Trypanosoma Inhibitor

Eflornithine hydrochloride hydrate (DFMO hydrochloride hydrate) is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine hydrochloride hydrate is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.

Diminazene aceturate (Diminazene diaceturate) is an anti-trypanosome agent for livestock. The main biochemical mechanism of the trypanocidal actions of Diminazene aceturate is by binding to trypanosomal kinetoplast DNA (kDNA) in a non-intercalative manner through specific interaction with sites rich in adenine-thymine base pairs. Diminazene aceturate is also an angiotensin-converting enzyme 2 (ACE2) activator and has strong and potent anti-inflammatory properties.

Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC₅₀ of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC₅₀ of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.

Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC₅₀ of 6.5 nM and K_d of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity.

Enfiborole is an oxaborolane ester inhibitor with trypanocidal activity against parasites. Enfiborole displays IC₅₀ values ≤ 20 nM against Trypanosoma brucei and Trypanosoma cruzi, and its IC₅₀ against replicating trypanosomes ranges from 21 to 999 nM. Enfiborole inhibits the growth of Trypanosoma brucei, suppresses hypoxanthine incorporation in replicating trypanosomes, and inhibits the growth of Trypanosoma cruzi amastigotes. Enfiborole can be used in studies related to trypanosome infections.

Naringenin 4',7-dimethyl ether, Naringenin (HY-N0100) derivative is an anti-seizure agent. Naringenin 4',7-dimethyl ether attenuates pentylenetetrazole-induced seizures in larval zebrafish and reduces seizures in the mouse 6-Hz psychomotor seizure model. Naringenin 4',7-dimethyl ether can be used for the research of epilepsy. Naringenin 4',7-dimethyl ether is an active agent against Leishmania mexicana (17.8 µM) and Trypanosoma brucei (17.5 µM).

Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC₅₀ of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

SQ109 is a potent inhibitor of the trypomastigote form of the parasite, with IC₅₀ for cell killing of 50±8 nM. SQ109, targets MmpL3, is an antitubercular agent.

K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC₅₀ of 60 nM. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC₅₀ values of 0.68 nM and 0.87 nM, respectively.

Acoziborole (SCYX-7158) is an effective, safe and orally active antiprotozoal agent for the research of human african trypanosomiasis (HAT). In the T. b. brucei S427 strain, the MIC value for SCYX-7158 is 0.6 μg/mL.

trans-4-Methylcyclohexanamine is an organic amine compound that can be used in the development of T. cruzi enzyme inhibitors.

Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with K_d values of 1.2 μM and 1.4 μM for Trypanosoma brucei (TB) and human CYP51, respectively.

N-p-trans-Coumaroyltyramine is a natural phenolic amide compound and an inhibitor of AChE (IC₅₀: 122 μM) and α-glucosidase (IC₅₀: 2.7 μM). N-p-trans-Coumaroyltyramine also has anti-trypanosomal activity, with an IC₅₀ of 13.3 µM against T. brucei rhodesiense. N-p-trans-Coumaroyltyramine can be used in the research of diseases such as Alzheimer's disease.

Benznidazole (Ro 07-1051) is an antiparasitic medication, with an IC₅₀ of 20.35 μM for Colombian T. cruzi strains, and has been used in the treatment of Chagas disease.

Harpagide is a class of iridoid glycoside isolated from Scrophularia ningpoensis and has antiparasitic activity, which exhibits good in vitro trypanocidal activities against African trypanosomes (T.b. rhodesiense) with an IC₅₀ of 21 μg/mL. Harpagide exerts significant antileishmanial activity against L. donovani with an IC₅₀ value of 2.0 μg/mL. Harpagide also possess significant anti-inflammatory activities.

Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal agent. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC₅₀s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei.

Ajugol is an orally active iridoid glycoside found in the traditional Chinese medicine Leonurus japonicus. Ajugol is an autophagy activator. Ajugol activates TFEB-mediated autophagy and lysosomal biogenesis. Ajugol also has anti-inflammatory effects. Ajugol has great potential in the research of asthma, non-alcoholic fatty liver disease (NAFLD), and osteoarthritis.

NPD-001 is a potent Trypanosoma brucei phosphodiesterases 1/2 (TbrPDEB1/2) inhibitor, with IC₅₀ values of 4 and 3 nM, respectively. NPD-001 also inhibits hPDE4. NPD-001 can increase cAMP levels in parasites, prevent cytokinesis, and cause the parasites to form multinucleated, multi-flagellated cells that eventually lyse. NPD-001 can be used for the research of infection.

Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria.