Recent Advancement of Synthesis of Isatins as a Versatile Pharmacophore: A review

Abstract

Isatin (1 H-indole-2, 3-Dione) and its derivatives are versatile compounds which acts as a precursor for a large number of pharmacologically active compounds. Therefore isatins have a significant importance in the synthesis of different heterocyclic compounds. Isatins show variety of biological activities. In this review we focus on synthetic methods of isatins and their biological activities such as antimicrobial, anticonvulsant, anti-inflammatory and analgesic activity, antitubercular activity.

Step-Economic Total Synthesis of Melosatin A from Eugenol

“…Based on these results, this procedure was considered unsatisfactory, and the need to follow an alternative strategy was put forward. Although several methodologies have been developed for the construction of isatins, most of them usually involve multi-step reactions, require proper substrate prefunctionalization, or demand harsh reaction conditions, or complex operations which must be adapted to milligram-scale reactions …”

The Multi‐Pharmacological Targeted Role of Indole and its Derivatives: A review

“…Additionally, the indole motif is present in a wide range of natural products, primarily in the form of alkaloids, and is infrequently employed in the synthesis of numerous synthetic compounds with effective biological evaluations. Moreover, indole is a advantaged scaffold in the development of new chemical entities and their bioactivities are extremely much renowned in the literature, some of them are Antidepressant-Tryptophan (2), Neurotransmitter-Serotonin (3), Sleep Aid-Melatonin (4), Psychedelic drug-Lysergic acid diethylamide (5), Pesticide-Strychnine (6), Anticancer-Mitomycin C (7)-&Vinblastine (8), Anti-inflammatory-Indomethacin (9),Analgesic-Pravadoline (10), Antihypertensive-Reserpine (11), Anti-leukemic-Panobinostat (12), Anti-migraine-Sumatriptan (13), and Hypercholesterolemia-Fluastatin (14). The structures of some selected drug candidates (2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14) having indole-nucleus were presented in Figure 2.…”

“…The developments of synthetic and biological potentials of indole cored motifs were reported by Thanikachalam et al [7] The structural activity relationship studies with respect to their biological potential are also discussed in their review. Gajendra Kumar and his research group [8] reviewed the many biological functions of isatins and their varied synthesis methods. In 2020, the current development of indole analogs with respect to biological activities was reviewed by Bhupinder Kumar et al [9] and in addition, SAR studies were also disclosed.…”

“…Moreover, indole is a advantaged scaffold in the development of new chemical entities and their bioactivities are extremely much renowned in the literature, some of them are Antidepressant-Tryptophan (2), Neurotransmitter-Serotonin (3), Sleep Aid-Melatonin (4), Psychedelic drug-Lysergic acid diethylamide (5), Pesticide-Strychnine (6), Anticancer-Mitomycin C (7)-&Vinblastine (8), Anti-inflammatory-Indomethacin (9),Analgesic-Pravadoline (10), Antihypertensive-Reserpine (11), Anti-leukemic-Panobinostat (12), Anti-migraine-Sumatriptan (13), and Hypercholesterolemia-Fluastatin (14). The structures of some selected drug candidates (2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14) having indole-nucleus were presented in Figure 2. [2][3][4] As a result, the construction of the indole nucleus and its derivatization is a key pasture in medicinal chemistry.…”

A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs)

“…Isatin derivatives possess a wide range of applications due to their inherent versatility in structure, which allows for the construction of diverse frameworks suitable for a specific biological or chemical property of interest. A variety of substituents, particularly at N-1, C-3 (C=O) and C5/C6/C7 (aromatic), can be introduced, modulating both the biological and chemical properties of the parent core [ 7 ].…”