trypanothione

Trypanothione, a bis-glutathionyl derivative present in trypanosomatids, offers protection against oxidative stress [1] [2] [3].

Trypanothione Synthetase-IN-1 (Compound 1) serves as a competitive inhibitor of Leishmania infantum trypanothione synthetase (TryS), demonstrating an IC50 value of 14.8 μM in the presence of the polyamine S, triamine spermidine [1].

Trypanothione Synthetase-IN-3, a mixed noncompetitive inhibitor of Trypanothione Synthetase (TryS) with an inhibition constant (Ki) of 0.8 μM, is useful in researching parasites like L. infantum [1].

Trypanothione synthetase-IN-4 is a L. infantumTryS inhibitor whose activity is dependent on the concentration of the polyamine substrate. trypanothione synthetase-IN-4 exhibits a strong anti-leishmanicidal effect (EC50: 0.6 μM, SI ( Trypanothione synthetase-IN-4 can be used to study leishmaniasis.

Trypanothione Synthetase-IN-2 (Compound 3) functions as a competitive inhibitor of Leishmania infantum trypanothione synthetase (TryS), demonstrating an inhibition constant (IC50) of 5.4 μM in the presence of the polyamine S, triamine spermidine [1].

2-Fluoro-4-iodo benzonitrile is a building block.1,2It has been used in the synthesis ofL. infantumtrypanothione reductase (Li-TryR) dimerization and oxidoreductase activity inhibitors.12-Fluoro-4-iodo benzonitrile has also been used in the synthesis of transient receptor potential ankyrin 1 (TRPA1) antagonists.2 1.Revuelto, A., Ruiz-Santaquiteria, M., de Lucio, H., et al.Pyrrolopyrimidine vs imidazole-phenyl-thiazole scaffolds in nonpeptidic dimerization inhibitors of Leishmania infantum trypanothione reductaseACS Infect. Dis.5(6)873-891(2019) 2.Vallin, K.S., Sterky, K.J., Nyman, E., et al.N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptorBioorg. Med. Chem. Lett.22(17)5485-5492(2012)

(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanothione reductase when used at a concentration of 200 μM.3(E)-Ajoene (25 mg/kg) is neuroprotective in a gerbil model of ischemia-reperfusion injury, reducing reactive astrocytosis and microgliosis in the hippocampal CA1 region.4 1.Yoshida, H., Iwata, N., Katsuzaki, H., et al.Antimicrobial activity of a compound isolated from an oil-macerated garlic extractBiosci. Biotechnol. Biochem.62(5)1014-1017(1998) 2.Kaschula, C.H., Hunter, R., Hassan, H.T., et al.Anti-proliferation activity of synthetic ajoene analogues on cancer cell-linesAnticancer Agents Med. Chem.11(3)260-266(2011) 3.Gallwitz, H., Bonse, S., Martinez-Cruz, A., et al.Ajoene is an inhibitor and subversive substrate of human glutathione reductase and Trypanosoma cruzi trypanothione reductase: Crystallographic, kinetic, and spectroscopic studiesJ. Med. Chem.42(3)364-372(1999) 4.Yoo, D.Y., Kim, W., Nam, S.M., et al.Neuroprotective effects of Z-ajoene, an organosulfur compound derived from oil-macerated garlic, in the gerbil hippocampal CA1 region after transient forebrain ischemiaFood Chem. Toxicol.721-7(2014)

Kukoamine A possesses anticancer, cytoprotective, antioxidant, and anti-inflammatory activities, it also has neuroprotective effects through inhibiting oxidative stress and apoptosis after whole-brain irradiation (WBI) in rats.

Chinifur is a selective inhibitor and subversive substrate for Trypanosoma congolense trypanothione reductase

Antileishmanial agent-23 (compound G1/9), a potent and selective trypanothione reductase (TR) inhibitor, exhibits an IC50 of 2.24 ± 0.52 μM. It effectively inhibits the growth of Leishmania, Trypanosoma cruzi, and Trypanosoma brucei [1].

Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor (IC50: 3.3 μM). Antitrypanosomal agent 1 inhibits glutathione reductase (IC50: 64.8 μM) and T. brucei (EC50: 1 μM).