antitrypanosomal

Antitrypanosomal agent 2 shows potent and specific antiparasite activities against Trypanosoma brucei.

Compound 18 (compound 8b), a nitrofuran derivative, exhibits potent in vitro trypanocidal activity, with an IC50 value of 0.03 μM [1].

Compound 17 (Compd 7a) exhibits potent antiamastigote activity, demonstrated by its IC50 value of 0.03 μM against the T. congolense strain IL3000 [1].

Antitrypanosomal agent 16 functions as a potent trypanocide, exhibiting an inhibitory concentration 50 (IC50) of 0.04μM against the T. congolense strain IL3000 [1].

Compound 4b (antitrypanosomal agent 13) is a potent antitrypanosomal with notable trypanocidal and cytotoxic activities, exhibiting GI50 values of 0.18 μM against T. brucei and 8.4 μM for HL-60 [1].

Antitrypanosomal agent 14 (Compound 1), a potent T. brucei inhibitor with an effective concentration (EC50) of 0.47 μM, also inhibits Tb GSK3 with an inhibitory concentration (IC50) of 12 μM, and is utilized in the research of Human African Trypanosomiasis [1].

Antitrypanosomal Agent 15 (Compound 26) is an orally active, brain-penetrant, selective inhibitor of the Trypanosoma cruzi proteasome, exhibiting a pIC50 of 7.4 for T. cruzi and <4 for the human proteasome. It possesses favorable ADME properties, rendering it useful for the study of Chagas disease [1].

Antitrypanosomal agent 9 is a potent compound with inhibitory activity against T. b. brucei, exhibiting an IC50 of 1.15 μM. It is utilized in research for human African trypanosomiasis (HAT).

Antitrypanosomal agent 4 (compound 19) is a potent antitrypanosomal agent that crosses the blood-brain barrier and shows good resistance to Trypanosoma cruzi and T. b. brucei with IC50 values of 1.2 μM and 70 nM respectively.

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).

The Antitrypanosomal agent 7 (compound 18c) is a potent anti-trypanosome agent and shows good ADME properties. The Antitrypanosomal agent 7 was more than two-fold more active against T. brucei (IC50: 0.71 μM) than Nifurtimox. Antitrypanosomal agent 7 has a strong interaction with DNA and can selectively bind to AT-rich DNA.

Antitrypanosomal agent 8 (compound 3b) showed a strong antitrypanosomal effect against Trypanosoma brucei (IC50: 0.79 μM). The IC50 value was 80.95 μM.

Antitrypanosomal agent 6 (compound 18a) is a potent antitrypanosomal agent showing good ADME properties. Antitrypanosomal agent 6 is more than twice as active as Nifurtimox against Trypanosoma brucei (T. brucei) with an IC50 of 0.47 μM. Antitrypanosomal agent 6 has a strong interaction with DNA and selectively binds AT-rich DNA.

Antitrypanosomal agent 12, a C20-phenylthiourea, exhibits trypanocidal and cytotoxic activities, demonstrating antitrypanosomal activity with GI50 values of 0.22 μM. It induces faster cell swelling in bloodstream-form trypanosomes compared to Salinomycin [1].

Antitrypanosomal Agent 11 is a chemical compound effective against Trypanosoma cruzi, exhibiting an inhibition concentration (IC 50) of 0.23 μM.

Antitrypanosomal agent 10, an antitrypanosomal compound, effectively inhibits Trypanosoma cruzi with an IC50 of 0.28 μM.

Antitrypanosal agent 5 is a selective anti-trypanosomal agent that acts on T. brucei (IC50: 1 nM) and HEK293 cells (IC50: 483.3 μM).

Puromycin dihydrochloride (CL13900 dihydrochloride) is a cinnamamide adenosine antibiotic and an inhibitor of protein synthesis. Puromycin dihydrochloride inhibits protein synthesis by binding to RNA and has antitumor and antitrypanosomal activity.

Girinimbine (Girinimbin) is a carbazole alkaloid isolated from the plants M. koenigii, M. koenigii and Murraya koenigii.Girinimbine has a wide range of biological effects, including apoptosis, antitrypanosomal, antiplatelet, antimicrobial, anti-inflammatory, antioxidant and antitumor activities. Girinimbine has a variety of biological effects, including apoptosis, antitrypanosomal, antibacterial, anti-inflammatory, antioxidant and antitumor activities.

SDZ285428 is a CYP24A1 inhibitor.

Puromycin (NSC-3055) is an antibiotic protein synthesis inhibitor. It inhibits protein synthesis by binding to RNA. It also serves as an anticancer drug by suppressing the growth and metastasis in esophagus cancer cells by Akt phosphorylation. It is an antineoplastic and antitrypanosomal agent and is used in research as an inhibitor of protein synthesis.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Methylenetanshinquinone shows antiplasmodial and antitrypanosomal activity, it is active against both Trypanosoma brucei rhodesiense and Plasmodium falciparum.

Dehydrobruceine A shows strong antitrypanosomal activities with IC(50) values in the range of 2.9-17.8nM.

Nucleocidin, an antitrypanosomal antibiotic, inhibits the transfer of labeled amino acids from S-RNA to protein.

Carviolin is an anthraquinone fungal metabolite that has been found inZ. longicaudatawith immunosuppressive and antitrypanosomal activities.1,2It inhibits LPS- or concanavalin A-induced proliferation of mouse splenocytes (IC50s = 4 and 4.5 μg/ml, respectively).1Carviolin is active againstT. b. brucei(MIC = 41.66 μM).2 1.Fujimoto, H., Nakamura, E., Okuyama, E., et al.Six immunosuppressive features from an ascomycete, Zopfiella longicaudata, found in a screening study monitored by immunomodulatory activityChem. Pharm. Bull. (Tokyo)52(8)1005-1008(2004) 2.Aly, A.H., Debbab, A., Clements, C.M., et al.NF kappa B inhibitors and antitrypanosomal metabolites from endophytic fungus Penicillium sp. isolated from Limonium tubiflorumBioorg. Med. Chem.19(1)414-421(2011)

Salviandulin E, a diterpenoid isolated from Salvia leucantha CAV., exhibits antitrypanosomal activity against T. b. brucei GUTat 3.1 parasites, demonstrating an IC50 value of 0.72 µg/mL [1] [2].

Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decreases phorbol 12-myristate 13-acetate (TPA)- and ionomycin-induced increased expression of COX-2 (IC50= 1 μM) and protein levels of IL-2 in Jurkat cells (IC50= 5.2 μM).1 1.Rether, J., Serwe, A., Anke, T., et al.Inhibition of inducible tumor necrosis factor-α expression by the fungal epipolythiodiketopiperazine gliovirinBiol. Chem.388(6)627-637(2007) 2.Howell, C.R., and Stipanovic, R.D.Gliovirin, a new antibiotic from Gliocladium virens, and its role in the biological control of Pythium ultimumCan. J. Microbiol.29(3)321-324(1983) 3.Iwatsuki, M., Otoguro, K., Ishiyama, A., et al.In vitro antitrypanosomal activity of 12 low-molecular-weight antibiotics and observations of structure/activity relationshipsJ. Antibiot. (Tokyo)63(10)619-622(2010)

Camaric acid shows antibacterial activity against Staphylococcus aureus and methicillin resistant S. aureus with IC50 values 8.74 and 8.09 uM, respectively, it also shows moderate antileishmanial activity and highly potent antitrypanosomal activity. Camar

Fexinidazole (HOE 239) is an antiparasitic agent. It has 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.

NPD-2975 (compound 30) is an orally active antitrypanosomal agent effective against Human African Trypanosomiasis (HAT), demonstrating acceptable metabolic stability and low toxicity potential in human MRC-5 lung fibroblasts, as well as in an acute mouse model of T. b. brucei infection. It inhibits T. b. brucei with an in vitro IC50 of 70 nM and yields IC50 values of 0.16 μM and 0.42 μM against CYP1A2 and CYP2C19 enzymes, respectively [1].

7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) has anti-inflammatory, antibacterial and antifungal activities, it also shows moderate antitrypanosomal activity with MIC value of 19.0 ug/ml

Chrysosplenol D, an efflux pump inhibitor that can potentiate the activity of commercially important antibiotics and antimalarials.

Euphorbadienol is a triterpenic compound isolated from the latex of Euphorbia resinifera. It has antileishmanial and antitrypanosomal activity.