trypanothione

Trypanothione是锥虫中发现的双谷胱甘肽衍生物，具有抵御氧化压力的保护功能。

Antitrypanosomal agent 1 是一种有效的选择性锥虫硫酮还原酶抑制剂，IC50为 3.3 μM。它抑制谷胱甘肽还原酶，IC50为 64.8 μM，抑制布氏锥虫，EC50为 1 μM。

Trypanothione synthetase-IN-4 是一个 L. infantumTryS 抑制剂，其活性依赖于多胺底物的浓度。Trypanothione synthetase-IN-4 表现出较强的抗 leishmanicidal 效果 (EC50: 0.6 μM，SI (选择性指数): 35）。Trypanothione synthetase-IN-4 能够用于研究利什曼病。

Trypanothione synthetase-IN-1 (Compound 1) 为一竞争性婴儿利什曼虫锥体胱甘肽合成酶(TryS)抑制剂，以三胺亚精胺为多胺S时，IC50值为14.8 μM。

Trypanothione synthetase-IN-2 (Compound 3) 为竞争性婴儿利什曼虫锥虫胱甘肽合成酶 (TryS) 抑制剂，以三胺亚精胺作为多胺S时，IC50 值为5.4 μM。

Trypanothione synthetase-IN-3是一种针对Trypanothione synthetase (TryS)的非竞争性混合双曲线抑制剂，其Ki值为0.8 μM。该化合物主要用于研究寄生虫，例如L. infantum。

Kukoamine A 是一种天然的精胺衍生物，具有抗癌、抗高血压、细胞保护、抗氧化和抗炎活性。它是锥虫硫磷还原酶抑制剂，Ki 值为 1.8 μM。

(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)

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)

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

Antileishmanial agent-23 (compound G1 9) 作为一种选择性trypanothione reductase (TR)抑制剂效力显著，展现了2.24 ± 0.52 μM的IC50值。该化合物有效抑制了利什曼原虫、克氏锥虫和布氏锥虫的生长。