Antiparasitic Chemical Compounds

                                                                                                                                                                                                                                  Download data

2,2'-bipyridine (bipy), 1,10-phenanthroline (phen) or dipyrido[3,2-d:2',3'-f]quinoxaline (dpq) synthesized by the reaction with SbCl3 or PhSbCl2.IC50 in the nanomolar range against Sb(III)-sensitive and -resistant Leishmania infantum (syn. Leishmania chagasi) and Leishmania amazonensis strainsComplexes of different nitrogen donor heterocyclic ligands with SbCl3 and PhSbCl2 as potential antileishmanial agents against Sb (III)-sensitive and -resistant parasites.24412095
Ketolide agents HMR 3004 and HMR 3647 (telithromycin)In vitro activity of HMR 3004 and HMR 3647 against?Plasmodium falciparum with IC50 values 3 and 15 nM respectivelyKetolide agents HMR 3004 and HMR 3647 (telithromycin) inhibit the growth of Plasmodium falciparum in vitro. Malaria is on the increase due to emergence of parasite drug resistance and there is thus an urgent need for the development of new antiparasitic drugs effective at low concentrations26958030
6-mercaptopurine and 6-thioguanineOf the studied 64 compounds, 22 produced a 50% inhibition of the growth of the human malaria parasite Plasmodium falciparum at a concentration of 50 microM or less.Two of the compounds which effectively inhibited parasite growth, 6-mercaptopurine and 6-thioguanine, were found to be potent competitive inhibitors of a key purine-salvaging enzyme (hypoxanthine-guanine-xanthine phosphoribosyltransferase) of the parasite.2201255
Mollemycin APotent and selective growth inhibitory activity against Gram-positive and Gram-negative bacteria (IC50 10-50 nM) and drug-sensitive (3D7; IC50 7 nM) and multidrug-resistant (Dd2; IC50 9 nM) clones of the malaria parasite Plasmodium falciparumMollemycin A: an antimalarial and antibacterial glyco-hexadepsipeptide-polyketide from an Australian marine-derived Streptomyces sp. (CMB-M0244)24611932
Nitrofuran isoxazolines and pentacyclic nitrofuransNitrofuran isoxazolines were potent inhibitors of T. Bruce proliferation at nanomolar concentrations, with pentacyclic nitrofurans being 100-fold more potent than nifurtimox.Pentacyclic nitrofuran isoxazolines warrant further development for the treatment of drug-susceptible and nifurtimox-resistant trypanosome infections.26682963
Copper catalysed Huigsen azide-alkyne 1, 3-dipolar cycloadditionExcellent broad spectrum antimicrobial and antiparasitic activity targeting Clostridium difficile, Entamoeba histolytica and Giardia lamblia.The copper catalysed Huigsen azide-alkyne 1, 3-dipolar cycloaddition offers a way to efficiently assemble new libraries of metronidazole analogues26117821
Indolone-N-oxide derivatives.Antibacterial, antifungal and antileishmanial activitiesINODs showed a broad spectrum of antimicrobial activity and offer a promising anti-infectious prototype worthy of being developed.22828966
Nitric Oxide (NO) and Tumor Necrosis Factor-alpha (TNF-alpha)In vitro activation of macrophage NO synthase by IFN-gamma induces a trypanostatic activity and TNF-alpha is involved in NO synthase induction.?Macrophage effector molecules participate with other immune effector mechanisms in resistance of host to trypanosomes.7496195
4-aminoquinoline-purine hybridsAntiplasmodial activities against both the sensitive and resistant strains of P. falciparum with up to six-fold better activity (compound 10i, IC50: 0.08 micro M) compared to the reference drug CQ (IC50: 0.5 micro M) against the resistant strainThe synthesized compounds were also checked for their cytotoxicity towards mammalian cells and with the exception of two compounds out of the twenty synthesized hybrids, all others were non-cytotoxic up to 11.86 ?M concentration.Design, synthesis and evaluation of 4-aminoquinoline-purine hybrids as potential antiplasmodial agents.27936446
1-amino-6-halo-beta-carbolinesSuperior activity to chloroquine itself against a resistant Plasmodium falciparum strainHere, we report the synthesis of some 6-halo-?-carbolines as analogues of the potent antimalarial natural product, manzamine A, retaining its heteroaromatic core whilst providing compounds with much improved synthetic accessibility.22275299