Soni Aditi, Sharma Monika, Singh Rajesh K
Department of Pharmaceutical Chemistry, Shivalik College of Pharmacy, Nangal, District Ropar, Punjab 140124, India.
Global College of Pharmacy, Kahnpurkhui, Anandpur Sahib, District Ropar, Punjab 140117, India.
Curr Top Med Chem. 2025 Apr 30. doi: 10.2174/0115680266375345250414050338.
1,4-Dihydropyridines (1,4-DHPs) serve as versatile scaffolds in medicinal chemistry, exhibiting multitarget potential with anticancer, cardiovascular, antioxidant, antiinflammatory, antimicrobial, and analgesic effects. Structural modifications enhance their binding affinity, bioavailability, and selectivity.
This review aims to explore the broad therapeutic potential of 1,4-DHPs by analyzing their biological activities and structure-activity relationships (SAR). Additionally, it seeks to provide medicinal chemists with insights into key structural modifications that can optimize their pharmacological efficacy.
A comprehensive literature search was conducted in PubMed, ScienceDirect, Elsevier, and Google Scholar, prioritizing peer-reviewed studies from the last decade. Inclusion criteria focused on pharmacological properties, SAR, and therapeutic potential of 1,4-DHPs, while nonpeer- reviewed or irrelevant studies were excluded. Data extraction analyzed SAR trends, emphasizing the impact of structural modifications on binding affinity, bioavailability, and biological activity.
The review highlights that specific modifications in aromatic substituents, ester groups, and heterocyclic rings play a crucial role in enhancing the biological activity and selectivity of 1,4- DHPs. Their ability to modulate key enzymes and receptors contributes to their effectiveness as multitarget agents. Comparative SAR analysis provides evidence of the potential of 1,4-DHPs as next-generation therapeutics.
1,4-DHPs offer a promising framework for drug development, with the potential to address complex, multifactorial diseases. By understanding and optimizing SAR, medicinal chemists can design more selective and potent 1,4-DHP-based drugs. Future research should focus on refining these structural modifications to unlock their full therapeutic potential.
1,4-二氢吡啶（1,4-DHPs）是药物化学中用途广泛的骨架结构，具有抗癌、心血管、抗氧化、抗炎、抗菌和镇痛等多靶点潜力。结构修饰可增强其结合亲和力、生物利用度和选择性。
本综述旨在通过分析1,4-DHPs的生物活性和构效关系（SAR）来探索其广泛的治疗潜力。此外，还旨在为药物化学家提供有关可优化其药理疗效的关键结构修饰的见解。
在PubMed、ScienceDirect、Elsevier和谷歌学术上进行了全面的文献检索，优先选择过去十年的同行评审研究。纳入标准侧重于1,4-DHPs的药理特性、SAR和治疗潜力，同时排除非同行评审或不相关的研究。数据提取分析了SAR趋势，强调结构修饰对结合亲和力、生物利用度和生物活性的影响。
该综述强调，芳香取代基、酯基和杂环的特定修饰在增强1,4-DHPs的生物活性和选择性方面起着关键作用。它们调节关键酶和受体的能力有助于其作为多靶点药物的有效性。比较SAR分析提供了1,4-DHPs作为下一代治疗药物潜力的证据。
1,4-DHPs为药物开发提供了一个有前景的框架，有可能解决复杂的多因素疾病。通过理解和优化SAR，药物化学家可以设计出更具选择性和强效的基于1,4-DHP的药物。未来的研究应侧重于完善这些结构修饰，以释放其全部治疗潜力。
