Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor with an IC50 of 3.3 μM. Antitrypanosomal agent 1 inhibits glutathione reductase (GR) (IC50=64.8 μM) and T. brucei (EC50=1 μM). Antitrypanosomal agent 1 has anti-trypanosomal activity[1].
Cephalexin-d5 is deuterium labeled Cephalexin. Cephalexin (Cefalexin; Cephacillin) is a potent, orally active and the first-generation cephalosporin antibiotic. Cephalexin kills gram-positive and some gram-negative bacteria by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of pneumonia, strep throat, and bacterial endocarditis, et al[1].
Urease-IN-10 (Conjugate 4) is a competitive Urease inhibitor, with an IC50 of 3.59±0.07 μM and a Ki of 7.45 μM. Urease-IN-10 is a conjugate consisting of Diclofenac (HY-15036) and Sulfanilamide (HY-B0242). Diclofenac-sulfanilamide inhibits the Jack bean urease(JBU) in a competitive manner[1].
Emamectin Benzoate (MK-244) works as a chloride channel activator by binding gamma aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods.
1-Methyl-2-pentyl-4(1H)-quinolinone, a quinolone alkaloid isolated from the fruits of Evodia Rutaecarpa, possesses antibacterial and cytotoxic activities for cancer cells[1].
GCA-186 is a potent anti-HIV-1 agent. GCA-186 is highly active against both wild type and mutated HIV-1 strains with EC50s of 1, 180, 1, and 40 nM for IIIB, IIIB-R(Y181C), NL4-3 and NL4-3K103N of HIV-1 strains, respectively[1].
Licoflavonol, a minor flavone from the roots of Glycyrrhiza uralensis, is an inhibitor of the Salmonella type III secretion system (T3SS)[1][2].
Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir sodium inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir sodium also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir sodium inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][4].
Dexamethasone-d4 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
GVLSNVIGYLKKLGTGALNAVLKQ is an antimicrobial peptide with 24-amino acid. GVLSNVIGYLKKLGTGALNAVLKQ can potentially form α-helix. GVLSNVIGYLKKLGTGALNAVLKQ (PGQ) has activity against Gram-negative, Gram-positive bacteria and the yeast Candida albicans[1].
13C-urea is the 13C labelled urea. The 13C-urea breath test (13C-UBT) is one of the best methods for the diagnosis of Helicobacter pylori infection[1].
Cefetamet is a cephalosporin antibiotic. Cefetamet has the potential for the research of both upper and lower community-acquired respiratory tract infections[1].
4-O-Methylepisappanol (compound 9) is nature product that could be isolated from heartwood of Caesalpinia sappan. 4-O-Methylepisappanol is a potent neuraminidase inhibitor on the surface of influenza viruses with IC50 values of 42.8, 63.2, and 63.2 µM for A/Chicken/Korea/MS96/96 [H9N2], A/PR/8/34 [H1N1], and A/Hong Kong/8/68 [H3N2], respectively[1].
Cilastatin-15N,d3 is a 15N-labeled and deuterium labeled Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct[1][2][3].
AX20017 is a small-molecule protein kinase G (PknG) inhibitor with an IC50 of 0.39 μM.
Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics[1][2][3].
BDM91514 improves antibiotic potency through AcrB inhibition. BDM91514 prevents the growth of E. coliBW25113 (EC90: 8 μM) in the presence of 8 μg/mL Pyridomycin. BDM91514 has suitable plasma and microsomal stability[1].
Olanexidine hydrochloride semihydrate is an antibacterial agent. Olanexidine hydrochloride semihydrate is active against a wide range of bacteria, imcluding both Gram-positive and Gram-negative bacteria Olanexidine hydrochloride semihydrate is also an antiseptic. Olanexidine hydrochloride semihydrate can be used in the research of infection and inflammation[1][2][3].
DSM265 is a PfDHODH inhibitor with an IC50 of 8.9 nM. DSM265 can also inhibit the growth of P. falciparum 3D7 parasites with an EC50 of 4.3 nM.
5'-O-TBDMS-dT is a nucleoside with protective and modification effects.
SARS-CoV-2 3CLpro-IN-2 (Compound 1) is a potent inhibitor of 3CL protease. SARS-CoV-2 3CLpro-IN-2 has the potential for the research of SARS-CoV-2 diseases[1].
Antitubercular agent-12 (Compound 2c) is an antitubercular agent (MIC = 1.439 μg/mL). Antitubercular agent-12 shows greatly lower cytotoxicity (CC50: 57.34 μg/mL)[1].
Lasalocid is an antibacterial agent and a coccidiostat, used in the feed additives
Penflufen is a highly efficient, broad-spectrum succinate dehydrogenase inhibitor (SDHI). Penflufen can be used as a fungicide and has broad bioactivity against many fungal diseases, including potato black scurf, wheat sharp eyespot, rice sheath blight, and root rot in peanut and other similar fungal diseases[1].
8-Abietenic acid is the secondary metabolite of mucorinic acid and is isolated from a solid culture of the fungus Mucor spp. isolated on insect Acalymma bivittula. 8-Abietenic acid exhibits antibacterial and insecticidal activities[1].
1,3,5-Tricaffeoylquinic acid is a tricaffeoylquinic acid derivative isolated from H. populifolium with anti-HIV effect[1].
Ganciclovir (INN) is an antiviral medication used to treat or prevent cytomegalovirus (CMV) infections. Ganciclovir is a synthetic analogue of 2′-deoxy-guanosine. It is first phosphorylated to ganciclovir monophosphate by a viral kinase encoded by the cytomegalovirus (CMV) gene UL97 during infection. Subsequently, cellular kinases catalyze the formation of ganciclovir diphosphate and ganciclovir triphosphate, which is present in 10-fold greater concentrations in CMV or herpes simplex virus (HSV)-infected cells than uninfected cells. A prodrug form with improved oral bioavailability (valganciclovir) has also been developed.
Antibacterial agent 18 is a multi-arm AIE molecule extracted from patent CN110123801A, compound 23. Antibacterial agent 18 can be used for resisting Gram-positive and Gram-negative bacteria. Antibacterial agent 18 can be conjugated in the cell wall of rigid arm configuration insertion bacterium, and block cell wall turns sugar and turns peptide process, to inhibit or kill bacterium[1].
SB-734117 is a human cytomegalovirus (HCMV) replication inhibitor that prevents CREB and histone H3 post-translational modifications[1].
Lupenone, isolated from Rhizoma Musae, belongs to lupane type triterpenoids. Lupenone shows various pharmacological activities including anti-inflammatory, anti-virus, anti-diabetes, anti-cancer, improving Chagas disease without major toxicity[1][2].