A Recent Perspective on Discovery and Development of Diverse Therapeutic Agents Inspired from Isatin Alkaloids

Abstract

Isatin as an alkaloidal framework have consistently attracted attention of medicinal chemist towards development of wide range of novel therapeutic agents. This review report has discussed significant isatin lead molecules and their derivatives which have shown promising biological potential in recent times. The substituted isatins showing a potent pharmacological activities such as antimicrobial, antitubercular, anticancer, antioxidant, anti-histaminic, anti-HIV, antiviral, anti-inflammatory, anti-Parkinson's and antidiabetic have been described in this review. The mechanism of action leading to therapeutic activity of the respective isatin derivation has also been recorded. This review reveals that the systematic and rational modifications on isatin motif exhibited significant bio-activities which can be exploited for the development of potent novel therapeutic agents in the future studies. Hence the quest to investigate more structural alterations on isatin scaffold should be continued.

N-Alkyl-Substituted Isatins Enhance P2X7 Receptor-Induced Interleukin-1βRelease from Murine Macrophages

“…Similarly, 1 N -methylisatin had no effect on P2X7-induced IL-1 β release, highlighting the importance of the chain length and/or hydrophobicity at N1 for activity. Despite reports of anti-inflammatory actions of isatin and various isatin derivatives [ 14 ], the compounds tested in the current study did not impair P2X7-induced IL-1 β release. However, it should be noted that the anti-inflammatory actions of isatin and isatin derivatives in vitro [ 32 ] are observed at concentrations greater than those used in the current study (30–100 μ M versus 1 μ M, resp.).…”

“…In the tissues of mammals, isatin concentrations vary from <0.1 to 10 μ M [ 11 ]. Due to the synthetic versatility of isatin, modification of this compound has resulted in the generation of a large number of isatin derivatives, which demonstrate a diverse array of antimicrobial, anti-inflammatory, anticonvulsant, and anticancer properties [ 12 – 14 ]. The biological targets of isatin derivatives are varied and include proteases, kinases, and caspases [ 15 ].…”

Hybrids of Isatin‐Pyrazole as Potential α‐Glucosidase Inhibitors: Synthesis, Biological Evaluations and Molecular Docking Studies

“…Isatin is an important heterocyclic system because of its inimitable role in medicinal chemistry. Numerous alkaloids, drugs, dyes, pesticides and analytical reagents contain this structural motif in their core structure . A large number of isatin derivatives have been reported in literature exhibiting a wide spectrum of biological activities that include anticancer, antibacterial, antiviral, anticonvulsant, anti‐inflammatory, antifungal activity, etc .…”

Comparative in silico and in vivo Analgesic and Anti-Inflammatory Activities of Some Novel Schiff Bases of Isatin

“…Isatin and pyrazole derivatives have achieved great importance due to the vast spectrum of pharmacological activities which are reflected by their use as antimicrobial, analgesic, antiinflammatory and anticonvulsant activities [1][2][3]. Indomethacin having indole nucleus and phenylbutazone, a pyrazolone derivative are among the most widely used drug as NSAID [4].…”