Epipodophyllotoxin acetate (4-O-Epipodophyllotoxinyl acetate; compound 4) is a cyclolignan that exhibits antineoplastic and antiviral activities. Epipodophyllotoxin acetate inhibits HSV and VSV, with IC50s of 0.2 and 0.1 μg/mL, respectively[1].
Sitafloxacin (DU6859a) monohydrate is a potent, orally active fluoroquinolone antibiotic. Sitafloxacin monohydrate shows antichlamydial activity and antibacterial activities against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin monohydrate can be used for the research of respiratory tract infection and urinary tract infection[1][2].
Cefprozil (Cefzil) is a second-generation cephalosporin type antibiotic[1].
Ombuin, isolated from Zanthoxylum armatum, displays broad spectrum antibacterial effect with MIC ranges from 125 to 500 μg/mL[1].
Raltegravir-d4 is deuterium labeled Raltegravir. Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
Trifluoromethyl-tubercidin (TFMT) inhibits host MTr1 and suppresses virus replication. TFMT inhibits MTr1 through interaction at its S-adenosyl-l-methionine binding pocket to restrict influenza virus replication. TFMT was effective in inhibiting viral replication in mice, displayed little toxicity.
ANS ammonium is a potent antibacterial agent and a textile dye. ANS ammonium can be used as fluorescence probe. ANS ammonium blocks the binding of triiodothyronine to thyroxine binding globulin in radioimmunoassay of triiodothyronine[1][2][3].
Lipoxamycin is an antifungal antibiotic and a potent serine palmitoyltransferase inhibitor with an IC50 of 21 nM[1][2].
Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
Hispidalin is a novel antimicrobial peptide with broad and efficient antibacterial activity against various bacterial and fungal pathogens, and can be used as an antibacterial agent and food preservative[1].
HSP90-IN-14 (compound 4) is a potent Hsp90 (heat shock protein 90) inhibitor, with a Kd of 0.26 μM. HSP90-IN-14 shows anti-influenza virus activity in MDCK cells, with EC50 values of 2.6, 3.9, and 17 μM for influenza A/H3N2, A/H1N1, and B, respectively[1].
Heneicosane-d44 is the deuterium labeled Heneicosane[1]. Heneicosane is an aroma component isolated from Streptomyces philanthi RL-1-178 or Serapias cordigera. Heneicosane is a pheromone and inhibits aflatoxin production[2][3][4].
T-2307, an arylamidine, has antifungal activities in vitro and in vivo. T-2307 exhibits broad-spectrum activity against clinically significant pathogens, including Candida species (MIC range, 0.00025 to 0.0078 μg/ml), Cryptococcus neoformans (MIC range, 0.0039 to 0.0625 μg/ml), and Aspergillus species (MIC range, 0.0156 to 4 μg/mL) [1].
Cefoperazone is a cephalosporin antibiotic for inhibition of rMrp2-mediated [3H]E217βG uptake with IC50 of 199 μM.Target: AntibacterialCefoperazone is a sterile, semisynthetic, broad-spectrum, parenteral cephalosporin antibiotic for intravenous or intramuscular administration. After intravenous administration of 2 g of Cefoperazone, levels in serum rang from 202μg/mL to 375 μg/mL depending on the period of drug administration. After intramuscular injection of 2 g of Cefoperazone, the mean peak serum level is 111 μg/mL at 1.5 hours. At 12 hours after dosing, mean serum levels are still 2 to 4 μg/mL. Cefoperazone is 90% bound to serum proteins.
Galidesivir (BCX 4430) is a viral RNA-dependent RNA polymerase (RdRp) inhibitor; demonstrated broad-spectrum activity in multiple viruses and a favorable preliminary preclinical safety profile.
Tryglysin A is an antimicrobial peptide inhibits the growth of other streptococci[1].
BMY-43748 is a promising antibacterial agent, exhibiting great in vitro and in vivo antibacterial activity.
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to drugs targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM[1].
BMS-626529 is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells.
Lauric acid-d3 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Tetrahydroepiberberine is a isoquinoline alkaloid isolated from Corydalis impatiens (Pall). Tetrahydroepiberberine has antifungal and selective inhibition against the PI-3 virus activities[1].
N-Butylthiophosphoric triamide (NBPT) is a potent urease inhibitor. Butylthiophosphoric triamide inhibits nitrification and reduces the conversion of urea to NH3 gas[1].
Amitivir (LY 217896), a thiadiazole derivative, possesses broad antiviral activity against orthomyxo- and paramyxoviruses. Amitivir is effective against influenza A and B viruses[1][2].
Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.Target: AntiparasiticAlbendazole, marketed as Albenza (United States), Eskazole, Zentel, Andazol and Alworm, is a benzimidazole drug used for the treatment of a variety of parasitic worm infestations. Although this use is widespread in the United States, the U.S. Food and Drug Administration (FDA) has not approved albendazole for this indication. It is marketed by Amedra Pharmaceuticals. Albendazole was first discovered at the SmithKline Animal Health Laboratories in 1972. It is a broad spectrum anthelmintic, effective against roundworms, tapeworms, and flukes of domestic animals and humans.Albendazole has been used as an anthelmintic and for control of flukes in a variety of animal species, including cattle, sheep, goats, swine, camels, dogs, cats, elephants, poultry and others. In many countries, it is very commonly used for ruminant livestock. For use in livestock, albendazole is marketed by Zoetis (formerly Pfizer Animal Health) in numerous countries (including the United States and Canada) as Valbazen in oral suspension and paste formulations; by Interchemie in the Netherlands and elsewhere as Albenol-100; by Channelle Animal Health Ltd. in the United Kingdom as Albex; by Ravensdown in New Zealand as Albendazole; etc. Although most formulations are administered orally, Ricomax (ricobendazole, or albendazole sulfoxide) is administered by subcutaneous injection.
Cefodizime is a third generation cephalosporin antibiotic with a broad spectrum of antibacterial activity. Cefodizime has no renal toxic effect, good tolerance and immune regulation activity, and is widely used in the treatment of severe infections of the respiratory and urinary tracts[1][2].
Antibacterial agent 103 (compound 7) has highly antibacterial activity against kinds of Gram-positive and -negative bacteria. Antibacterial agent 103 can be used for researching inhibition of resistance bacterial strains[1].
Procodazole is a non-specific active immunoprotective agent against viral and bacterial infections, used as a potentiator.
Amustaline (S-303) dihydrochloride, a nucleic acid-targeted alkylator, is an efficient pathogen inactivation agent for blood components containing red blood cells. Amustaline dihydrochloride has three components: an acridine anchor (an intercalator that targets nucleic acids non-covalently), an effector (a bis-alkylator group that reacts with nucleophiles), and a linker (a small flexible carbon chain containing a labile ester bond that hydrolyzes at neutral pH to yield non-reactive breakdown products)[1][2].
Deaminase inhibitor-1 is a small molecule inhibitor of APOBEC3G DNA Deaminase, with an IC50 value of 18.9 μM[1].
Itraconazole is a triazole antifungal agent.IC50 Value: N/ATarget: antifungalin vitro: Itraconazole is pharmacologically distinct from other azole antifungal agents in that it is the only inhibitor in this class that has been shown to inhibit both the hedgehog signaling pathway and angiogenesis[1, 2]. These distinct activities are unrelated to inhibition of the cytochrome P450 lanosterol 14 alpha-demethylase and the exact molecular targets responsible remain unidentified. Functionally, the antiangiogenic activity of itraconazole has been shown to be linked to inhibition of glycosylation, VEGFR2 phosphorylation and cholesterol biosynthesis pathways [2].Evidence suggests the structural determinants for inhibition of hedgehog signaling by itraconazole are recognizably different from those associated with antiangiogenic activity [3].in vivo: Nine volunteers were given either 200 mg itraconazole, or matched placebo orally once daily for 4 days. On day 4, itraconazole increased the area under the midazolam concentration-time curve from 10 to 15 times (p < 0.001) and mean peak concentrations three to four times (p < 0.001) compared with the placebo phase. In psychomotor tests, the interaction was statistically significant (p < 0.05) until at least 6 hours after drug administration. Inhibition of the cytochrome P450IIIA by itraconazole may explain the observed pharmacokinetic interaction [4].