ROLE OF HETEROCYCLES IN DRUG DISCOVERY: AN OVERVIEW
Authors/Creators
Description
Heterocycles represent one of the most important classes of chemical scaffolds in modern drug discovery. Their widespread presence in natural products and synthetic drugs underscores their versatility and biological significance. More than half of all approved small-molecule drugs feature at least one heterocyclic ring, reflecting their ability to fine-tune pharmacological and physicochemical properties. In this review, we highlight the contribution of different classes of heterocycles—including five- and six-membered rings, non-aromatic systems, and fused heterocycles—to medicinal chemistry. Their applications across therapeutic areas such as oncology, infectious diseases, central nervous system (CNS) disorders, and antiviral therapy are discussed. Finally, we outline recent advances in rational drug design, computational methods, and emerging trends such as targeted therapy, nanotechnology, and personalized medicine, emphasizing the continued importance of heterocycles in shaping the future of therapeutics.
Files
3 WJAPS 269.pdf
Files
(382.4 kB)
| Name | Size | Download all |
|---|---|---|
|
md5:727b98cc81228f234d30729241527ca8
|
382.4 kB | Preview Download |
Additional details
Identifiers
- ISSN
- 3049-3013
Related works
- Is referenced by
- Journal article: 3049-3013 (ISSN)
References
- Sharma A, Gupta P. Pyrrole derivatives as anticancer agents: recent developments. Eur J Med Chem., 2022; 240: 114543.
- Singh R, et al. Novel pyrrole compounds as potent tuberculostatic agents. Bioorg Med Chem Lett., 2021; 45: 128274.
- Endo A, Kuroda M, Tsujita Y. ML-236A, ML-236B, and ML-236C, new inhibitors of cholesterogenesis produced by Penicillium citrinium. J Antibiot, 1976; 29(12): 1346-1348.
- Khan I, et al. Thiazole-based scaffolds as potential anti-TB agents. Pharmacol Rep., 2023; 75: 445-459.
- Kumar A, et al. Imidazo[2,1-b]thiazoles targeting DprE1 for TB drug discovery. J Med Chem., 2022; 65(12): 8724-8738.
- Li H, et al. Thiazole-containing CNS active agents: recent insights. MedChemComm., 2024; 15: 56-67.
- Patel J, et al. Therapeutic potential of imidazole derivatives. Front Pharmacol, 2024; 15: 110239.
- Hassan M, et al. Imidazole-based antimicrobials against resistance. Bioorg Chem., 2023; 136: 106479.
- Yadav R, et al. Pyrazole derivatives in medicinal chemistry: a review. Eur J Med Chem., 2018; 144: 834-885.
- Wang X, et al. Pyrazole derivatives with antifungal potential. Pest Manag Sci., 2023; 79: 1985-1997.
- Zhang L, et al. Triazole-based antifungal agents: recent progress. Future Med Chem., 2024; 16: 771-789.
- Chen Y, et al. Fluorinated triazoles in drug discovery. Eur J Med Chem., 2023; 250: 115167.
- Zhao J, et al. Pyridine derivatives as anticancer agents. Bioorg Med Chem., 2025; 33: 117342.
- Brown A, et al. Pyridine scaffolds in drug discovery. Drug Discov Today, 2024; 29(3): 507-520.
- Thomas M, et al. Pyrimidine-based anticancer drugs. Curr Med Chem., 2024; 31(9): 1524-1542.
- Gupta S, et al. Pyrido[2,3-d]pyrimidines in anticancer therapy. Eur J Pharm Sci., 2023; 183: 106338.
- Wang P, et al. Quinazoline derivatives in cancer therapy. Eur J Med Chem., 2025; 256: 115653.
- Sharma K, et al. Microwave-assisted synthesis of quinazolines. Synth Commun, 2023; 53(2): 148-162.
- Roberts L, et al. Triazine scaffolds in drug discovery. J Med Chem., 2023; 66(5): 2344-2359.
- Chen Z, et al. Piperidine derivatives in medicinal chemistry. Front Chem., 2023; 11: 118733.
- Carreira E, et al. Oxetanes as solubility enhancers in drug design. Angew Chem Int Ed., 2024; 63: 11212-11225.
- Matsuoka J, et al. THF-containing anticancer natural products. Nat Prod Rep., 2023; 40(8): 1402-1421.
- Banerjee A, et al. Indole derivatives in drug discovery. Med Res Rev., 2024; 44: 112-145.
- Singh V, et al. Quinoline scaffolds in infectious disease therapy. Curr Opin Pharmacol, 2024; 78: 102546.
- Rahman M, et al. Benzimidazole derivatives: recent advances. Eur J Med Chem., 2024; 242: 114875.
- Brody T. Purine analogues in anticancer chemotherapy. Cancer Treat Rev., 2022; 109: 102447.
- Li X, et al. Coumarins in modern drug discovery. Phytomedicine, 2024; 123: 155782.