Sharma Vishal, Das Rina, Kumar Mehta Dinesh, Gupta Sumeet, Venugopala Katharigatta N, Mailavaram Raghuprasad, Nair Anroop B, Shakya Ashok K, Kishore Deb Pran
MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala 133207, India.
MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala 133207, India.
Bioorg Med Chem. 2022 Apr 1;59:116674. doi: 10.1016/j.bmc.2022.116674. Epub 2022 Feb 18.
Quinolones are a type of bicyclic privileged building block with immense therapeutic potential. They are known for their crucial role in modulating numerous diseases conditions. In the present review, quinolone and its derivatives with different pharmacological properties like antibacterial, anticancer, anti-HIV, antitubercular and antimalarial activities are described on the basis of their structure activity relationship studies. Literature is mainly focused on the structural changes responsible for the significant increase in the therapeutic profile of the quinolone scaffold and its derivatives. The substitution pattern in the scaffold responsible for a substantial rise in the potency of specific activity has also been discussed, while emphasizing their potential as lead molecule for the drug discovery and development. Moreover, updates of recent research findings on this scaffold are also discussed.
喹诺酮类是一类具有巨大治疗潜力的双环优势结构单元。它们因其在调节多种疾病状况中的关键作用而闻名。在本综述中,基于结构活性关系研究,描述了具有不同药理特性(如抗菌、抗癌、抗HIV、抗结核和抗疟活性)的喹诺酮及其衍生物。文献主要关注导致喹诺酮骨架及其衍生物治疗特性显著提高的结构变化。还讨论了骨架中的取代模式,其导致特定活性的效力大幅提高,同时强调了它们作为药物发现和开发先导分子的潜力。此外,还讨论了关于该骨架的最新研究结果的更新情况。