Aplidine (Plitidepsin) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM)[1]. Aplidine possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Aplidine is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research[1][2].
Levofuraltadone (NF-602) is an antibacterial and antiparasitic agent. Levofuraltadone has anti-trypanosomiasis activity and can be used in the study of human african trypanosomiasis as well as bacterial infections[1].
Sulfameter(Bayrena) is a long-acting sulfonamide antibacterial.Target: AntibacterialSulfameter(Bayrena) is a long-acting sulfonamide antibacterial. It is used as a leprostatic agent in the treatment of urinary tract infections.Six physically healthy patients each were given 2 g of sulfameter simultaneously with a high lipid, high protein and high carbohydrate test meal. This experiment was designed as a threefold crossover study, and there was a randomized assignment of patients to the different conditions. The results show that sulfameter is significantly better absorbed when administered with a high lipid meal than when given with a high protein or high carbohydrate meal, demonstrated by the areas under the serum concentration curves (AUC), by the peak serum concentration and by the cumulative renal excretion.
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].
HIV-1 inhibitor-37 (Compound 83) is a potent HIV-1. HIV-1 inhibitor-37 has the potential for further development as novel latency reversing agents[1].
Corydine is a naturally occurring alkaloid which can be extracted from plants such as Croton echinocarpus leaves. Corydine is efficient on inhibiting reverse transcriptase (RT) activity with an IC50 of 356.8 μg/mL. Corydine displays significant in vitro anti-HIV potential, inhibiting 40% of the HIV-1 reverse transcriptase enzyme activity at a concentration of 450 μg/mL of Corydine[1].
Sodium copper chlorophyllin exerts antiviral activities against Influenza virus and HIV with IC50s of 50 to 100 μM for both of them.
FadD32 Inhibitor-1 is a potent FadD32 inhibitor with anti-tubercular activity[1].
Piromidic acid is a quinolone antibiotic.
Doripenem is a new member of the carbapenem class of beta-lactam antibiotics with broad-spectrum coverage of Gram-positive, Gram-negative and anaerobic pathogens.Target: AntibacterialDoripenem is an ultra-broad-spectrum injectable antibiotic. It is a beta-lactam and belongs to the subgroup of carbapenems. It was launched by Shionogi Co. of Japan under the brand name Finibax in 2005 and is being marketed outside Japan by Johnson & Johnson. It is particularly active against Pseudomonas aeruginosa. It is recommended that those allergic to doripenem or to any type of beta-lactam antibiotics such as cephalosporin or other Carbapenems not receive doripenem.Doripenem appears as crystalline powder anywhere from a white to somewhat yellowish colour.Doripenem is moderately soluble in water, slightly soluble in methanol, and virtually insoluble in ethanol. Doripenem is also solution in N,N-dimethylformamide. Doripenem's chemical configuration has 6 asymmetrical carbon atoms (6 stereocentres) and is most commonly supplied as one pure isomer. In terms of doripenem for injection, the crystallized powered drug can form a monohydrate when mixed with water. However, Doripenem has not been proven to possess polymorphism.
Cefetamet is a potent antibiotic to treat respiratory and urinary tract infections.
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]
Ethyl acetoacetate-13C4 is the 13C labeled Ethyl acetoacetate[1]. Ethyl acetoacetate (Ethyl acetylacetate) is an ester widely used as an intermediate in the synthesis of many varieties of compounds[2][3][4]. Ethyl acetoacetate is an inhibitor of bacterial biofilm[5].
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].
Mupirocin (BRL-4910A) lithium is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin lithium apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis[1][2][3][4][5].
Apramycin sulfate is an aminoglycoside antibiotic mproduced by a strain of Streptomyces tenebrarius, used in veterinary practice.
Pendulone is a isoflavanquinone with good antiplasmodial activity with an IC50 of 7.0 µM. Pendulone also has antileishmanial, antibacterial and anticancer activity[1][2].
AAI101 is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens.
Manoalide is a potent Phospholipase A2 (PLA2) and Phospholipase C (PLC) inhibitor. Manoalide, a sesterpenoid compound, displays anti-inflammatory and antibacterial activities[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].
DprE1-IN-8 is a potent DprE1 inhibitor with an IC50 value of <0.75 μM. DprE1-IN-8 is against Mtb H37Rv with an IC50 of 6 nM and can be used for tuberculosis research[1].
XT-4 is an antimicrobial peptide derived from skin secretions of Xenopus tropicalis. XT-4 has strong activity against E.coli, the vaule of MIC is 18 μM[1].
DHDPS-IN-1 (compound 8) is a DHDPS inhibitor (IC50: 39 μM). DHDPS-IN-1 can be used in the area of antibacterial and herbicidal[1].
Penicillin G benzathine (Benzathine benzylpenicillin) is an antibiotic against many bacterial infections[1].
IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
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].
NSC260594 (NSC 260594) is a specific inhibitor of HIV-1 RNA packaging, which involves preventing the interaction of Gag with SL3 by stabilizing this small RNA stem-loop which then leads to stabilization of the global packaging signal region (psi or ψ); specifically blocks HIV-1 RNA encapsidation, binds to HIV-1 gRNA and exhibits potent antiviral activity; NSC260594 also is a small molecule inhibitor of the Escherichia coli condensin MukBEF, affects MukB directly.
Mellein is an antibiotic isolated from culture fluids of this Aspergillus[1].
C-215 is a novel inhibitor of mycobacterial membrane protein large 3 (MmpL3) with MIC90 of 16 uM against M. tuberculosis.
GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.IC50 value: Target: Anti-parasitic agentGNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not.