Discovery and evaluation of chalcone derivatives as novel potential anti-Toxoplasma gondii agents

Antiviral and antimicrobial applications of chalcones and their derivatives: From nature to greener synthesis

“…Among these, four compounds displayed strong activity against T. gondii and minimal cytotoxicity in vitro. Moreover, the proliferation of Toxoplasma tachyzoites was inhibited by three of these derivatives in vivo [ 158 ]. Three types of chalcones were designed with substituents H, OH, or NH 2 at the C‐2′ position in ring A and substituents with electron‐releasing and electron‐withdrawing characteristics, such as OCH 3 , NO 2 , and halogens (Cl, F), in ring B.…”

“… [ 157 ] “(E)-3-(2-bromophenyl)-1-(4-(isopropylamino)phenyl)prop2-en-1-one” “(E)-3-(2-bromophenyl)-1-(4-(ethylamino)phenyl)prop-2-en1-one” Toxoplasma gondii In vitro, In vivo Significant anti-toxoplasma activity and reduction of biochemical variables as well as liver and spleen indices Anti-Toxoplasma effects are enhanced by the Michael receptor found in chalcones' molecular skeleton. [ 158 ] Chalcone derivatives with substituents in the A and B rings “1‐(2‐Aminophenyl)‐3‐(3,4,5‐trimethoxyphenyl)prop‐2‐en‐1‐one” “1‐(2‐Aminophenyl)‐3‐(3,5‐dimethoxyphenyl)prop‐2‐en‐1‐one” “1‐(2‐Hydroxyphenyl)‐3‐(3,4,5‐trimethoxyphenyl)prop‐2‐en‐1‐one” Leishmania braziliensis , Trypanosoma cruzi , Plasmodium falciparum In vitro EC 50 : 5.7 against L. braziliensis ; EC 50 against T. cruzi : 8.1 μM; EC 50 against P. falciparum : 59.2 μM The antiparasitic properties were affected by the hydrogen bonds at C-2′ with carbonyl and the electron-donating substituents in ring B. [ 153 ] Chalcone-thiosemicarbazones “(1 E ,2 E )-3-(phenyl)-1-phenylprop-2-en-1-one thiosemicarbazone” “(1 E ,2 E )-3-(40 -chlorophenyl)-1-phenylprop-2-en-1-one thiosemicarbazone” Leishmania amazonensis In vitro IC 50 against intracellular amastigotes: 3.40 μM, IC 50 against Promastigotes: 5.22 μM Anti-leishmanial properties were improved by moieties with electronic withdrawing effects.…”

New Nucleic Base-Tethered Trithiolato-Bridged Dinuclear Ruthenium(II)-Arene Compounds: Synthesis and Antiparasitic Activity

“…However, these treatments are unspecific, adverse effects have been frequently documented, and clinical failures have been reported [ 17 ]. A considerable effort is being made to identify better solutions [ 17 , 18 , 19 , 20 ] and new structures are emerging [ 21 , 22 , 23 , 24 , 25 , 26 , 27 ]. For example, experimental compounds such as bumped kinase inhibitors, which impair the activity of T. gondii calcium dependent protein kinase 1 (essential for host cell invasion and egress), endochin-like quinolones (ELQs) that are specific and potent T. gondii cytochrome bc1 inhibitors, and a leucinostatin-derived antimicrobial peptide that interferes in multipole metabolic pathways, have been demonstrated to exert anti-parasitic effects in vitro and in vivo [ 28 , 29 , 30 ].…”

Licochalcone A Derivatives as Selective Dipeptidyl Peptidase 4 Inhibitors with Anti-Inflammatory Effects

“…In the past decade, many studies have reported on the DPP4 inhibitory activity of natural products. − Nonetheless, most known natural product families, including anthocyanins, phenolic substances, and alkaloids, exhibit weak anti-DPP4 activity. ,, The chalcone scaffold is a privileged scaffold in medicinal chemistry because of its high synthetic convenience and structural variability. − Several natural or synthetic chalcone derivatives ( 1 – 5 ) have been reported to have protective effects against inflammatory injury in diabetic mice. − This prompted us to develop antidiabetic drugs with anti-inflammatory functions starting with this scaffold. Licochalcone A has been reported to have anti-inflammatory effects, anti-DPP4 effects, and protective effects against diabetic nephropathy.…”