Cefuroxime Axetil, a prodrug of the cephalosporin cefuroxime and an oarl broad spectrum antibiotic, inhibits several gram-positive and gram-negative organisms, including those most frequently associated with various common community-acquired infections[1].
EGCG Octaacetate is a prodrug of Green tea epigallocatechin-3-gallate (EGCG), utilized to enhance the stability and bioavailability of EGCG in vivo. EGCG Octaacetate has high efficacy, bioavailability, anti-oxidation and anti-angiogenesis capacities[1]. EGCG octaacetate is the potential antibacterial compound for gram-positive bacteria (GPB) and gram-negative bacteria (GNB) [2].
Cepeginterferon alfa-2b is a pegylated interferon. And Cepeginterferon alfa-2b has PEG with molecular weight of 20 kDa as a pegylated base. Cepeginterferon alfa-2b can be used for research of various diseases, such as hepatitis C virus (HCV), polycythemia vera (PV) and essential thrombocythemia (ET)[1][2].
Oxfendazole is the sulfoxide form of fenbendazole which is a broad spectrum benzimidazole anthelmintic. Target: AntiparasiticOxfendazole is the sulfoxide form of fenbendazole, a broad spectrum benzimidazole anthelmintic. Its main use is for protecting livestock against roundworm, strongyles and pinworms.[1]. Pigs in the treated group received Oxfendazole orally at 30 mg/kg dose. At five days post-treatment, animals were sacrificed and the clinical efficacy of the Oxfendazole treatment was established following the currently available WAAVP guidelines for a controlled efficacy test. None of the animals involved in this experiment showed any adverse events during the study. Oxfendazole treatment given as a single 30 mg/kg oral dose showed a 100% efficacy against all the nematode parasites present in the three experiments. In conclusion, under the current experimental conditions, Oxfendazole orally administered to naturally parasitized piglets at a single dose of 30 mg/kg was safe and highly efficacious (100%) against adult stages of A. suum, Oesophagostomum spp., T. suis and Metastrongylus spp [1].
Thanatin is an antimicrobial peptide which is antifungal to some gram-positive bacteria[1].
Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects[1][2][3][4].
L-Fd4A is an adenine derivative. L-Fd4A has anti-human immunodeficiency virus (HIV) (EC50=1.5 μM) and anti-hepatitis B virus (HBV) (EC50=1.7 μM) activity. L-Fd4A has low cytotoxicity[1].
Desbutyl Lumefantrine is a metabolite of lumefantrine with antimalarial activity[1].
CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. CS-003 Free base (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.
A BIX-01294 derivative that inhibit malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death; inhibits P. falciparum 3D7 parasites in culture with IC50 of 100 nM, >22-fold more potent than IC50 toward two human cell lines and one mouse cell line; significant reduces histone H3K4me3 levels in a concentration-dependent and exposure time-dependent manner in treatment of P. falciparum parasites.
Tenofovir alafenamide (GS-7340) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
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.
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].
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].
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.
Hydroxystilbamidine bis(methanesulfonate), a dye capable of binding to both DNA and RNA, has been found to be a powerful inhibitor of cellular ribonucleases.
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].
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].
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].
Serylleucine is a dipeptide. Serylleucine's core 1 o-glycosylated peptide (SLC1G) can be detected in urine as a metabolite and is a biomarker in TB studies[1].
Meropenem trihydrate is a carbapenem antibiotic with broad-spectrum antibacterial activity.
CCR-11 is an antibacterial agent. CCR-11 can inhibit the proliferation of B. subtilis cells with an IC50 value of 1.2 μM. CCR-11 inhibits HeLa cell proliferation with an IC50 value of 18.1 μM. CCR-11 inhibits bacterial cytokinesis by inhibiting FtsZ assembly. CCR-11 can be used for the research of FtsZ-targeted antibacterial agents[1].
Friulimicin D, a lipopeptide antibiotic, like Friulimicin B, is isolated from the actinomycete Actinoplanes friuliensis[1].
2-Hydroxy-1-methoxyanthraquinone could be isolated from the stem bark of Morinda lucida Benth. (Rubiaceae) and possesses antibacterial activity[1].