Recent Advances in Analgesic Drug Discovery: Azole-Based Heterocycles as Key Scaffolds
Session
Medicine and Nursing
Description
This review presents the latest progress in the design and synthesis of small-molecule analgesics incorporating azole-based heterocyclic frameworks. The study highlights how structural variations in rings such as imidazole, triazole, thiazole, indazole, and oxadiazole contribute to diverse analgesic mechanisms, including cyclooxygenase inhibition, opioid receptor modulation, and sodium channel blockade. Structure–activity relationship (SAR) analyses reveal that fine-tuning substituents and introducing bioisosteric replacements enhance both potency and safety profiles. Moreover, azole scaffolds have shown remarkable adaptability in computational drug design (CADD) workflows, facilitating the identification of novel analgesic leads. Emphasis is also placed on optimizing formulation properties alongside pharmacological efficacy, as delivery potential remains a crucial aspect of therapeutic development. Collectively, this work provides a comprehensive insight into the evolving role of azole-based heterocycles as essential pharmacophores in modern analgesic drug discovery and innovation.
Keywords:
Analgesics, heterocyclic compounds, azoles, structure–activity relationship, drug design, bioisosterism, pain modulation
Proceedings Editor
Edmond Hajrizi
ISBN
978-9951-982-41-2
Location
UBT Lipjan, Kosovo
Start Date
25-10-2025 9:00 AM
End Date
26-10-2025 6:00 PM
DOI
10.33107/ubt-ic.2025.357
Recommended Citation
Evren, Asaf Evrim; Nuha, Demokrat; Kayaa, Aybüke Züleyha; Karakaya, Abdullatif; Tutuş, Beyzanur; Güngör, Emine Merve; Osmaniye, Derya; Kaya, Betül; Çevik, Ulviye Acar; Yurttaş, Leyla; and Kaplancikli, Zafer Asım, "Recent Advances in Analgesic Drug Discovery: Azole-Based Heterocycles as Key Scaffolds" (2025). UBT International Conference. 2.
https://knowledgecenter.ubt-uni.net/conference/2025UBTIC/MN/2
Recent Advances in Analgesic Drug Discovery: Azole-Based Heterocycles as Key Scaffolds
UBT Lipjan, Kosovo
This review presents the latest progress in the design and synthesis of small-molecule analgesics incorporating azole-based heterocyclic frameworks. The study highlights how structural variations in rings such as imidazole, triazole, thiazole, indazole, and oxadiazole contribute to diverse analgesic mechanisms, including cyclooxygenase inhibition, opioid receptor modulation, and sodium channel blockade. Structure–activity relationship (SAR) analyses reveal that fine-tuning substituents and introducing bioisosteric replacements enhance both potency and safety profiles. Moreover, azole scaffolds have shown remarkable adaptability in computational drug design (CADD) workflows, facilitating the identification of novel analgesic leads. Emphasis is also placed on optimizing formulation properties alongside pharmacological efficacy, as delivery potential remains a crucial aspect of therapeutic development. Collectively, this work provides a comprehensive insight into the evolving role of azole-based heterocycles as essential pharmacophores in modern analgesic drug discovery and innovation.