Tachyplesin I is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I exhibits cytotoxic properties against various human tumor cell lines acting primarily by impairing the integrity of the outer cell membrane[1].
Ciluprevir(BILN 2061) is a specific and potent peptidomimetic inhibitor of the HCV NS3 protease with an IC50 of 3.0 nM.
Influenza A virus-IN-4 (compound 23b), an Oseltamivir derivative, is a potent inhibitor of neuraminidase. Influenza A virus-IN-4 exerts powerful inhibitions on influenza viruses[1].
Abacavir sulfate (ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS. Target: NRTIAbacavir is a nucleoside reverse transcriptase inhibitor marketed since 1999 for the treatment of infection with the human immunodeficiency virus type 1 (HIV). Despite its clinical efficacy, abacavir administration has been associated with serious and sometimes fatal toxic events. Abacavir has been reported to undergo bioactivation in vitro, yielding reactive species that bind covalently to human serum albumin, but the haptenation mechanism and its significance to the toxic events induced by this anti-HIV drug have yet to be elucidated. The mechanism underlying abacavir hypersensitivity syndrome is related to the change in the HLA-B*5701 protein product. Abacavir binds with high specificity to the HLA-B*5701 protein, changing the shape and chemistry of the antigen-binding cleft. This results in a change in immunological tolerance and the subsequent activation of abacavir-specific cytotoxic T cells, which produce a systemic reaction known as abacavir hypersensitivity syndrome.
HIV-1 inhibitor-42 (compound 5b) is a potent HIV-1 inhibitor, with an IC50 of 0.06 μM. HIV-1 inhibitor-42 inhibits HIV-1 RT RNA-dependent DNA polymerase and DNA-dependent DNA polymerase, with IC50 values of 0.518 and 0.072 μM[1].
Moracin T can be isolated from the bark of mulberry trees and has antibacterial activity.
InhA-IN-3 (Compound TU12) is a Mycobacterium tuberculosis InhA (an enoyl ACP-reductase) inhibitor with an IC50 of 17.7 μM[1].
Fungicide4 shows the high activity against the P. infestans strain.
Heraclenol, a coumarin, is isolated from the fruits of Angelica lucida, and exhibits antibacterial activities[1].
10-Undecenoic acid zinc salt is a natural or synthetic fungistatic fatty acid, is used topically in creams against fungal infections, eczemas, ringworm, and other cutaneous conditions. The zinc provides an astringent action.
PMEDAP is a potent inhibitor of human immunodeficiency virus (HIV) replication. PMEDAP has anti-murine cytomegalovirus (MCMV) activity. PMEDAP is a very potent inhibitor of Moloney murine sarcoma virus (MSV)-induced tumor formation and associated mortality[1][2].
Bipolamine G is an antibacterial polyketide alkaloid[1].
Juncuenin D induces caspase-3-mediated cytotoxicity in HT22 cells. Juncuenin D also has anti-bacterial activity against MRSA strains. Juncuenin D can be isolated from J. effusus[1].
SMAP-29, a promising antiinfective agent, is a broad spectrum antibacterial and antifungal α-helical cathelicidin-derived peptide. SMAP-29 acts by permeabilizing bacterial membranes and inducing remarkable changes in the surface morphology of susceptible microorganism[1][2].
Benzoxonium chloride is an anti-leishmanial agent. Benzoxonium chloride inhibits bacteria, certain protozoa, yeasts and non-spore forming organisms[1].
Axinysone B can be isolated from Laurencia similis. Axinysone B has antibacterial activity against Staphylococcus sp.[1].
Ibalizumab (TMB-355) is a humanised IgG4 monoclonal antibody that prevents HIV cell entry by binding to CD4 receptor. Ibalizumab has the potential for HIV-1 infection research[1].
Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s = 0.04 µM and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s = 0.073 µg/mL and 4.6 µg/mL respectively). Propiconazole increases production of reactive oxygen species (ROS).
Radalbuvir (GS-9669) is a non-nucleoside inhibitor of nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp). Radalbuvir shows strong anti-HCV potency (GT1a intrinsic EC50 = 2.9 nM, GT1b EC50 = 6 nM)[1].
Antibacterial agent 104 (Compound 7) is a potent antibacterial agent. Antibacterial agent 104 displays excellent antibacterial activity in vitro and good efficacy in vivo against MRSA[1].
HIV-1 Nef-IN-1 is an HIV-1 Nef protein inhibitor that efficiently competes for Nef-SH3Hck interactions with a Kd of 6.7 μM[1].
Tuberculosis inhibitor 1 is a potent and non-cytotoxic trypanosoma brucei growth inhibitor with an EC50 of 5 nM[1].
Bicyclol(SY 801) is a anti-hepatitis drug.Target: HBVOral administration of bicyclol normalized the elevated serum transaminases (ALT, AST) by approximately 50% in chronic viral hepatitis B and C, and also showed certain level of inhibiting HBV and HCV replication. No noticeable adverse reaction has been observed. In combination therapy of bicyclol with interferon alpha, lamivudine and adefovir dipivoxil in HBV or HCV, bicyclol may potentiate the anti-viral efficacy and reduce YMDD mutant and side effects. In 2004 China FDA issued license to manufacture bicyclol. Since then bicyclol has been widely used to treat chronic HBV and HCV in China [1].
FK-3000 is a potent anti-tumor agent that inhibits the growth of carcinoma cells through apoptosis and induction cell cycle arrest. FK-3000 also exhibit antiviral effects against HSV-1 and HIV-1[1][2][3][4].
Cefuroxime sodium is an enteral or oral second-generation cephalosporin antibiotic.
Gancaonin G is a 6-prenylated isoflavanone that can be isolated from Glycyrrhiza uralensis. Gancaonin G has antibacterial activity against Streptococcus mutants and MRSA strains[1].
Resiquimod-d5 (R848-d5) is deuterium labeled Resiquimod. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α[1][2].
Fluazinam impurity 1 is an impurity of Fluazinam with antifungal activity. Fluazinam impurity 1 is active against Sphaerotheca fuliginea, Pyricularia oryzae and Rhizoctonia solani[1].
AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[1][2].
Naringenin is the predominant flavanone in grapefruit; displays strong anti-inflammatory and antioxidant activities.