Relevância dos compostos heterocíclicos à química medicinal e saúde humana
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May 30, 2025
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Resumo
Objetivo: Sintetizar evidências científicas visando apontar a relevância dos compostos heterocíclicos à química medicinal e saúde humana. Revisão Bibliográfica: Os compostos heterocíclicos são caracterizados pela presença de anel fechado contendo um ou mais átomos diferentes de carbono. Esses compostos têm ganhado significativa atenção devido à grande versatilidade de uso no contexto da saúde. Diversas biomoléculas naturais ou sintéticas são constituídas por anéis heterocíclicos, tais como a molécula de DNA, o ATP, antibióticos utilizados em infecções de importância clínica, a cafeína, anticoagulantes como a varfarina e diversos outros compostos capazes de curar ou melhorar a qualidade de vida dos seres humanos. O interesse da pesquisa relacionada a esses compostos está aumentando rapidamente, devido aos avanços em metodologias sintéticas e a sua versatilidade na interação com alvos biológicos. Na presente revisão, relata-se os recentes avanços de derivados heterocíclicos, como os derivados de piridina, tiofeno, pirrol, cumarinas, furano, quinolina e outros, no desenvolvimento de anti-inflamatórios, anticancerígenos, antibióticos, antifúngicos e outros. Considerações Finais: A pesquisa contínua relacionada à síntese de novas substâncias derivadas de compostos heterocíclicos é essencial para redução da morbi-mortalidade de diversas doenças que afligem a sociedade.
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Como Citar
LealM. M. F. V., MarquesD. S. C., Cruz FilhoI. J. da, GaiãoW. D. C., Silva JúniorJ. J. da, MachadoD. C., RodriguesC. G., & LimaM. do C. A. de. (2025). Relevância dos compostos heterocíclicos à química medicinal e saúde humana. Revista Eletrônica Acervo Saúde, 25(5), e20249. https://doi.org/10.25248/reas.e20249.2025
Seção
Revisão Bibliográfica
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Referências
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15. GABRIEL I. ‘Acridines’ as New Horizons in Antifungal Treatment. Molecules. 2020; 25(7): 1480.
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17. JÓŹWIAK M, et al. Anticancer activities of fatty acids and their heterocyclic derivatives. Eur J Pharmacol. 2020; 871: 172937.0,
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21. LING Y, et al. The Expanding Role of Pyridine and Dihydropyridine Scaffolds in Drug Design. Drug Des Devel Ther. 2021; 15: 4289-4338.
22. LIU H, et al. Synthesis, preliminary structure-activity relationships, and in vitro biological evaluation of 6-aryl-3-amino-thieno[2,3-b]pyridine derivatives as potential anti-inflammatory agents. Bioorg Med Chem Lett. 2013; 23(8): 2349-52.
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26. MONTAGUT-ROMANS A, et al. Synthesis and Biological Evaluation of C-3 Aliphatic Coumarins as Vitamin K Antagonists. Bioorg. Med. Chem. Lett. 2017, 27 (7): 1598–1601.
27. MU JX, et al. Microwave assisted synthesis, antifungal activity, DFT and SAR study of 1,2,4-triazolo[4,3-a]pyridine derivatives containing hydrazone moieties. Chem Cent J. 2016; 10: 50.
28. MUSTAFA YF. Synthesis, characterization and antibacterial activity of novel heterocycle, coumacine, and two of its derivatives. Saudi Pharm J. 2018; 26(6): 870-875.
29. NASCIMENTO PH, et al. Preliminary evaluation of the interaction with Albumin/DNA and in vitro evaluation of the antioxidant properties promoted by thiosemicarbazones and thiazole compounds. Sci. Electronic Arch. 2024; 17(3).
30. PADMANABHAN P, et al. Antiviral activity of Thiosemicarbazones derived from α-amino acids against Dengue virus. J Med Virol. 2017; 89(3): 546-552.
31. PIBIRI I. Recent Advances: Heterocycles in Drugs and Drug Discovery. International Journal of Molecular Sciences. 2024; 25(17): 9503–3.
32. REISER O. Heterocyclic Chemistry – A Mature Area in Its Infancy! European Journal of Organic Chemistry. 2019; 019(31-32): 4973–5.
33. SAHU R, et al. Pyridine Moiety: Recent Advances in Cancer Treatment. Indian Journal of Pharmaceutical Sciences. 2022; 22(2): 248-272.
34. SELIEM IA, et al. New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2. Bioorganic Chemistry. 2021; 114: 105117.
35. SILVA AR. Síntese, caracterização e atividades biológicas de 1, 2, 4-oxadiazóis. Trabalho de Conclusão de Curso (Licenciatura em Química) - Departamento de Química, Universidade Federal Rural de Pernambuco, Recife, 2020.
36. SOUZA LG, et al. Coumarins as cholinesterase inhibitors: A review. Chemico-Biological Interactions. 2016;254: 11–23.
37. VILKOVÁ M, et al. Acridine Based N-Acylhydrazone Derivatives as Potential Anticancer Agents: Synthesis, Characterization and ctDNA/HSA Spectroscopic Binding Properties. Molecules. 2022; 27(9): 2883.
38. VITAKU E, et al. Analysis of the structural diversity, substitution patterns, and frequency of nitrogen heterocycles among U.S. FDA approved pharmaceuticals. J Med Chem. 2014; 57(24): 10257-74.
39. WEI L, et al. Synthesis, Characterization, and Antifungal Activity of Schiff Bases of Inulin Bearing Pyridine ring. Polymers (Basel). 2019; 11(2): 371.
2. AHMED EY, et al. VEGFR-2 inhibiting effect and molecular modeling of newly synthesized coumarin derivatives as anti-breast cancer agents. Bioorganic & Medicinal Chemistry. 2020; 28(5): 115328.
3. AL-MULLA A. A review: biological importance of heterocyclic compounds. Der Pharma Chemica, 2017; 9(13): 141-147.
4. AL-WARHI T, et al. Recent advancements of coumarin-based anticancer agents: An up-to-date review. Bioorganic Chemistry. 2020; 103: 104163.
5. ALMUTAIRI FM, et al. Synthesis, Molecular Docking, c-Met Inhibitions of 2,2,2-Trichloroethylidene- cyclohexane-1, 3-dione Derivatives Together with their Application as Target SARS-CoV-2 main Protease (Mpro) and as Potential anti-COVID-19. Comb Chem High Throughput Screen. 2023; 26(7): 1437-1449.
6. ARASTEHFAR A, et al. Antifungal susceptibility, genotyping, resistance mechanism, and clinical profile of Candida tropicalis blood isolates. Med Mycol. 2020; 58(6): 766-773.
7. AUTI PB, BOTHARA KG. Diverse Heterocyclic Ring Systems: Innovative Advances in Medicinal Chemistry. Mini Rev Med Chem. 2021; 21(2): 134.
8. BANSAL, RK. Heterocyclic Chemistry. 5th ed. New Age International Publisher, 2014, 572p.
9. DE FARIA, R. et al. Perfil de resistência à antimicrobianos da classe dos Beta-lactâmicos e Aminoglicosídeos em cepas de Escherichia coli isoladas entre janeiro de 2015 e dezembro de 2018 / Antimicrobial resistance profile of the Beta-lactams and Aminoglycosides class in Escherichia coli strains isolated between january 2015 and december 2018. Braz. J. Develop. 2022; 8(7): 51673-91
10. DE S, et al. Pyridine: the scaffolds with significant clinical diversity. RSC Advances. 2022; 12(24): 15385–406.
11. EL-SHANBAKY H, et al. Synthesis of Heterocyclic and Non-heterocyclic Compounds Derived from Novel 2-Furanones and Evaluation of their Anti-viral Activity. Journal of Advanced Pharmacy Research, 2021; 5(1): 202-210.
12. FERREIRA MVC, et al. Penicilina: oitenta anos. Rev Med (São Paulo). 2008; 87(4): 272-6.
13. FRANCO DP, et al. A importância das cumarinas para a química medicinal e o desenvolvimento de compostos bioativos nos últimos anos. Quím Nova. 2021; 44(2): 180–97..
14. FUKUSHIMA AR, et al. Da química medicinal aos anticorpos monoclonais, como a bioinformática poderá revolucionar a indústria farmacêutica?. BWSJ. 2022; 5:1-7.
15. GABRIEL I. ‘Acridines’ as New Horizons in Antifungal Treatment. Molecules. 2020; 25(7): 1480.
16. JAMPILEK J. Heterocycles in Medicinal Chemistry. Molecules. 2019; 24(21): 3839.
17. JÓŹWIAK M, et al. Anticancer activities of fatty acids and their heterocyclic derivatives. Eur J Pharmacol. 2020; 871: 172937.0,
18. KABIR E, UZZAMAN M. A review on biological and medicinal impact of heterocyclic compounds. Results in Chemistry. 2022;4: 100606.
19. KAUSAR S, et al. A review: Mechanism of action of antiviral drugs. International Journal of Immunopathology and Pharmacology. 2021;35.
20. KIM S, et al. PubChem 2025 update. Nucleic Acids Res. 2025; 53(D1): D1516-D1525.
21. LING Y, et al. The Expanding Role of Pyridine and Dihydropyridine Scaffolds in Drug Design. Drug Des Devel Ther. 2021; 15: 4289-4338.
22. LIU H, et al. Synthesis, preliminary structure-activity relationships, and in vitro biological evaluation of 6-aryl-3-amino-thieno[2,3-b]pyridine derivatives as potential anti-inflammatory agents. Bioorg Med Chem Lett. 2013; 23(8): 2349-52.
23. MATHEW B. SAR Analysis of Various Heterocyclic Compounds in Medicinal Chemistry: Recent Updates-Part-I. Curr Top Med Chem. 2021; 21(30): 2694.
24. MELO MC, et al. Inhibition of the hemolytic activity caused by Staphylococcus aureus alpha-hemolysin through isatin-Schiff copper(II) complexes. FEMS microbiology letters. 2016; 363(1): fnv207.
25. MERMER A, et al. Recent studies of nitrogen containing heterocyclic compounds as novel antiviral agents: A review. Bioorg Chem. 2021;114: 105076.
26. MONTAGUT-ROMANS A, et al. Synthesis and Biological Evaluation of C-3 Aliphatic Coumarins as Vitamin K Antagonists. Bioorg. Med. Chem. Lett. 2017, 27 (7): 1598–1601.
27. MU JX, et al. Microwave assisted synthesis, antifungal activity, DFT and SAR study of 1,2,4-triazolo[4,3-a]pyridine derivatives containing hydrazone moieties. Chem Cent J. 2016; 10: 50.
28. MUSTAFA YF. Synthesis, characterization and antibacterial activity of novel heterocycle, coumacine, and two of its derivatives. Saudi Pharm J. 2018; 26(6): 870-875.
29. NASCIMENTO PH, et al. Preliminary evaluation of the interaction with Albumin/DNA and in vitro evaluation of the antioxidant properties promoted by thiosemicarbazones and thiazole compounds. Sci. Electronic Arch. 2024; 17(3).
30. PADMANABHAN P, et al. Antiviral activity of Thiosemicarbazones derived from α-amino acids against Dengue virus. J Med Virol. 2017; 89(3): 546-552.
31. PIBIRI I. Recent Advances: Heterocycles in Drugs and Drug Discovery. International Journal of Molecular Sciences. 2024; 25(17): 9503–3.
32. REISER O. Heterocyclic Chemistry – A Mature Area in Its Infancy! European Journal of Organic Chemistry. 2019; 019(31-32): 4973–5.
33. SAHU R, et al. Pyridine Moiety: Recent Advances in Cancer Treatment. Indian Journal of Pharmaceutical Sciences. 2022; 22(2): 248-272.
34. SELIEM IA, et al. New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2. Bioorganic Chemistry. 2021; 114: 105117.
35. SILVA AR. Síntese, caracterização e atividades biológicas de 1, 2, 4-oxadiazóis. Trabalho de Conclusão de Curso (Licenciatura em Química) - Departamento de Química, Universidade Federal Rural de Pernambuco, Recife, 2020.
36. SOUZA LG, et al. Coumarins as cholinesterase inhibitors: A review. Chemico-Biological Interactions. 2016;254: 11–23.
37. VILKOVÁ M, et al. Acridine Based N-Acylhydrazone Derivatives as Potential Anticancer Agents: Synthesis, Characterization and ctDNA/HSA Spectroscopic Binding Properties. Molecules. 2022; 27(9): 2883.
38. VITAKU E, et al. Analysis of the structural diversity, substitution patterns, and frequency of nitrogen heterocycles among U.S. FDA approved pharmaceuticals. J Med Chem. 2014; 57(24): 10257-74.
39. WEI L, et al. Synthesis, Characterization, and Antifungal Activity of Schiff Bases of Inulin Bearing Pyridine ring. Polymers (Basel). 2019; 11(2): 371.