antitrypanosomal agent 2

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

Antitumor agent-2 has anti-inflammatory and anti-tumor activity and can be used to study cancer.

Anticonvulsant agent 2 is a potent, orally active anticonvulsant demonstrating antiepileptic activity in a drug-resistant epilepsy model.

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

Analgesic Agent-2, a selective orally active inhibitor of the NaV1.8 channel, demonstrates an IC50 of 50.18 nM in HEK293 cells that stably express the human NaV1.8 channel, indicating its potential for analgesic activity [1].

Compound 56 (Antidiabetic agent 2) is a glucose-uptake promoter that inhibits DPP-4, PTP-1B, α-amylase, and α-glucosidase, with IC50 values of 0.036, 0.042, 0.241, and 0.185 μM, respectively. This agent effectively decreases blood glucose levels [1].

Antiplatelet agent 2 is a ticagrelor analogue that exhibits anti-platelet effects and can be used in platelet agglutination studies.

Anti-MRSA agent 2 (compound 14) is a potent inhibitor of methicillin-resistant Staphylococcus aureus (MRSA) (MIC: 0.098 μg ml), exhibiting relatively low toxicity to normal cells. It strongly disrupts bacterial membranes and effectively binds to bacterial genomic DNA.

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

N-(4-Isopropyloxy phenyl)-N-(1H-pyrrol-2-ylmethyl)urea; flavoring agent, flavor modifier is a useful organic compound for research related to life sciences and the catalog number is TNU1282.

Antihypertensive agent 2 (Compound 4g) effectively antagonizes angiotensin II receptor 1 and reduces blood pressure with potency equal to or greater than Losartan [1].

The antitrypanosomal agent 8 (compound 3b) demonstrated a potent effect against Trypanosoma brucei with an IC50 of 0.79 μM, while the IC50 value was 80.95 μM.

Antimalarial agent 2 is an orally active, novel antimalarial agent that exhibits rapid in vitro killing effects.

Antipsychotic agent-2 (Compound 11) is a potent antipsychotic with high affinities for 5-HT1A, 5-HT2A, 5-HT2C, D2, and H1 receptors, exhibiting Ki values of 56.6, 66.7, 552, 596, and 1140 nM, respectively. It also possesses blood-brain barrier (BBB) permeability [1].

Antiangiogenic agent 2 (compound 3b) is a potent thymidine phosphorylase inhibitor (IC50: 39.71 μM) with demonstrated anti-angiogenic effects.

Antimicrobial agent-2 (compound V-a) is a broad-spectrum antimicrobial agent effective against various Gram-positive and Gram-negative bacteria, with low toxicity, no obvious resistance, and good bioavailability. It damages the membrane, leading to protein leakage and inducing ROS production. It notably inhibits Methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 1 μg mL [1].

Antituberculosis agent-2 (Compound 8d) is effective against both multidrug-resistant and drug-sensitive tuberculosis, exhibiting favorable microsomal stability in mouse and human, low cytotoxicity, and acceptable oral bioavailability. The MIC values against M. tuberculosis H 37 R v, 13946, and 14862 are 0.454, 1.757, and 1.644 μg mL, respectively [1].

Antitrypanosomal agent 6 (compound 18a) is a potent antitrypanosomal agent demonstrating good ADME properties, with an IC50 of 0.47 μM against Trypanosoma brucei (T. brucei), making it more than twice as active as Nifurtimox; it also exhibits a strong interaction with and selective binding to AT-rich DNA.

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

Insecticidal agent 2 (example 2) is an effective pesticide that significantly inhibits pest growth [1].

GABAA receptor agent 2 TFA is a potent, high-affinity GABAA receptor antagonist with an IC50 of 24 nM [human α1β2γ2GABAA-expressing tsA201 cells] and a Ki of 28 nM [rat GABAA receptor]. GABAA receptor agent 2 TFA has no effect on four human GABA transport proteins [hGAT-1, hBGT-1, hGAT-2, and hGAT-3].

Antifungal agent 2 is a broad-spectrum inhibitor effective against Cryptococcus, Candida, and Aspergillus species, inhibiting growth at concentrations as low as 0.5 μg mL.

P-CAB agent 2 hydrochloride is a potent, orally active potassium-competitive acid blocker (P-CAB) and gastric acid secretion inhibitor. It effectively inhibits H+ K+-ATPase activity, with an IC50 value of <100 nM, and targets the hERG potassium channel with an IC50 value of 18.69 μM. Moreover, P-CAB agent 2 hydrochloride demonstrates no acute toxicity and effectively inhibits histamine-induced gastric acid secretion [1].

Antiparasitic agent-2 (compound 8a) exhibits potent antiparasitic activity against Leishmania infantum (L. infantum) and Trypanosoma cruzi (T. cruzi) with IC50s of 7.28 μM and 2.30 μM, respectively, and demonstrates moderate cytotoxicity against HepG2 cells with a CC50 of 26.79 μM [1].

Anti-infective agent 2 (compound 3k) is an antiprotozoal and antimycobacterial agent. It exhibits antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 0.07 and 2.20 μM, respectively, and shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 32 μg mL [1].

Antidepressant agent 2 showed significant antidepressant effects with a MED value of 0.1 mg/kg.

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

Compound 6k, also known as Anti-hepatic fibrosis agent 2, is an orally active inhibitor of the COL1A1 enzyme and exerts anti-fibrogenic effects by targeting the Ewing sarcoma breakpoint region 1 (EWSR1)[1].

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.

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].

Apoptotic agent-2 is capable of downregulating Bcl-2 and upregulating Bax and caspase-3 to induce apoptosis, exhibiting anti-proliferative effects that can be used in cancer research.

Antistaphylococcal agent 2 is an anti-staphylococcal therapeutic agent.

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).

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 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].

Anti-TNBC agent-2 (3j), a purine derivative, acts as an anti-triple negative breast cancer (TNBC) therapeutic. It promotes apoptosis in MDA-MB-231 cells, while also inhibiting their migration and angiogenesis. Moreover, anti-TNBC agent-2 suppresses tumor growth and metastasis, and downregulates Ki67 and CD31 protein expression in TNBC xenograft models. It may be utilized for TNBC research [1].

Antimycobacterial agent-2 is an effective anti-mycobacterial agent with a MIC99 of 0.8 μM against Mycobacterium tuberculosis (M.tb) H37Rv. Antimycobacterial agent-2 is cytotoxic, acting on CHO cells (IC50: 48.1 μM).

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.

Antioxidant agent-2 (comp 3c), a BBB-penetrating and selective metal ion chelator, exhibits significant neuroprotective and hepatoprotective effects, making it beneficial for Alzheimer’s disease research.

P-CAB Agent 2 is a potent, orally active potassium-competitive acid blocker (P-CAB) and gastric acid secretion inhibitor that effectively inhibits H+/K+-ATPase activity, showing an IC50 value of <100 nM. It also demonstrates inhibition of the hERG potassium channel with an IC50 value of 18.69 M, indicating no acute toxicity. P-CAB Agent 2 effectively curbs histamine-induced gastric acid secretion [1].

Antiulcer Agent 2, a tetrapeptide comprising aspartic acid, alanine, histidine, and lysine, localizes at the N-terminal of human albumin. This compound shows promise in treating ulcers and producing active oxygen [1] [2].

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].

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

Antibiofilm Agent-2 (Compound 4T) serves as a potent biofilm inhibitor, exhibiting an IC50 of 3.6 μM, and impairs the quorum sensing system along with iron homeostasis, acting as antibacterial synergists against Pseudomonas aeruginosa [1].