Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively[1]. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection[2].
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].
HBV-IN-22 (Compound LC5f) is an inhibitor of HBV DNA replication with IC50 values of 0.71 µM and 0.84 µM against wild-type and drug resistant HBV strains, respectively[1].
Propoxur is a carbamate insecticide with a fast knockdown and long residual effect used against turf, forestry, and household pests and fleas.
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].
SID-852843 is a WNV NS2B-NS3 proteinase inhibitor. SID-852843 can inhibit WNV NS2B-NS3 proteinase activity with IC50 value of 0.105 μM. SID-852843 can be used for the research of virus infection[1].
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.
Etidocaine (EDC) is a long aminoamide local anesthetic[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].
Diguanosine 5′-triphosphate (Gp3G) is a kind of homodinucleotide from by GTP:GTP guanylyltransferase[1]. Diguanosine 5′-triphosphate is a virus-specific oligonucleotide, can be used to prime reovirus transcription and inhibit RNA methylation[2].
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].
Delmitide (RDP58) is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide can be used for the research of ulcerative colitis[1][2].
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].
LmCPB-IN-1 (compound 35) is a potent and reversible covalent Leishmania mexicana cysteine protease B (LmCPB) inhibitor with a pKi of 9.7[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.
FSL-1 is a TLR2/6 agonist (also a putative TLR10 ligand). FSL-1 activates NF-κB. FSL-1 induces pro-inflammatory cytokines including IL-8, IL-1β, CCL20 and TNF-α in vitro. FSL-1 synergizes with IFNγ to induce CXCL10 release from melanoma cells.
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.
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].
Hydroxystilbamidine bis(methanesulfonate), a dye capable of binding to both DNA and RNA, has been found to be a powerful inhibitor of cellular ribonucleases.
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].
Sahandol is a diterpene, that can be isolated from Salvia sahendica. Sahandol shows antiplasmodial, antitrypanosomal, and cytotoxic activities[1].
Apramycin sulfate is an aminoglycoside antibiotic mproduced by a strain of Streptomyces tenebrarius, used in veterinary practice.
CcpA-IN-1 is a Staphylococcus aureus antibiotic. CcpA-IN-1 has significant bactericidal activity (MICS=460 nM)[1].