Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside (compound 1) is a lignan with anti-HBC activity. Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside targets HBV surface antigen with IC50s of 0.58 mM (HBsAg) and >2.4 mM (HBeAg). Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside can be isolated from star anise[1].
RSV L-protein-IN-5 (compound E) is a potent inhibitor of Respiratory syncytial virus (RSV) (EC50=0.1 μM). RSV L-protein-IN-5 inhibits Polymerase (IC50=0.66 μM)，and blocks RSV mRNA synthesis by inhibiting guanylation of viral transcripts. RSV L-protein-IN-5 shows moderate cytotoxicity (CC50=10.7 μM，HEp-2)，also exhibits activity and lowers virus titers in mouse models of RSV infection[1].
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].
(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].
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].
d-Atabrine dihydrochloride is an active enantiomer of quinacrine which displays antiprion activity.
Himastatin is a antitumor antibiotic produced by a strain of S. hygroscopicus sp. Himastatin is a dimeric cyclohexadepsipeptide containing piperazic acid and a unique central aromatic core[1].
Novel Inhibitor of Bacterial Cytokinesis, inhibiting FtsZ
Oxantel pamoate is a widely available dewormer, potently against Trichuris muris and Hookworms.
Mebendazole is a highly effective, broad-spectrum antihelmintic indicated for the treatment of nematode infestations; has been found as a hedgehog inhibitor.
Allergen Gal d 4 (46-61), chicken is a hen egg white lysozyme peptide.
Tobramycin is an aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius.Target: AntibacterialTobramycin is an aminoglycoside antibiotic derived from Streptomyces tenebrarius and used to treat various types of bacterial infections, particularly Gram-negative infections. It is especially effective against species of Pseudomonas [1]. Tobramycin works by binding to a site on the bacterial 30S and 50S ribosome, preventing formation of the 70S complex. As a result, mRNA cannot be translated into protein and cell death ensues. Tobramycin is preferred over gentamicin for Pseudomonas aeruginosa pneumonia due to better lung penetration. From Wikipedia [2].
Cidofovir is an anti-CMV drug which can suppress CMV replication by selective inhibition of viral DNA polymerase and therefore prevention of viral replication and transcription.IC50 Value:Target: CMV DNA polymerasein vitro: The minimum concentrations of (S)-HPMPC required to inhibit CMV plaque formation by 50% was microgram/ml. The selectivity indices of (S)-HPMPC, as determined by the ratio of the 50% inhibitory concentration for cell growth to the 50% inhibitory concentration for plaque formation for CMV (AD-169 strain), was 1,500 [1]. The time course of uptake of HPMPC into Vero cells was linear between 10 and 75 min and proportional to the concentration in the medium from 10(-6) to 10(-2) M. HPMPC uptake was temperature sensitive and the rate of uptake was considerably lower at 27 degrees than at 37 degrees and almost totally inhibited at 4 degrees [2]. in vivo: Levels of cidofovirin serum following intravenous infusion were dose proportional over the dose range of 1.0 to 10.0 mg/kg of body weight and declined biexponentially with an overall mean +/- standard deviation terminal half-life of 2.6 +/- 1.2 h (n = 25). Approximately 90% of the intravenous dose was recovered unchanged in the urine in 24 h. The overall mean +/- standard deviation total clearance of the drug from serum (148 +/- 25 ml/h/kg; n = 25) approximated renal clearance (129 +/- 42 ml/h/kg; n = 25), which was significantly higher (P < 0.001) than the baseline creatinine clearance in the same patients (83 +/- 21 ml/h/kg; n = 12) [3]. Positive CMV urine cultures reverted to negative in 2 of 8 patients receiving doses of < or = 1.5 mg/kg twice weekly and 11 of 13 patients receiving higher doses. Cidofovir has in vivo anti-CMV activity demonstrated by prolonged clearing of CMV viruria, although this observation is tempered by the fact that clearance of viremia could not be demonstrated [4].Toxicity: Patients receiving 0.5 or 1.5 mg/kg twice weekly experienced no serious toxicity. The first two patients who received 5 mg/kg twice weekly developed glycosuria and 2+ proteinuria. Subsequent patients received concomitant probenecid to attempt to ameliorate renal toxicity [4].Clinical trial: FDA approved drug
Y18501 is a oxysterol-binding protein (OSBPI) inhibitor with a similar structure to Oxathiapiprolin. Y18501 shows strong inhibitory activities against Phytophthora spp. and Pseudoperonospora cubensis, with EC50 ranging from 0.0005 to 0.0046 μg/mL. Y18501 shows excellent protective and curative activities against P. cubensis. Y18501 in combination with Chlorothalonil (HY-N6625) can significantly promote the inhibition of P. cubensis[1].
Adenallene, a nucleoside analogue, is an anti-HIV compound. Adenallene inhibits replication and cytopathic effect of HIV-1 and HIV-2[1].
QPX7728 is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. QPX7728 inhibits key serine and metallo beta-lactamases at a nano molar range[1].
Canadensolide is an antifungal metabolite of Penicillium canadense.
Fiztasovimab (NPC-21; EV2038) is a fully human IgG1λ mAb against human cytomegalovirus (hCMV). Fiztasovimab acts neutralizing activity by binding to the antigenic domain 1 of glycoprotein B on hCMV envelope. Fiztasovimab inhibits cell-to-cell transmission of hCMV[1].
Nucleoside-Analog-2 is a 4'-Azidocytidine analogue against Hepatitis C virus (HCV) replication.
Cefotiam hexetil hydrochloride (CTM-HE) is an oral third-generation cephalosporin, which is a prodrug of cefotiam, but has no anti-bacterial property. Cefotiam is an antibiotic[1].
Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities[1][2][3][4][5].
MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA)[1].
Bithionol sulfoxide(Bitin-S) is a clinically approved anti-parasitic drug; has been shown to inhibit solid tumor growth in several preclinical cancer models.IC50 value:Target: anticaner agentBithionol caused dose dependent cytotoxicity against all ovarian cancer cell lines tested with IC50 values ranging from 19 μM - 60 μM. BT treatment resulted in cell cycle arrest at G1/M phase and increased ROS generation [1]. Both bithionol and bithionol sulphoxide demonstrated in vitro toxicity to Neoparamoeba spp. at all concentrations examined (0.1 to 10 mg l(-1) over 72 h), with a comparable toxicity to freshwater observed for both chemicals at concentrations > 5 mg l(-1) following a 72 h treatment [2].
HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity[1].
Lenapenem (BO-2727 free acid), a carbapenem antibiotic, has potent antibacterial activity against Gram-positive and Gram-negative bacteria including P. aeruginosa[1].
Calceolarioside A is phenylethanoid glycoside with moderate binding affinity on HIV gp41[1].
Antibacterial agent 107 (compound 14) is a potent antibacterial agent. Antibacterial agent 107 shows potent antibacterial activity against Gram-positive bacteria, with a MIC of 1.56 μg/mL (MRSA). Antibacterial agent 107 exhibits low hemolytic activity, high membrane selectivity, and rapid bactericidal activity. Antibacterial agent 107 shows effective in vivo efficacy in the murine model of bacterial keratitis caused by Staphylococcus aureus ATCC29213[1].
HIV-1 inhibitor-31 (compound 4) is a potent HIV-1 inhibitor. HIV-1 inhibitor-31 can be used for researching AIDS[1].
MK-3402 is a metallo-beta-lactamase inhibitor (Example 303 in reference patent). MK-3402can be used in the research of bacteria[1].