing opportunity. Therefore, this review highlights the application of histidine and tryptophan, two heteroaromatic amino acids, in fused heterocyclic scaffold synthesis and their use in bioactive compounds.
format Article
id doaj-art-830c8dc82bfb42ec824ebb63cb798422
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publishDate 2025-05-01
publisher MDPI AG
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series Organics
spelling doaj-art-830c8dc82bfb42ec824ebb63cb7984222025-08-20T03:16:21ZengMDPI AGOrganics2673-401X2025-05-01622310.3390/org6020023Beyond Peptides and Peptidomimetics: Natural Heteroaromatic Amino Acids in the Synthesis of Fused Heterocyclic Frameworks for Bioactive AgentsIsis Apolo Silveira de Borba0Jamile Buligon Peripolli1Angélica Rocha Joaquim2Fernando Fumagalli3Pharmaceutical Sciences Graduate Program, Federal University of Santa Maria, Santa Maria 97105-900, RS, BrazilPharmacy Course, Federal University of Santa Maria, Santa Maria 97105-900, RS, BrazilDepartment of Pharmacy, Health Sciences Centre (DFI/CCS), Federal University of Santa Maria, Santa Maria 97105-900, RS, BrazilDepartment of Pharmacy, Health Sciences Centre (DFI/CCS), Federal University of Santa Maria, Santa Maria 97105-900, RS, BrazilHeterocycle cores are widely used in medicinal chemistry for developing bioactive compounds. In this scenario, using cheap and accessible starting material to build these heterocycles is desirable to obtain new drug candidates for cost-efficient processes. One easily accessible source of starting material are amino acids. Usually, these compounds are employed in peptide synthesis, but their use for building heterocycle frameworks presents another appealing opportunity. Therefore, this review highlights the application of histidine and tryptophan, two heteroaromatic amino acids, in fused heterocyclic scaffold synthesis and their use in bioactive compounds.https://www.mdpi.com/2673-401X/6/2/23histidinetryptophanmedicinal chemistryheterocyclic core
spellingShingle Isis Apolo Silveira de Borba
Jamile Buligon Peripolli
Angélica Rocha Joaquim
Fernando Fumagalli
Beyond Peptides and Peptidomimetics: Natural Heteroaromatic Amino Acids in the Synthesis of Fused Heterocyclic Frameworks for Bioactive Agents
Organics
histidine
tryptophan
medicinal chemistry
heterocyclic core
title Beyond Peptides and Peptidomimetics: Natural Heteroaromatic Amino Acids in the Synthesis of Fused Heterocyclic Frameworks for Bioactive Agents
title_full Beyond Peptides and Peptidomimetics: Natural Heteroaromatic Amino Acids in the Synthesis of Fused Heterocyclic Frameworks for Bioactive Agents
title_fullStr Beyond Peptides and Peptidomimetics: Natural Heteroaromatic Amino Acids in the Synthesis of Fused Heterocyclic Frameworks for Bioactive Agents
title_full_unstemmed Beyond Peptides and Peptidomimetics: Natural Heteroaromatic Amino Acids in the Synthesis of Fused Heterocyclic Frameworks for Bioactive Agents
title_short Beyond Peptides and Peptidomimetics: Natural Heteroaromatic Amino Acids in the Synthesis of Fused Heterocyclic Frameworks for Bioactive Agents
title_sort beyond peptides and peptidomimetics natural heteroaromatic amino acids in the synthesis of fused heterocyclic frameworks for bioactive agents
topic histidine
tryptophan
medicinal chemistry
heterocyclic core
url https://www.mdpi.com/2673-401X/6/2/23
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