PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle[1][2]. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
WU-FA-01, a hydrogenated derivative of WU-FA-00, is an antibacterial agent that exhibits high levels of antibacterial activity against Gram-positive strains and also has some anti-inflammatory activity[1].
α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation.
Acetyllovastatin, a acetate of Lovastatin, presentes a moderate inhibitory effect against the enzyme acetylcholinesterase with an IC50 of 79 μg/mL. Lovastatin has been found to display antifungal activity, and suppresses proliferation of a number of transformed cell lines[1].
TAPI-0 is a TACE (TNF-α converting enzyme; ADAM17) inhibitor with an IC50 of 100 nM. TAPI-0 is a MMP inhibitor and also attenuates TNF-α processing[1][2].
Ro 20-0657/000 is a metabolite of Trimethoprim. Trimethoprim is a dihydrofolate reductase inhibitor, used as an antibacterial agent in human and veterinary medicine[1][2][3].
ODN 2216 is a TLR9 (toll-like receptor 9) ligand or agonist. ODN 2216 induces high amounts of IFN-α and IFN-β. ODN 2216 induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 can activate NK cells and promote IFN-γ production of TCR-triggered CD4+ T cells[1][2][3][4].
Thalifendine chloride is a metabolite of Berberine (HY-N0716), with antiplasmodial and antiamoebic activities. Thalifendine chloride shows activity against P. falciparum and E. histolytica with IC50s of 7.91 μM and 116 μM, respectively[1][2].
HIV-IN petide is a competitive inhibitor of HIV-1 protease (Ki=50 nM)[1].
GlyRS-IN-1 is a glycyl-tRNA synthase (GlyRS) inhibitor extracted from patent WO 2017066459 A1. GlyRS-IN-1 can also inhibit the growth of bacteria.
(+)-Magnoflorine iodide (Magnoflorine iodide), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm[1]. (+)-Magnoflorine iodide has anti-fungal, anti-antidiabetic and anti-oxidative activity[2].
Coblopasvir (KW-136) dihydrochloride is a pangenotypic non-structural protein 5A (NS5A) inhibitor. Coblopasvir dihydrochloride can be used for research of chronic hepatitis C virus infection[1].
Terbinafine lactate (TDT 067 lactate) is an orally active and potent antifungal agent. Terbinafine lactate is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine lactate also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria[1][2][3].
19,20-Epoxycytochalasin C, a cytochalasin, is a fungal metabolite from Nemania sp. 19,20-Epoxycytochalasin C shows potent in vitro antiplasmodial activity and phytotoxicity[1].
HCV-IN-40 (Compound 18c) is a potent, orally active hepatitis C virus (HCV) nucleoside inhibitor with EC50 values of 0.259, 0.434 and 0.069 μM against GT1a, GT1b and GT1b CES1 replicons[1].
Kanamycins sulfate is a broad-spectrum antibiotic, can be used in certain severe staphylococcal or Gram-negative bacillary infections. Kanamycin sulfate has certain ototoxicity[1][2].
Colistin methanesulfonate sodium salt exhibits MIC values ranged from 4 to 16 mg/liter against susceptible strains (P. aeruginosa)[1].
Antibiotic PF 1052 is an antibiotic extracted from a natural product library. Antibiotic PF 1052 has an inhibitory effect on murine neutrophil migration[1].
Gimsilumab (MORAb-022) is a humanized anti-GM-CSF monoclonal antibody. Gimsilumab has the potential for the research of COVID-19 and rheumatoid arthritis (RA)[1][2].
(+)-Totarol is a diterpenoid compound isolated from Podocarpus spp.. (+)-Totarol is a potent antioxidant and antibacterial agent[1].
Daphnoretin (Dephnoretin), isolated from Wikstroemia indica, possesses antiviral activity[1]. Daphnoretin likes PMA, may direct activation of protein kinase C which in turn activated NADPH oxidase and elicited respiratory burst[2].
FgGpmk1-IN-1 is a novel fusarium graminearum mitogen-activated protein kinase (FgGpmk1) inhibitor with an EC50 value of 3.46 μg/mL.
Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.
HCV-IN-34 (compound 3i) is an orally active and potent HCV entry inhibitor. HCV-IN-35 shows excellent antiviral activity, with an EC50 of 0.010 μM and a CC50 (half-maximal cytotoxic concentration) of 8.23 μM[1].
Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity[1].
Idarubicin is an orally active and potent anthracycline antileukemic agent. Idarubicin inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin shows induction of DNA damage. Idarubicin inhibits DNA synthesis and of c-myc expression. Idarubicin inhibits the growth of bacteria and yeasts[1][2][3][4][5].
Tulathromycin A is a macrolide antibiotic.IC50 Value: 1 microg/ml (MIC90 for Pasteurella multocida) [2]Target: Antibacterialin vitro: Two highly pathogenic strains of M. bovis (with minimum inhibitory concentration values for tulathromycin of 1 and >64 microg/ml) were inoculated into 145 calves. Four days after inoculation, calves with clinical BRD were treated subcutaneously with saline or tulathromycin (2.5 mg/kg). Compared with saline, BRD-related withdrawals, peak rectal temperatures, and lung lesion scores were significantly lower for tulathromycin-treated calves (P < .01). Tulathromycin was highly effective in the treatment of BRD due to M. bovis in calves regardless of the minimum inhibitory concentration of the challenge strain (1 or >64 microg/ml) [1]. The lowest concentrations inhibiting the growth of 90% of isolates (MIC90) for tulathromycin were 2 microg/ml for Mannheimia (Pasteurella) haemolytica, 1 microg/ml for Pasteurella multocida (bovine), and 2 microg/ml for Pasteurella multocida (porcine) and ranged from 0.5 to 4 microg/ml for Histophilus somni (Haemophilus somnus) and from 4 to 16 microg/ml for Actinobacillus pleuropneumoniae [2]. in vivo: Each study randomly allocated 250 calves to receivetulathromycin at 2.5 mg/kg and 250 calves to receive either tilmicosin at 10 mg/kg (Colorado site) or florfenicol at 40 mg/kg (Idaho and Texas sites) on arrival at the feedlot. Calves were housed by treatment group in pens with 50 calves/pen [3]. The treatment groups were physiologic saline (n = 160) given SC at 0.02 ml/kg, tulathromycin (n = 320) given SC at 2.5 mg/kg, and tilmicosin (n = 320) given SC at 10 mg/kg [4].Tulathromycin is a triamilide antimicrobial that has been approved for use in the treatment and prevention of bovine respiratory disease and the treatment of swine respiratory disease. Toxicity: No adverse events related to tulathromycin were reported [4].Clinical trial:
Sennidin B, a stereoisomer isolated from the leaves of Cassia angustifolia, has lower activity than Sennidin A. Sennidin A inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation [1][2].
Myriceric acid B is a potent HIV-1 entry inhibitor targeting gp41. Myriceric acid B is an antitumor agent[1][2].
PC786 is an inhaled respiratory syncytial virus (RSV) L protein polymerase inhibitor. PC786 demonstrates potent antiviral activity against RSV-A (IC50 <0.09 to 0.71 nM) and RSV-B (IC50, 1.3 to 50.6 nM)[1].