Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives

Design, synthesis and in vitro antikinetoplastid evaluation of N-acylated putrescine, spermidine and spermine derivatives

“…Spermidine conjugated with a truncated CoA analogue 1, 20 and 24 were synthesized from their Boc-protected counterparts 21, 19 and 23, respectively, in a two-step procedure: amide formation with bromoacetyl bromide and subsequent nucleophilic substitution involving the required thiol derivatives namely 3-acetamido-N-(2-mercaptoethyl)propanamide or N-acetyl-cysteamine.…”

“…19 Pentamidine and miltefosine were included in the assays as positive controls for T. brucei and L. donovani, respectively. In this evaluation, the activity was expressed in IC 50 (concentration inhibiting the parasite growth of 50%).…”

“Squalenoylcurcumin” Nanoassemblies as Water‐Dispersible Drug Candidates with Antileishmanial Activity

“…[86] In vitro antileishmanial evaluation on intramacrophagic amastigotes: The mouse monocyte/macrophage cell line RAW 264.7 was maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10 % heat-inactivated fetal bovine serum. Cultures were incubated with test compounds for 72 h at 37 8C in the dark under a 5 % CO 2 atmosphere.…”

“…[86] The results are expressed as the MTC (maximum tolerated concentration), the maximum concentration for which no toxicity was observed. RAW 264.7 cells were seeded into a 96-well microtiter plate at a density of 5 10 3 cells well À1 in DMEM (100 mL).…”

Copper‐Catalyzed Domino Cycloaddition/CN Coupling/Cyclization/(CH Arylation): An Efficient Three‐Component Synthesis of Nitrogen Polyheterocycles

“…Then, in the presence of an ortho-carbonyl-substituted aryl halide III, the same catalytic system should enable an intermolecular Goldberg amidation (to give V), followed by a Camps cyclization (intramolecular aldol-dehydration sequence) to form a 2-quinolinone ring VI. [16,17] In the case of more reactive electrophiles, such as 2-bromobenzaldehyde, an alternative sequence involving a Knoevenagel condensation followed by intramolecular N-arylation is also possible and leads to the same product VI. When the R 3 substituent in VI is a 2'-bromoaryl group, the domino sequence should continue to evolve, as the triazolyl group is now perfectly positioned for an intramolecular copper-mediated C À H arylation to afford a pentacycle VII.…”