antitrypanosomal agent-1

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).

Antiulcer Agent 1 is a 2-(3,4-dimethoxyphenyl)ethylamine derivative for oral administration.

Acetic acid, 2-[4-[(2-ethyl-3-benzofuranyl)carbonyl]phenoxy]- is a compound used for antiviral activity determinations.

anti-TB agent 1 is a potent and orally active anti-tuberculosis agent (MICs: < 2 nM against the Mtb strains H37Rv, rRMP and rINH).

Anxiolytic/nonsedative agent-1 (TCS 1205) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo.

ethyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxylate is a synthetic compound belonging to the curcumin family. It is involved in the regulation of immune response and inflammation through inhibition of the NF-κB signaling pathway, in the regulation of antioxidant response through activation of the Nrf2 signaling pathway, and in the regulation of cell survival and proliferation through inhibition of the Akt signaling pathway.

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

Anticonvulsant agent 1 is an anticonvulsant compound.

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].

Therapeutic Agent-1, a heteroaryl compound, serves as an enzyme replacement therapy to enhance glucocerebrosidase activity in the treatment of Gaucher disease [1].

Compound 11, labeled as a weak Hepatoprotective agent-1, is a naturally occurring substance extracted from the fruits of Arctium lappa L. It demonstrates modest hepatoprotective effects when applied at a concentration of 10 μM [1].

Herbicidal agent 1 ((S)-6q) exhibits superior activity compared to its racemic form [1].

Insecticidal agent 1 exhibits greater insecticidal potency than both obacunone and toosendanin.

Antimalarial agent 1 is an effective antimalarial agent.

Compound 3, a molluscicidal agent, is a saponin extractable from S. vesicaria [1].

Ros-generating agent 1 has anticancer activity and generates ROS by covalently modifying Sec-498 residues of TrxR. ROS-generating agent 1 reduces intracellular TrxR protein levels and promotes ROs-dependent apoptosis and ferroptosis in NCI-H460 cells.

anti-TNBC agent-1 is a highly effective compound specifically designed to target and combat triple-negative breast cancer (TNBC). It demonstrates remarkable potency against various breast cancer cell types, with IC50 values spanning from 0.20 μM to 0.27 μM. The mechanism of action of anti-TNBC agent-1 involves inducing apoptosis in SUM-159 cells through the mitochondria pathway, as well as causing G1 phase arrest in these cells.

Anti-MI/R injury agent 1 (compound 18), derived from Panaxatriol, represents an orally administered, potent agent against myocardial ischemia/reperfusion (MI/R) injury. It improves cell viability in cardiomyocytes subjected to oxygen-glucose deprivation and reperfusion (OGD/R)-induced injury. Furthermore, this compound significantly reduces myocardial infarction size, diminishes levels of circulating cardiac troponin I (cTnI), and mitigates cardiac tissue damage in rat models [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 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-amyloid agent-1 is a potent compound that inhibits amyloid aggregation, offering a promising approach for research into the treatment of amyloidosis [1].

Compound 3l, a paclitaxel derivative known as Microtubule Stabilizing Agent-1, effectively enhances tubulin polymerization and demonstrates antitumor efficacy [1].

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

Anti-neurodegeneration agent 1 a neurodegeneration-targeting agent.

Antileishmanial agent-1 demonstrates activity against both L. amazonensis promastigotes (IC 50 = 15.52 μM) and intracellular amastigotes (IC 50 = 4.10 μM).

Anti-MRSA agent 1 is an MRSA inhibitor with an MIC value of 0.5 μg/mL and is effective in alleviating the effects of MRSA resistance.

Anti-melanoma agent 1 (Compound 5m) is an anti-melanoma agent that induces apoptosis.

Analgesic agent-1 is a potent analgesic that exhibits significant analgesic activity.

Anti-TSWV agent 1 is a highly effective inactivator (EC50:144 μg/mL) of tomato spotted wilt virus (TSWV).

Anti-osteoporosis agent-1 (comp 4aa) is an effective RPA (replication protein A) inhibitor, demonstrating potency with an IC50 value of 18 μM [1].

Lipid-lowering agent-1 is a potent lipid-lowering agent that significantly inhibits the pharmacological effects of low-density lipoprotein cholesterol (LDLC) and promotes the production of high-density lipoprotein cholesterol (HDLC).Lipid-lowering agent-1 significantly reduces fat in rats on a high-fat diet.

Anti-NASH Agent 1 (Compound 3d), derived from Elafibranor, serves as a strong PPAR-α/δ agonist aimed at treating nonalcoholic steatohepatitis (NASH). At dosages of 3-10 mg/kg over four weeks, this compound ameliorates hyperlipidemia, liver fat degeneration, and inflammation in a methionine-choline deficiency (MCD)-induced NASH mouse model, exhibiting minimal hepatotoxicity while providing substantial hepatic protection [1].

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

Anti-Heart Failure Agent 1 is an orally available compound suitable for the treatment of heart failure without inducing vomiting, nausea, and restlessness.

Anti-inflammatory agent 1 is an anti-inflammatory compound.

Bronchospasmolytic agent 1 is a flutropium bromide compound and acts as a bronchospasmolytic agent.

Anti-hyperglycemic agent 1 is a potent inhibitor of alpha-glucosidase (IC50: 0.53 μM). anti-Hyperglycemic agent 1 can be used to study diabetes.

Antiplatelet agent 1 is a ticagrelor analogue that exhibits anti-platelet effects and can be used in platelet agglutination studies.

Anti gram-positive/negative bacteria agent 1 is an antibiotic linked with a synthetic MECAM-based siderophore, serving as a conjugate aimed at combating gram-positive and gram-negative bacteria.

Anabolic agent-1 is a novel bone morphogenetic protein-2 up regulator, with the capability of rectifying bone loss in patients and exhibiting versatile clinical applicability.

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.

Hypoglycemic agent 1 has an action for lowering blood sugar. It acts as a therapeutic and/or prophylactic agent for diabetes.

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).

Anti-infective agent 1 (compound 3a) serves as a potent, selective antiprotozoal and antimycobacterial compound. It showcases antiparasitic efficacy against P. falciparum and T. brucei rhodesiense, demonstrating IC50 values of 10.95 and 0.06 μM, respectively. Moreover, it displays antimycobacterial properties against Mycobacterium smegmatis, exhibiting a minimum inhibitory concentration (MIC) of 8 μg/mL [1].

Antiallergic agent-1, an Src family kinase inhibitor, is a new and valuable lead compound with potential as an anti-allergic agent.

Anti-virus agent 1 (compound 4i), a phosphoramidate prodrug of GS-5734, exhibits potent antiviral efficacy. It is primarily utilized in the study of coronavirus and Ebola virus (EBOV).