Isatin Conjugates as Antibacterial Agents: A Brief Review

Abstract

Pathogenic bacteria, with their innate resistance to drugs, pose a constant threat to human health and well-being and put a persistent strain on the health care system. Development of more effective and safer novel antibacterial drugs is warranted to counter the menace unleashed by pathogenic bacteria. Integration of privileged pharmacophores from various bioactive molecules into a single template is a promising strategy to obtain new leads with unique mechanisms of action to overcome drug resistance. In the past few years, numerous isatin-based hybrid molecules were screened and their pharmacological properties were explored in efforts to develop novel therapeutics. The results of screening show that isatin conjugates exhibit promising activity against a broad range of highly pathogenic gram-positive and gram-negative bacteria and can serve as important leads in the discovery of highly potent broad spectrum antibacterial drugs. Herein, we review the antibacterial bioactive profile of a variety of hybrid isatin derivatives, including isatin–azole, isatin–quinoline/quinolone, isatin–furan/coumarin, isatin–hydrazone/(thio)semicarbazone, isatin dimers, and isatin–indole hybrids.

Synthesis of Functionalized 2′,5‐Oxo‐spiro[furan‐2,3′‐indoline]‐3‐carboxylate Derivatives as Antiproliferative Agents: ADMET Studies, and Molecular Docking against P2Y12 Inhibitors

“…Chemical species with a very high PPB scores tend to have comparatively higher persistence in the circulation or an elongated plasma half‐life (t 1/2 ). More importantly, high PPB efficiency also impacts the drug efficacy as usually the circulating fraction of drugs is accredited to the potent pharmacological actions [30,31] . In the same vein, the PPB for novel spirooxindole‐oxofurans ( 4 a – d ) ranged from 87.828 to 94.40 % for 4 d and 4 a , respectively.…”

“…More importantly, high PPB efficiency also impacts the drug efficacy as usually the circulating fraction of drugs is accredited to the potent pharmacological actions. [30,31] In the same vein, the PPB for novel spirooxindole-oxofurans (4 a-d) ranged from 87.828 to 94.40 % for 4 d and 4 a, respectively. While, Carmustine exerted comparatively lower PPB efficiency (only 18.081 %), which could be associated with the poor absorption/distribution as well as its limited efficiency in the management of different malignancies.…”

Novel Functionalized Spiro [Indoline-3,5′-pyrroline]-2,2′dione Derivatives: Synthesis, Characterization, Drug-Likeness, ADME, and Anticancer Potential

“…In nature, different conformations of spirooxindole scaffolds ( Figure 1 ) have been isolated from specific plants, animals, and fungi, which are used for the treatment of various carcinomas [ 33 , 34 ]. Actually, spiro-quaternary-carbon centers have shown greater therapeutic potential in targeting distinct human ailments [ 35 , 36 , 37 , 38 , 39 ].…”

Eco-friendly one-step synthesis of highly functionalized-spirooxindole-pyranopyrazoles and their in-vitro anticancer studies

“…Although the discovery of anticancer drugs has been a challenging task for a chemist. Spirooxindioles (natural and synthetic) were shown to be more significant as promising anticancer agents, according to previous studies [7][8][9][10]. Moreover, the core of isatin has been inspired due to the dioxindoles (DOXs) being transformed into various spirooxindoles using different chemical transformations.…”