Setrobuvir (ANA598) is an orally active non-nucleosidic HCV NS5B polymerase inhibitor. ANA-598 inhibits both de novo RNA synthesis and primer extension, with IC50s between 4 and 5 nM. Setrobuvir also shows excellent binding affinity to SARS-CoV-2 RdRp and induces RdRp inhibition[1][2].
FAAL-IN-1 (compound 32) is a selective inhibitor of fatty acyl-AMP ligase (FAAL), with a Ki of 0.7 μM for FAAL28. FAAL-IN-1 shows antimycobacterial activity[1].
Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection. IC50 Valur: 2 nM (Ki for HIV-1 protease) [2]Target: HIV Proteasein vitro: In vitro exposure (72 hours) of HAECs to NEL (0.25-2 μg/mL) decreased both basal (2.5-fold) and insulin-induced NO production (4- to 5-fold). NEL suppressed insulin-induced phosphorylation of both Akt and eNOS at serine residues 473 and 1177, respectively. NEL decreased tyrosine phosphorylation of IR-β, IRS-1, and PI3K. Coexposure to troglitazone (TRO; 250 nM) ameliorated the suppressive effects of NEL on insulin signaling and NO production. Coexposure to TRO also increased eNOS expression in NEL-treated HAECs [1]. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively [2].in vivo: In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans [2].
Mupadolimab (CPI-006) is an IgG1κ humanized FcγR binding-deficient anti-CD73 monoclonal antibody (mAb) that activates CD73POS B cells[1].
Antibacterial agent 114 (compound 1) is a potent antibacterial agent. Antibacterial agent 114 shows antibacterial activity against P.aeruginosa, B.subtilis, E.coli, E.faecalis, S.typhimuriumand, S.mutans, and S.aureus microorganisms, with MIC values of 625, 625, 625, 625, 625, 1250 and 1250 μM, respectively[1].
Antibacterial agent 53 (example 19) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
NOSO-502 (NOSO502) is a novel inhibitor of bacterial translation, has MIC values of 0.5-4 ug/ml against standard Enterobacteriaceae strains and carbapenem-resistant Enterobacteriaceae (CRE) isolates that produce KPC, AmpC, or OXA enzymes and metallo-β-lactamases; interacts strongly with a specific site on the 30S subunit of bacterial ribosomes but has no significant activity against any of the 55 cell surface receptors, transporters, or ion channels; NOSO-502 is active against a panel of Gram-positive and Gram-negative bacteria, including carbapenem-resistant and polymyxin-resistant strains, and exhibits promising in vivo activity in various murine infection models, a favorable in vitro safety profile, and a low potential for resistance development.
HSV-1/HSV-2-IN-2 is a HSV-1, HSV-2 and VV inhibitor with EC50 values of 6.8, 8.9 and 8.9 µM, respectively. HSV-1/HSV-2-IN-2 shows antiviral activity[1].
Lyoniside is a lignan glycoside with antioxidant, allelopathic and antifungal activities, which can be isolated from the rhizomes and stems of bilberry (Vaccinium myrtillus L.). Lyoniside exhibits radical scavenging properties with an IC50 value of 23 μg/mL in DPPH assay. Lyoniside inhibits the mycelial growth of Fusarium oxysporum and Mucor hiemalis at 50 μg/mL with inhibitory rates of 78% and 80%, respectively[1].
(S)-Hydroxychloroquine ((S)-HCQ) is the enantiomer of Hydroxychloroquine[1]. Hydroxychloroquine, a synthetic antimalarial drug, inhibits Toll-like receptor 7/9 (TLR7/9) signaling, and shows efficiently inhibits SARS-CoV-2 infection in vitro[2][3][4].
Polyvinylpyrrolidone is a compound which has been widely tested and used in human and veterinary medicine as an effective wound healing accelerator and disinfectant when combined with iodine and other compounds.
Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analogue of sulfaquinoxaline, is a topoisomerase II alpha/beta poison. Chloroquinoxaline sulfonamide is used to control coccidiosis in poultry, rabbit, sheep, and cattle[1]. Antitumor activity[2].
Rifaquizinone (CBR-2092) is a Rifamycin-Quinolone Hybrid Antibiotic. Rifaquizinone inhibits wild-type S. aureus RNA polymerase with an IC50 of 34 nM. Rifaquizinone is effective against S. aureus infections, with MICs ranged from 0.008 to 0.5 μg/mL for 300 clinical isolates of staphylococci and streptococci[1][2].
Cephalothin sodium is a first generation cephem antibiotic with a wide range antibacterial activity, is active against gram-positive and gram-negative bacteria.
HBV-IN-34 (compound 17i) is a potent HBsAg production inhibitor. HBV-IN-34 exhibits excellent in vitro anti-HBV potency, with an EC50 of 0.018 μM and 0.044 μM for HBV DNA and HBsAg, respectively[1].
Cytochalasin O (compound 13) is a secondary metabolite of the phytopathogenic fungus P. sp. CIB-109[1].
Anti-Trypanosoma cruzi agent-3 (Compound 7c) is an antiprotozoal agent[1].
L18-MDP is a derivative of muramyl dipeptide, an antibacterial agent. L18-MDP has antibacterial activity and has potential applications in bacterial and fungal infections[1].
Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
Ceftezole (CTZ) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole (CTZ) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity[1][2].
TAT (48-57) is a cell-permeable peptide, derived from HIV-1 transactivator of transcription (Tat) protein residue 48-57.
Thio-ITP (6-Thioinosine 5′-triphosphate) is a RNA polymerase activities competitive inhibitor[1].
Diallyl Trisulfide is isolated from Garlic. Diallyl Trisulfide suppresses the growth of Penicillium expansum (MFC99 value: ≤ 90 μg/mL) and promotes apoptosis via production of reactive oxygen species (ROS) and disintegration of cellular ultrastructure. Anticancer effect[1].
Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells[1]. Destruxin B significantly activates caspase-3 and reduces tumor cell proliferation through caspase-mediated apoptosis, not only in vitro but also in vivo[2].
Xanthoquinodin A1 is an anticoccidial antibiotic having a new xanthone-anthraquinone conjugate system[1].
Temafloxacin (TMFX) hydrochloride is an orally active quinolone broad-spectrum antibacterial agent. Temafloxacin hydrochloride is well tolerated in lower respiratory and genitourinary tract infections[1][2].
Aurein 2.3 is an antibiotic antimicrobial peptide. Aurein 2.3 partially inhibits E.coli ATPase activity and inhibits cell growth[1][2].
d-Atabrine dihydrochloride is an active enantiomer of quinacrine which displays antiprion activity.
ODN 2007, a class B CpG ODN (oligodeoxynucleotide), is a Toll-like receptor (TLR) ligand. ODN 2007 can be used as an immunomodulator, vaccine adjuvant, and enhance immune responses in mammals, fish, and humans. ODN 2007 sequence: 5'-TCGTCGTTGTCGTTTTGTCGTT-3'[1][2][3].