Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties[1].
Metalaxyl-M-d6 is the deuterium labeled Metalaxyl-M[1]. Metalaxyl-M ((R)-Metalaxyl) is the active (R)-enantiomer of Metalaxyl. Metalaxyl-M is a broad-spectrum fungicide that inhibits protein and ribosomal RNA synthesis in?fungi. Metalaxyl is used for research of plant diseases caused by pathogens of the Oomycota division[2].
Piperacillin sodium is a broad-spectrum β-lactam antibiotic.
Mipeginterferon alfa-2b is an interferon alpha-2b (IFNA2b) analogue, with an average number of 5 substituted among 11 amino groups (one N-terminal and 10 lysine N6). Mipeginterferon alfa-2b has the relative molecular mass of 40 kDa[1].
Levonadifloxacin ((S)-(-)-Nadifloxacin; WCK 771) is a broad-spectrum anti-staphylococcal agent. Levonadifloxacin shows antibacterial activity against Methicillin (HY-121544)-susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant S. aureus (MRSA) strains, with a reduction of which phagocytized in THP-1 monocytes[1].
Erythromycin dihyrate dihydrate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin dihyrate acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1].
Artemotil (β-Arteether) is a fast acting blood schizonticide specifically indicated for the treatment of chloroquine-resistant Plasmodium falciparum malaria and cerebral malaria cases. Target:Artemotil is a semi-synthetic derivative of artemisinin, a natural product of the Chinese plant Artemisia annua.
Dicloxacillin is a β-lactam antibiotic of the penicillin family. Dicloxacillin against Gram-positive bacteria. Dicloxacillin is active against β-lactamase-producing organisms such as Staphylococcus aureus[1].
Garcinone B, a xanthone derivative, is a nature product that could be isolated from the pericarp of Mangosteen. Garcinone B is a potent ACE2 and Mpro inhibitor. Garcinone B can be used in research of COVID-19[1].
Aurein 2.5 is an antibiotic antimicrobial peptide. Aurein 2.5 has antibacterial and antifungal activity[1][2]
Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product[1][2].
Pulcherriminic acid is a cyclic dipeptide antimicrobial agent with high affinity for Fe3+, found mainly in Bacillus and yeast. Pulcherriminic acid chelates iron ions through a non-enzymatic reaction to form the extracellular red pigment pulcherrimin, which competes for iron nutrition and thus achieves an antibacterial effect. Pulcherriminic acid has great applications in food, agriculture and medical industries[1][2].
Cymal-6 (Cyclohexyl-hexyl-β-D-maltoside) is a potent TEM-1 beta-lactamase inhibitor with an Ki value of 40.05 µM. Cymal-6 (Cyclohexyl-hexyl-β-D-maltoside) can be used as glycosidic surfactant[1][2].
Antimalarial agent 14 (Compound N3) is a potent inhibitor of mitochondrial electron transport. Antimalarial agent 14 can serve as an anti-malarial agent[1].
RSV604 R enantiomer is the R-enantiomer of RSV604. RSV604 is an inhibitor of respiratory syncytial virus (RSV) replication. R-enantiomer is less active against RSV.
β-Amyrin acetate is a triterpenoid with potent anti-inflammatory, antifungal, anti-diabetic, anti-hyperlipidemic activities. β-Amyrin acetate can inhibit HMG-CoA reductase activity by locating in the hydrophobic binding cleft of HMG CoA reductase[1][2][3][4].
Isepamicin sulfate (Sch 21420 sulfate) is a broad spectrum aminoglycoside antibiotic. Isepamicin sulfate exhibits considerable antimicrobial activity against Gram-negative non-fermenters in a region with high antimicrobial resistance[1][2].
(9Z)-9,17-Octadecadiene-12,14-diyne-1,11,16-triol is a nature product that could be isolated from the ethyl acetate extract of Cassonia barteri (Araliaceae) leaves. (9Z)-9,17-Octadecadiene-12,14-diyne-1,11,16-triol has antibacterial activity against Bacillus subtilis and Pseudomonas fluorescens, antifungal activity against Cladosporium cucumerinum, moiluscicidal activity against Biomphalaria glabrata[1].
Antitubercular agent-24 (Compound 1) is an anti-tubercular agent with an extracellular IC50 of 0.83 μM and an intracellular IC50 of 0.17 μM against M. tuberculosis H37Rv[1].
Dynapyrazole A is a specific inhibitor of microtubule dynamin that specifically inhibits the ATPase activity of microtubule-stimulated dynamin without blocking microtubule-independent basal activity[1].
Piromidic acid is a quinolone antibiotic.
Mt KARI-IN-5 (compound 6c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 4.72 μM. Mt KARI-IN-5 has inhibitory activity against Mtb H37Rv (MIC = 1.56 μM) and low cytotoxicity (HEK IC50 > 64 μg/mL)[1]
EcDsbB-IN-9 (Compound 9) is a potent E. coli DsbB (EcDsbB) inhibitor with an IC50 of 1.7 μM and a Ki of 46 nM[1].
HIV-1 inhibitor-30 (compound 10i) is a potent HIV-1 inhibitor with an EC50 value of 40 nM and an IC50 value of 80 nM for HIV-1 RT DNA polymerase. HIV-1 inhibitor-30 has highly antiretroviral activity against seven non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant HIV-1 strains (RT-K103N; RT-Y181C; RT-K103N,Y181C; RT-L100I,K103N; RT-Y188L; RT-K103N,G190A; RT-K103N,V108I) with IC50s of 0.04~1.42 μM. HIV-1 inhibitor-30 can be used for researching AIDS[1].
Sahandol is a diterpene, that can be isolated from Salvia sahendica. Sahandol shows antiplasmodial, antitrypanosomal, and cytotoxic activities[1].
ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial[1][2][3].
Chloroquine D5 is deuterium labeled Chloroquine. Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
SBP1 peptide is a chemically synthesized 23-mer peptide fragment of the ACE2 PD α1 helix. SBP1 peptide associates with micromolar affinity to insect-derived SARS-CoV-2-RBD protein [1].
Maximin 7 is an antimicrobial peptide derived from toad Bombina maxima[1].
CK2-IN-4 (compound 5) is a protein kinase (CK2) inhibitor (IC50=8.6 µM). CK2-IN-4 has good potential for research in the areas of cancer, viral infections and glomerulonephritis[1].