Discovery of novel phthalimide analogs: synthesis, antimicrobial and antitubercular screening with molecular docking studies

Amide Synthesis through the In Situ Generation of Chloro- and Imido-Phosphonium Salts

“…Protected tryptophan amino acid was also converted into the corresponding amide in moderate yields when coupling with primary amines ( 3ga 54% yield) but failed to provide the desired product with secondary amines ( 3gb ) most likely due to amine-induced Fmoc deprotection. Finally, our method enabled the synthesis of antifungal agrochemical Mepronil 3lc from the ortho -substituted carboxylic acid in 55% yield in milder conditions than current approaches. , …”

“…Acyl phthalimides are important precursors for the formation of the biologically active N- , O -acetal motifs found in several natural products . Acyl phthalimides also hold merit as potential anxiolytic, antibacterial, and antifungal compounds . Synthetic applications have also been explored using acyl imides as efficient acylating and coupling agents in metal-catalyzed reactions .…”

Exploring of N-phthalimide-linked 1,2,3-triazole analogues with promising ­anti-SARS-CoV-2 activity: synthesis, biological screening, and molecular modelling studies

“…These effects include tumorigenic effects and reproductive consequences. In addition, we investigated some drug-relevant characters, such as cLogP, LogS as an indication of the compounds solubility, drug-likeness, and overall drug-score 69 , 70 . We compared the results from our molecules with two drugs, GC-376 and Lopinavir.…”

Novel Oleanolic Acid-Phtalimidines Tethered 1,2,3 Triazole Hybrids as Promising Antibacterial Agents: Design, Synthesis, In Vitro Experiments and In Silico Docking Studies

“…Using our recently reported one-pot reduction-acetylation protocol, imide 6g afforded the α-acetoxy-lactam 8g in a 98% overall yield (Scheme 2) [79]. The second precursors, namely N/O-propargylated isoindolinones 6-8, were also synthesized using previously published protocols [70][71][72][73][74][75][76]. Substrates 6a-g were prepared through two synthetic routes involving base-assisted N-alkylation of phtalimide 5a, hydantoin 5b, succinimide 5c, and saccharin 5d rings with propargyl bromide resulting in the isolation of the precursors 6a-d in well isolated yields (87 to 97%).…”