Department of Pharmaceutical Chemistry, Hacettepe University, Faculty of Pharmacy, Ankara 06100, Turkey.
Future Med Chem. 2021 Feb;13(3):287-311. doi: 10.4155/fmc-2020-0234. Epub 2020 Dec 4.
Azolo[]pyridazinone is a privileged structure and versatile pharmacophore whose derivatives are associated with diverse biological activities, in particular antidiabetic, antiasthmatic, anticancer, analgesic, anti-inflammatory, antithrombotic, antidepressant and antimicrobial activities. The importance of this scaffold against some targets like PDE, COX and DPP-4 has been reviewed in detail previously. In the present review, we have summarized comprehensive information on azolo[]pyridazinone derivatives investigated by many researchers for their diverse pharmacological activities, structure-activity relationship and molecular modeling studies since 2000. The review may lead scientists in the research fields of organic synthesis, medicinal chemistry and pharmacology to the strategic design and development of azolo[]pyridazinone-based drug candidates in the future.
氮杂[1,5-a]哒嗪酮是一种重要的结构和多功能药效团，其衍生物具有多种生物活性，特别是抗糖尿病、抗哮喘、抗癌、镇痛、抗炎、抗血栓形成、抗抑郁和抗菌活性。该支架针对 PDE、COX 和 DPP-4 等靶点的重要性以前已经有详细的综述。在本综述中，我们总结了自 2000 年以来，许多研究人员针对氮杂[1,5-a]哒嗪酮衍生物的多种药理学活性、构效关系和分子建模研究的综合信息。这篇综述可能会引导有机合成、药物化学和药理学领域的科学家在未来对基于氮杂[1,5-a]哒嗪酮的候选药物进行战略性设计和开发。
