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Identification of Novel Chemical Scaffolds Inhibiting Trypanothione Synthetase from Pathogenic Trypanosomatids

Fig 2

Structure of compounds affecting tritryp trypanothione synthetase activity.

AI (P), 4,5-dihydroazepino[4,5-b]indol-2(1H,3H,6H)-one derivatives, paullones derivatives, (FS-554 and MOL2008), five APPDA, 6-arylpyrido[2,3-d]pyrimidine-2,7-diamine derivatives (ZEA10, ZEA35, ZEA40, ZEA41 and ZVR159), eight BDA, N,N'-bis(3,4-substituted-benzyl) diamine derivatives (EAP1-47, EAP1-63, APC1-67, APC1-87, APC1-89, APC1-99, APC1-101 and APC1-111), seven BBHPP, 1-(benzo[d]thiazol-2-yl)-4-benzoyl-3-hydroxy-5-phenyl-1H-pyrrol-2(5H)-one derivatives (AD81, AD84, ADMRC158, ADKPN160, ADKPN161, ADKPN164 and ADKPN165), three BZ, benzofuroxan derivatives (J18, J20 and J31) and one PD, 1H-purine-2,6(3H,7H)-dione derivatives [(Z)-8-(2-(2,4-dihydroxybenzylidene)hydrazinyl)-7-(2-hydroxy-3-phenoxy propyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione, TC227]. iPr, tBu, OBn, Mo and Ph, correspond to an isopropyl, tert-butyl, O-benzyl, 4 -morpholinyl and phenyl substitution, respectively.

Fig 2

doi: https://doi.org/10.1371/journal.pntd.0004617.g002