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合成与结构多样的酞嗪衍生物的生物活性:系统评价。

Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review.

机构信息

Y. B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Rauza Baugh, Aurangabad, MS, India.

Y. B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Rauza Baugh, Aurangabad, MS, India.

出版信息

Bioorg Med Chem. 2019 Sep 15;27(18):3979-3997. doi: 10.1016/j.bmc.2019.07.050. Epub 2019 Aug 1.

Abstract

Phthalazine, a structurally and pharmacologically versatile nitrogen-containing heterocycle, has gained more attention from medicinal chemists in the design and synthesis of novel drugs owing to its pharmacological potential. In particular, phthalazine scaffold appeared as a pharmacophoric feature numerous drugs exhibiting pharmacological activities, in particular, antidiabetic, anticancer, antihypertensive, antithrombotic, anti-inflammatory, analgesic, antidepressant and antimicrobial activities. This review presents a summary of updated and detailed information on phthalazine as illustrated in both patented and non-patented literature. The reported literature have described the optimal pharmacological characteristics of phthalazine derivatives and highlighted the applicability of phthalazine, as potent scaffold in drug discovery.

摘要

酞嗪是一种结构和药理多功能的含氮杂环,由于其潜在的药理作用,在新型药物的设计和合成中引起了更多的关注。特别是,酞嗪支架作为一种药效团特征出现在许多具有药理活性的药物中,特别是抗糖尿病、抗癌、抗高血压、抗血栓形成、抗炎、镇痛、抗抑郁和抗菌活性的药物中。本综述总结了专利和非专利文献中报道的更新和详细的酞嗪信息。所报道的文献描述了酞嗪衍生物的最佳药理特性,并强调了酞嗪作为药物发现中有效支架的适用性。

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