Cheke Rameshwar S, Patil Vaishali M, Firke Sandip D, Ambhore Jaya P, Ansari Iqrar A, Patel Harun M, Shinde Sachin D, Pasupuleti Visweswara Rao, Hassan Md Imtaiyaz, Adnan Mohd, Kadri Adel, Snoussi Mejdi
Department of Pharmaceutical Chemistry, Dr. Rajendra Gode College of Pharmacy, Malkapur 443101, Maharashtra, India.
Department of Pharmaceutical Chemistry, KIET School of Pharmacy, KIET Group of Institutions, Delhi-NCR, Ghaziabad 201206, Uttar Pradesh, India.
Pharmaceuticals (Basel). 2022 Feb 22;15(3):272. doi: 10.3390/ph15030272.
Isatin (1 indole 2, 3-dione) is a heterocyclic, endogenous lead molecule recognized in humans and different plants. The isatin nucleus and its derivatives are owed the attention of researchers due to their diverse pharmacological activities such as anticancer, anti-TB, antifungal, antimicrobial, antioxidant, anti-inflammatory, anticonvulsant, anti-HIV, and so on. Many research chemists take advantage of the gentle structure of isatins, such as NH at position 1 and carbonyl functions at positions 2 and 3, for designing biologically active analogues via different approaches. Literature surveys based on reported preclinical, clinical, and patented details confirm the multitarget profile of isatin analogues and thus their importance in the field of medicinal chemistry as a potent chemotherapeutic agent. This review represents the recent development of isatin analogues possessing potential pharmacological action in the years 2016-2020. The structure-activity relationship is also discussed to provide a pharmacophoric pattern that may contribute in the future to the design and synthesis of potent and less toxic therapeutics.
异吲哚酮（1-吲哚-2,3-二酮）是一种杂环内源性先导分子，在人类和不同植物中都有发现。异吲哚酮核及其衍生物因其多样的药理活性，如抗癌、抗结核、抗真菌、抗菌、抗氧化、抗炎、抗惊厥、抗艾滋病毒等，而受到研究人员的关注。许多研究化学家利用异吲哚酮的温和结构，如1位的NH以及2位和3位的羰基官能团，通过不同方法设计具有生物活性的类似物。基于已报道的临床前、临床和专利细节的文献调查证实了异吲哚酮类似物的多靶点特性，从而证实了它们作为一种有效的化疗药物在药物化学领域的重要性。本综述介绍了2016 - 2020年期间具有潜在药理作用的异吲哚酮类似物的最新进展。还讨论了构效关系，以提供一种药效团模式，这可能在未来有助于设计和合成高效低毒的治疗药物。
