Synthesis, X-ray molecular structure, biological evaluation and molecular docking studies of some N 4 -benzyl substituted 5-nitroisatin-3-thiosemicarbazones

Synthesis and in vitro Bio-activity Evaluation of N4-benzyl Substituted 5-Chloroisatin- 3-thiosemicarbazones as Urease and Glycation Inhibitors

“…In view of this and as an extension of our earlier studies [36][37][38][39][40][41][42][43][44][45][46][47] aiming to the synthesis of novel isatin derivatives with enhanced or diverse biological activities, we very recently reported the synthesis of a series of N 4 -benzyl substituted 5-nitroisatin-3-thiosemicarbazones (derivatives of thiourea, a substrate-like urease inhibitor) as highly effective urease inhibitors. 48 Interestingly, all these compounds demonstrated either induced or increased urease inhibitory activity in comparison to the respective N 4 -phenyl substituted derivatives tested in our earlier assays. 38,45 Furthermore, a number of other derivatives of thiourea are reported to show promising glycation inhibitory activity.…”

Synthesis of New Oxindoles and Determination of Their Antibacterial Properties

“…Although in other research they evaluated several isatin-3-hydrazonothiazolines as urease inhibitors, despite some good results, substituents like 5-OCF 3 and 5-F over the isatin ring decreased the activity in various cases [33,34]. In a more recent research, Pervez et al reported several thiosemicarbazone-isatin derivatives with important activity as a urease inhibitors with lower IC 50 (0.87 to 11.23 μM) than thiourea (IC 50 � 22.3 μM) [35][36][37]. According to the abovementioned background about this kind of products, we have designed a series of isatin-pyrazole hybrids that could be effective as antimicrobials.…”

Camphor-Based Thiosemicarbazone Analogues Induced G2 Cell Cycle Arrest and Apoptosis via Reactive Oxygen Species (ROS)-Mediated Mitochondrial Pathway in Human Breast Cancer Cells

“…Thiosemicarbazones possess a remarkable pharmacological profile, and occupy a prominent position in pharmaceutical chemistry on account of their broad biological activity such as antiparasitic, [3][4][5] antibacterial, [6][7] antiviral [8][9] and anticancer. [10][11][12] Currently, the application of thiosemicarbazones in cancer therapy is being most extensively investigated. In 2007, de Oliveira et al [13] reported a series of thiosemicarbazone derivatives, as well as their in vitro antiproliferative activity against eight human tumor cell lines, and compound 1-1 (Figure 1) was the most promising against michigan cancer foundation-7 (MCF-7) cell (IC 50 ＝0.25 µmol•L -1 ).…”