Rational structural modification of the isatin scaffold to develop new and potent antimicrobial agents targeting bacterial peptidoglycan glycosyltransferase

Abstract

Isatin-based small molecules targeting bacterial peptidoglycan glycosyltransferase are potent antimicrobial agents against S. aureus, E. coli and methicillin-resistant Staphylococcus aureus strains.

The development of thymol–isatin hybrids as broad-spectrum antibacterial agents with potent anti-MRSA activity

“…2). [30][31][32] Molecular hybridization is a well-established stratagem in which two or more pharmacophores are clubbed together for generating desired hybrid molecule that possess the biological efficacy of its parent pharmacophores with enhanced potency and reduced toxicity along with lower drug resistance and eliminated drug-drug interactions. 33 1,2,3-Triazole is a widely popular and versatile nucleus in medicinal chemistry, which is efficiently used as a linker for the development of hybrid molecules with a wide range of biological activities.…”

Novel isatin–triazole based thiosemicarbazones as potential anticancer agents: synthesis, DFT and molecular docking studies

“…1 They play an important role as a core moiety in a diverse range of natural products, including hemoglobin, biomolecules, RNA, DNA, proteins, vitamins, and biologically active compounds. 2 Isatin (1H indole-2,3-dione) has attracted the interest of researchers in both synthetic and medicinal chemistry due to its chemical reactivity and broad range of applications, which include antimicrobial, 3,4 anti-cancer, 5,6 anti-HIV, 7 anticonvulsant, 8 antioxidant, 9,10 anti-inammatory, 3,11 antitubercular, [12][13][14] and antidiabetic 11,15,16 properties. Sutent (SU11248), also known as Sunitinib, is a drug derived from 5-uoro isatin that is used for targeted therapy in gastrointestinal stromal tumors, advanced renal cancer, and pancreatic neuroendocrine carcinoma.…”

Synthesis and Biological Evaluation of Isatin Derivatives as Antibacterial Inhibitors

“…Heterocyclic compounds with an isatin nucleus have assorted biological merits, including anti-inflammatory, analgesic [1][2][3][4][5], anticancer [6][7][8][9][10][11], antiglycation [12], antimalarial [13][14][15][16][17], antioxidant [18][19][20][21], anthelmintic [22], and antianxiety activities [23]. Moreover, they work as anticonvulsants [24,25], anti-HIV [26][27][28], antiviral [29], antibacterial [30][31][32][33][34], anti-fungal [35], and anti-tubercular agents [36][37][38][39]. Isatin derivatives also have various industrial applications, they are used as corrosion inhibitors [40][41][42], fluorescent sensors [43][44][45][46], and also in the dye industry [47,…”