Artemether is an antimalarial for the treatment of resistant strains of falciparum malaria.Target: AntiparasiticArtemether is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with lumefantrine for improved efficacy. Artemether exhibits the highest activity against juvenile stages of the parasites, while adult worms are significantly less susceptible. There was no indication of neurotoxicity following repeated high doses of artemether given fortnightly for up to 5 months. Artemether-integrated with other control strategies-has considerable potential for reducing the current burden of schistosomiasis in different epidemiological settings [1]. There were remarkably inhibitory effects of artmeter on brain glioma growth and angiogenesis in SD rats and the mechanism that artemether inhibited brain glioma growth might be penetrating the blood-brain barrier and inhibiting angiogenesis [2].
RSV604 is a novel inhibitor of respiratory syncytial virus replication(EC50=0.86 uM); a putative RSV nucleoprotein(N) inhibitor in phase 2 clinical trials.IC50 value: 0.86 uM(EC50) [1]Target: RSV inhibitorRSV604, a novel benzodiazepine with submicromolar anti-RSV activity. It proved to be equipotent against all clinical isolates tested of both the A and B subtypes of the virus. The compound has a low rate of in vitro resistance development. Sequencing revealed that the resistant virus had mutations within the nucleocapsid protein. This is a novel mechanism of action for anti-RSV compounds. In a three-dimensional human airway epithelial cell model, RSV604 was able to pass from the basolateral side of the epithelium effectively to inhibit virus replication after mucosal inoculation. RSV604, which is currently in phase II clinical trials, represents the first in a new class of RSV inhibitors and may have significant potential for the effective treatment of RSV disease.
3,5-Dimethoxybenzoic acid, isolated from Melia azedarach L. leaves with antifungal activity, is an intermediate in organic synthesis[1].
DNDI-8219 is a novel potent, orally active antileishmanial agent with IC50 of 0.19 uM against Leishmania donovani (L. don); also has IC050 of 0.53 and 0.15 uM against L. inf and T. cruzi, displayes promising activity in the more stringent Leishmania infantum hamster model, with better solubility and pharmacokinetic properties, as well as minimal hERG inhibition.
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
Isoaltenuene is an anti-bacterial agent with moderate activity against Staphylococcus aureus. Isoaltenuene can be isolated from fungus Alternaria alternate cib-137[1].
Fosmidomycin sodium salt is a phosphonic acid antibiotic and a antimalarial drug, which is active against both Gram-negative and Gram-positive bacteria.
Erythrocentaurin, a natural compound, is a new class of hepatitis B virus inhibitor[1].
DHODH-IN-8 (Compound 27) is an inhibitor of human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) with IC50s of 0.13 μM and 47.4 μM, and Kis of 0.016 μM and 5.6 μM, respectively. DHODH-IN-8 has antimalarial activity[1].
(R)-Larotrectinib is a potent TRK inhibitor with an IC50 value of 28.5 nM for TrkA. (R)-Larotrectinib can be used for researching cancer, inflammatory and certain infectious diseases[1]
Antibacterial agent 56 (example 22) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Arasertaconazole is a potent 14α-lanosterol demethylase inhibitor. Arasertaconazole has antifungal and antibacterial activity[1].
iHCK-37 (ASN05260065) is a potent and specific Hck inhibitor with a Ki value of 0.22 μM. iHCK-37 blocks HIV-1 viral replication with an EC50 value of 12.9 μM. iHCK-37 is used for chronic myeloid leukemia (CML) research[1].
HCoV-OC43-IN-1 (Compound IV-16) is a coronavirus HCoV-OC43 inhibitor. HCoV-OC43-IN-1 has antiviral efficacy (EC50: 90 nM). HCoV-OC43-IN-1 inhibits the mRNA level and expression of viral nucleocapsid protein (NP)[1].
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes[1]. Enniatin B1 crosss the blood-brain barrier[2]. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation[3].
PF429242 is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC50 of 175 nM[1].
LANA-DNA-IN-1 is a potent LANA-DNA inhibitor. LANA-DNA-IN-1 has inhibition activity for LBS2, LBS1 and LBS3 with IC50 values of 8 μM, 9μM and 8μM. LANA-DNA-IN-1shows against wild-type LANA with IC50 value of 53 μM. LANA-DNA-IN-1 can be used for the research of infection[1].
Zanamivir–cholesterol conjugate is a long-acting neuraminidase inhibitor with potent efficacy against drug-resistant influenza viruses.
2',3'-Dehydrosalannol is a potent antibacterial agent. 2',3'-Dehydrosalannol shows antibacterial activity against K. pneumonia ATCC 13883, P. aeruginosa ATCC 27853, S. aureus ATCC 25922, E. coli ATCC 11775, and E. faecalis ATCC 10541, with MIC values of 0.78, 1.56, 1.56, 6.25, and 25 µg/mL, respectively[1].
Enterotoxin STp (E. coli) is a heat-stable enterotoxin that can be used in vaccine research[1].
Loracarbef hydrate, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class[1][2].
(R)-(-)-α-Phellandrene ((-)-α-Phellandrene) is an the (R)-(-)-stereoisomer of α-phellandrene. α-phellandrene is an orally active cyclic monoterpene that attenuates inflammatory response, and induces DNA damage[1][2][3].
4'-Hydroxy-2,4-dimethoxychalcone is a natural chalcone derivatives in the red herbal resin of Dracaena cochinchinensis. 4'-Hydroxy-2,4-dimethoxychalcone displays a wide range of biological activities including antimalarial, antiprotozoal, antibacterial, antifungal activity[1][2].
Lesofavumab (MHAB5553A) is a human IgG1κ anti-influenza B virus antibody[1].
Hydroxychloroquine sulfate is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling.
UGM-IN-3 (compound 10a) is a UDP-galactopyranose mutase (UGM) inhibitor with a Kd of 66 μM. UGM-IN-3 inhibits the growth of Mycobacterium tuberculosis with a MIC value of 6.2 μg/mL[1].
Riodoxol is an antiviral agent. Riodoxol affects multiplication and maturation of the virus[1].
Isomangiferin, a natural product, is reported to have antiviral activity.
Cepharanthine, an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities[1][2][3]. Cepharanthine attenuates muscle and kidney injuries induced by limb ischemia/reperfusion (I/R)[3]. Cepharanthine induces autophagy, apoptosis and cell cycle arrest in breast cancer cells[4]. Cepharanthine inhibits the HIV-1 entry process by reducing plasma membrane fluidity[5].
S-F24 is an antifungal agent with excellent broad-spectrum. S-F24 inhibits CYP3A4 with an IC50 value of 0.4 μM. S-F24 displays a good safety profile with high selectivity, low hemolytic effects, and low tendency to induce resistance. S-F24 can be used for research on fungal infections[1].