cruzi

T.cruzi-IN-1 (MDK1088) is a Trypanosoma cruzi inhibitor.

Anti-Trypanosoma cruzi agent-6 (Compound 8) exhibits inhibitory activity against Trypanosoma cruzi. It effectively suppresses the epimastigote, trypomastigote, and amastigote forms of T. cruzi, with IC50 values of 24.7 µM, 1.8 µM, and 1.6 µM, respectively.

Anti-Trypanosoma cruzi agent-1 (Compd 3b), a selective compound against NINOA trypomastigote (IC 50 = 0.51 μM) and INC-5 epimastigote (IC 50 = 3.06 μM), also possesses anti-T. gondii activity [1].

Anti-Trypanosoma cruzi agent-1 (Compd E5) demonstrates a potent anti-Toxoplasma effect.

Anti-Trypanosoma cruzi agent-3 is an antiprotozoal agent.

Anti-Trypanosoma cruzi Agent-4 is a Trypanosoma cruzi inhibitor utilized for the investigation of infections caused by this parasite.

T.cruzi Inhibitor hydrochloride is a Trypanosoma cruzi inhibitor.

K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

Moxipraquine is a novel 8-aminoquinolone compound with anti-infective activity against Trypanosoma cruzi. Moxipraquine effectively inhibited parasitemia but did not eradicate infections in mice or guinea pigs. Moxipraquine was effective against experimental infections of Leishmania major, Lactobacillus mexicanus, and Lactobacillus brasiliensis, but was Ineffective.

Nifurtimox (BAY-A-2502) is an antiprotozoal agent (IC50s = 9.91, 12.28, and 10.44 μM against Taluahuén, LQ, and Brener strains of T. cruzi- epimastigotes, respectively).

1, 2, 3, 4, 6-Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) and gallic acid from Pistacia lentiscus have antimutagenic and antioxidant activities. 2. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose (PGG) possesses potent anti-proliferative and anti-invasive effects, it also has inhibition of inducible nitric oxide synthase and cyclooxygenase-2 activity. 3. PGG may serve as a model for the development of new types of anti-diabetic and anti-metabolic syndrome therapeutics. 4. 1, 2, 3, 4, 6-Penta- O -galloyl-β- d -glucose has vasodilatory and anti-inflammatory effects, it dilates vascular smooth muscle and suppresses the vascular inflammatory process via endothelium-dependent nitric oxide (NO) cGMP signaling. 5. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose can decrease the level of extracellular hepatitis B virus (HBV) (IC5, 1. microg ml) in a dose-dependent manner, it also can reduce the HBsAg level by 25% at a concentration of 4 microg ml; the gallate structure of PGG may play a critical role in the inhibition of anti-HBV activity, suggests that PGG could be a candidate for developing an anti-HBV agent. 6. 1, 2, 3, 4, 6-Penta-O-galloyl-β-D-glucose has anti-parasitic activity, displays an EC5 value of 67 μM, at least 6.6-fold more effective than the standard drug benznidazole against trypomastigote forms of T. cruzi.

1. Lycobetaine (Ungeremine) is a potential biofungicide against Penicillium roqueforti and Aspergillus niger.2. Lycobetaine have strong antibacterial activity against Flavobacterium columnare . 3. Lycobetaine effectively targets mammalian as well as bacterial type I and type II topoisomerases.4. Lycobetaine shows strong acetylcholinesterase inhibitory activity(IC(50) value of 0.35 microM). 5. Lycobetaine has antiprotozoal activity, it shows good activity in in vitro assays against Trypanosoma brucei rhodesiense, T. cruzi.

Cruzain-IN-1 (ML092) is a covalent and reversible Cruzain inhibitor (IC50: 10 nM).

Benznidazol (Benznidazole)e has an antiprotozoal activity by interfering with parasite protein biosynthesis, influencing cytokines production and stimulating host phagocytosis.

Diloxanide furoate (Dichlofurazol) is an antiprotozoal compound with oral activity that can be used in the study of amoebas in tissues and several other protozoal infections.

TcNTPDase1-IN-1 (compound 16) serves as an inhibitor of nucleoside triphosphate diphosphohydrolase 1 (TcNTPDase1) from Trypanosoma cruzi in vitro. This compound is applicable in research related to antibacterial, antitoxic, and antitumor activities.

VNI is an effective inhibitor of CYP51. It suppresses sterol synthesis in Trypanosoma cruzi, exhibiting anti-Trypanosoma cruzi activity.

Se2h is a cruzain inhibitor exhibiting potent activity against intracellular amastigotes of Trypanosoma cruzi (EC50< 1 μM, SI> 10), with an inhibitory effect on cruzain of IC50< 100 nM (SI> 5.55). Compared to Benznidazole and cruzain inhibitor K777, Se2h shows superior selectivity and inhibition while its selenazole structure reduces selenium-related toxicity. Se2h demonstrates antiparasitic activity and holds promise for Chagas disease research.

MCG-02 is an inhibitor of cruzain (CRZ) and cathepsin L-like protease (CATL), capable of inhibiting CRZ in Trypanosoma cruzi and CATL in Trypanosoma brucei, with IC50 values of 0.2 μM and 0.02 μM, respectively.

PFK-IN-1 (compound 1) is an inhibitor of 6-phosphofructo-1-kinase (PFK), demonstrating IC50 values of 0.41 and 0.23 μM against T. brucei and T. cruzi PFK, respectively, and an ED50 of 15.18 μg mL for T. brucei. The compound has a half-life of 9.7 minutes in rat liver microsomes and 408 minutes in mouse liver microsomes.

TSO-13 is an inhibitor of the major cysteine protease Cruzipain found in Trypanosoma cruzi, with an IC50 of 2.2 μM. In Vero cells, TSO-13 also suppresses T. cruzi, exhibiting an IC50 of 1.9 μM.

Antiparasitic agent-24 (Compound 14a) is an antiparasitic compound with EC50 values of 0.005 μM for L. maj, 0.069 μM for L. don, 0.82 μM for T. brucei, and 4.1 μM for T. cruzi.

CZP-IN-1 (compound SH-1) is an inhibitor targeting the pathogen Trypanosoma cruzi protease (CZP) without affecting cathepsin L (IC50=28 nM). This compound is applicable in Chagas disease research.

Fexinidazole (HOE 239) is an antiparasitic agent with activity against Trypanosoma cruzi, Tritrichomonas foetus, Trichomonas vaginalis, Entamoeba histolytica, Trypanosoma brucei, and Leishmania donovani. The biologically relevant active metabolites in vivo are the sulfoxide and sulfone.