Xenopsin precursor fragment is an antimicrobial peptide, and has antibacterial/antifungal (10-500 μg/mL) and anti-protozoal (MIC: 2-20 μg/mL) activity[1].
Tiprelestat is a potent human neutrophil elastase inhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease[1].
MA220607 is an antibacterial agent with low hemolytic toxicity and a dual-target mechanism of action (MOA). MA220607 promotes FtsZ protein polymerization, also increases the permeability of bacterial membranes and inhibits biofilm formation. The resistance rate of MA220607 is low, and the MICs against Gram-positive bacteria and Gram-negative bacteria are Table 0.062-2 μg/mL and 0.5-4 μg/mL, respectively)[1].
Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca2+ influx through voltage-gated Ca2+ channels, leading to the reduction in [Ca2+]i in vascular smooth muscle cells and consequent peripheral vasodilation[1]. Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM[2].
Faldaprevir (BI 201335) is a potent, orally active and selective noncovalent inhibitor of NS3/4A protease of HCV (hepatitis C virus) genotypes 1a and 1b, with Ki values of 2.6 and 2.0 nM, respectively. Faldaprevir inhibits HCV RNA replication, with EC50 values of 6.5 and 3.1 nM, respectively. Faldaprevir has potent antiviral activity against chronic HCV infection[1][2].
Avermectin B1a is an antiparasitic agent that paralyzes nematodes without causing hypercontraction or flaccid paralysis.
DMT-dC(ac) Phosphoramidite is a modified phosphoramidite monomer, which can be used for the oligonucleotide synthesis.
Pirlindole is a novel potent inhibitor of Enteroviruse that targets Viral Protein 2C, inhibits EV-B and EV-D through the inhibition of genome replication (CV-B3 EC50=9.91 uM).
Antileishmanial agent-11 (compound 4d) is a potent anti-leishmanial agent. Antileishmanial agent-11 shows antiprotozoal activity against Leishmania brazilensis, Leishmania infantum, and T. cruzi, with IC50 values of 28.3, 24.8 and 13.0 μM, respectively[1].
Cyclotriazadisulfonamide (CADA) is a specific CD4-targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibits the co-translational translocation of human CD4 (huCD4) into the ER lumen in a signal peptide (SP)-dependent way[1][2].
Hs-1 is an antimicrobial peptide displays 80% protection against the dengue-2 virus [1].
ND-011992 is a reversible, selective quinazoline-type inhibitor targeting quinone reductases and quinol oxidases. ND-011992 inhibits respiratory complex I and bo3 oxidase in addition to bd-I and bd-II oxidases in E. coli strain BL21*Δcyo with the IC50 of 0.12, 2.47, 0.63 and 1.3 μM, respectively. ND-011992 can be used for tuberculosis study[1].
Delafloxacin meglumine is a fluoroquinolone antibiotic agent.IC50 Value: MICs ranging from 0.0078 to 0.125 micro g/ml for levofloxacin-resistant Streptococcus pneumoniae strains [1]Target: AntibacterialABT-492 was more potent against quinolone-susceptible and -resistant gram-positive organisms, had activity similar to that of ciprofloxacin against certain members of the family Enterobacteriaceae, and had comparable activity against quinolone-susceptible, nonfermentative, gram-negative organisms.in vitro: ABT-492 exhibited excellent in vitro activities against all 326 aerobic and anaerobic antral puncture sinus isolates tested with MICs (in micrograms per milliliter) at which 90% of the isolates tested were inhibited as follows: Haemophilus influenzae, 0.001; Moraxella catarrhalis, 0.008; and Streptococcus pneumoniae, 0.015 [2]. ABT-492 was as active as trovafloxacin against Chlamydia trachomatis, indicating good intracellular penetration and antibacterial activity [3].in vivo:Clinical trial:
AWZ1066S is a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis, with an EC50 of 2.5 nM in cell assay[1].
Pancixanthone A is a xanthone that can be isolated from Garcinia vieillardii. Pancixanthone A has antimalarial activity against chloroquino-resistant strains of Plasmodium falciparum with an IC50 of 1.6 μg/mL[1].
Benzimidazole is a heterocyclic aromatic organic compound and acts as an important pharmacophore in medicinal chemistry. Benzimidazole derivatives have been reported to possess various biological activities such as anti-cancer, anti-viral, anti-bacterial, anti-fungal, anti-helmintic, anti-inflammatory, proton pump inhibitor and anti-coagulant property[1][2][3].
Penciclovir (VSA 671) sodium is a potent and selective anti-herpesvirus agent with EC50 values of 0.5, 0.8 µg/ml for HSV-1 (HFEM), HSV-2 (MS), respectively. Penciclovir sodium shows anti-herpesvirus activity with no-toxic. Penciclovir sodium preventes mortality in mouse[1][2].
Malonomicin (Antibiotic K16) is an antibiotic with anti-protozoa and anti-trypanosome activities. Malonomicin also shows anti-trypanosome activity in vivo[1][2].
Baquiloprim-d6 is deuterium labeled Baquiloprim. Baquiloprim, an antibiotic, is a selective inhibitor of bacterial dihydrofolate reductases. Baquiloprim possesses in vitro bacteriostatic activity against both Gram-negative and Gram-positive bacteria[1][2].
Cyclo(L-Pro-L-Val) is a 2,5-diketopiperazine, with toxic activity against phytopathogenic microorganisms (such as R. fascians LMG 3605). Cyclo(L-Pro-L-Val) shows toxicity similar to Chloramphenicol (HY-B0239) with comparable concentration. Cyclo(L-Pro-L-Val) can also inhibit gram-positive phytopathogenic bacterium. Cyclo(L-Pro-L-Val) has potential development as biopesticide[1].
Indinavir sulfate ethanolate (MK-639 ethanolate) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate ethanolate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate ethanolate is also a SARS-CoV 3CLpro inhibitor[1][2][3][4].
lsocryptomerin is a membrane-active antifungal compound that can be isolated from Selaginella tamariscina. lsocryptomerin can depolarize fungal plasma membrane. lsocryptomerin also shows anticancer and antibacterial activities[1][2].
Maximin 9 is an antimicrobial peptide derived from toad Bombina maxima[1].
SARS-CoV-2-IN-12 (Compound 27) is a potent SARS-CoV-2-related 3C-like protease inhibitor (Ki=32.1 pM) for preventing SARS-CoV-2 viral replication and that could be useful in the research of COVID-19[1].
Clorobiocin is a MlaC protein inhibitor that could bind to the MlaC protein. Clorobiocin has antibacterial effects[1].
Resveratrol (SRT 501), a natural polyphenol that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. It has a wide spectrum of targets including mTOR, JAK, β-amyloid.
Banksialactone A is the metabolite of an Australian fungus, Aspergillus banksianus[1].
Chamaejasmenin C, a biflavanone, shows nematicidal activity against second-stage juveniles (J2s) of B. xylophilus and B. mucronatus[1][2].
A potent RIG-I-like receptor (RLR) agonist that triggers IRF3-dependent innate immune antiviral genes and IFN-β expression; shows antiviral activity against a broad range of RNA viruses, including dengue virus, and hepatitis C virus, as well as viruses of the families Filoviridae (Ebola virus), Orthomyxoviridae (influenza A virus), Arenaviridae (Lassa virus), and Paramyxoviridae (respiratory syncytial virus, Nipah virus).
Triptonine B, a sesquiterpene pyridine alkaloid that isolated from Tripterygium hypoglaucum and Tripterygium wilfordii, inhibits HIV replication in H9 lymphocytes with an EC50 value of <0.10 μg/mL[1].