Distamycin A (NSC-82150), an oligopeptide antibiotic, is a minor groove binder which binds to B-form DNA, preferentially at A/T rich sites.Distamycin A can change Enediyne-induced DNA cleavage sites and enhances apoptosis[1][2][3].
Antifungal agent 74 (compound 3c) is a potent antifungal agent that displays excellent fungicidal activity against C. arachidicola and R. solani. Antifungal agent 74 exerts its fungicidal activity by disrupting steroid biosynthesis and ribosome biogenesis in eukaryotes[1].
Myclobutanil is a conazole class fungicide widely used as an agrichemical.
Caprazol is a core structure of Caprazamycin (HY-N9425)[1].
Reltecimod (AB-103) is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod can be used to research necrotizing soft-tissue infections (NSTIs)[1][2].
HCV-IN-30 (compound 48) is a HCV NS5A replication complex inhibitor, with IC50s of 901 and 102 nM for genotypes 1a and 1b replicons, respectively[1].
Eleutherol is a naphthalene isolated from E. americana with antifungal activities[1]. Eleutherol is against yeasts Candida albicans, C. tropicalis, Saccharomyces cerevisiae and Cryptococcus neoformans with MIC values between 7.8 µg/mL and 250 µg/mL[1]. Eleutherol inhibits α-glucosidase function with an IC50>1.00 mM[2].
Cephaloridine hydrate is a broad-spectrum antibacterial antibiotic. Cephaloridine has certain dose-related nephrotoxicity[1][2].
Demeclocycline is an orally active tetracycline antibiotic. Demeclocycline impairs protein synthesis by binding to the 30S ribosomal subunit to inhibit binding of aminoacyl tRNA. Demeclocycline shows anti-bacterial activitise to a wide variety of bacterial infections[1][2].
LeuRS-IN-1 hydrochloride is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS-IN-1 hydrochloride has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively[1]. LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM)[2].
Cleistanthin B (Diphyllin O-glucoside) is an orally active arylnaphthalene lignan lactone glycoside. Cleistanthin B exhibits anti-SARS-CoV-2 effects in Vero cells, with EC50 of 6.51 µM. Cleistanthin B also exhibits antitumor, diuretic and antihypertensive effects in vivo[1][2][3][4].
Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis; B-type AChR activator.
Noraucuparin is a biphenyl-type phytoalexin. Noraucuparin has antifungal effect. Noraucuparin can be isolated from the leaves of Sorbus pohuashanensis[1].
Clonostachydiol is an anthelmintic macrodiolide from the fungus Clonostachys cylindrospora (strain FH-A 6607)[1].
Methyl tanshinonate is a tanshinone, that can be isolated from Salvia miltiorrhiza (S. miltiorrhiza) Bunge (Lamiaceae). Methyl tanshinonate is a potent inhibitor of Mpro enzyme in SARS-CoV (IC50 = 21.1 µM). Methyl tanshinonate can be used for diabetes and SARS-CoV research[1][2][3].
EP2 is an antimicrobial peptide. EP2 has antibacterial and antifungal activities. EP2 inhibits E. gallinarum, P. pyocyanea, A. baumanii, K. terrigena with a MIC value of 11.4 μg/mL[1].
ST-193 is a potent broad-spectrum arenavirus inhibitor; inhibits Guanarito, Junin, Lassa and Machupo virus with IC50 values of 0.44, 0.62, 1.4 and 3.1 nM, respectively.
Dirithromycin(LY 237216) is a macrolide glycopeptide antibiotic by binding to the 50S subunit of the 70S bacterial ribosome to inhibit the translocation of peptides.Target: AntibacterialDirithromycin is a new macrolide with a spectrum and degree of in vitro antimicrobial activity similar to that of erythromycin. Compared with erythromycin, dirithromycin has a long elimination half-life enabling once-daily administration, and it also achieves a greater cellular:extracellular concentration ratio and higher concentration in some tissues. Multicentre double-blind clinical trials have shown dirithromycin to be similar in efficacy to erythromycin in the treatment of uncomplicated bacterial infections of the respiratory tract and of skin and soft tissues [1]. Dirithromycin offers some attractive pharmacokinetic properties. The long elimination half-life of dirithromycin allows once-daily dosing and higher and more prolonged tissue concentrations than are achievable with erythromycin. The spectrum of activity, adverse effect profile, clinical efficacy, and bacteriologic eradication rate of dirithromycin may be similar to those of erythromycin [2, 3].
Filibuvir is a potent, selective non-nucleoside inhibitor (NNI) of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase, and it binds noncovalently in the “Thumb 2” pocket of NS5B. In vitro, filibuvir is equipotent against genotype 1a and 1b replicons, with an EC50 of 59 nM[1].
2-Hydroxyacetophenone is a principal root volatile of the Carissa edulis[1]. 2-Hydroxyacetophenone shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC50 of 1.8 mM[2].
RO-9187 is a potent inhibitor of HCV virus replication with an IC50 of 171 nM.
PCL 016 is a topical antiviral agent, which inhibits adenovirus replication in rabbit.
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacterium tuberculosis H37Rv with a MIC value of 0.1 μg/mL[1].
PA3552-IN-1 (compound 15) is an antibiotic adjuvant that restores sensitivity of MDR P. aeruginosa DK2 strain to Polymyxin B. PA3552-IN-1 can reduce PA3552 expression[1].
Calphostin C is a potent and specific inhibitor of protein kinase C. Calphostin C is an antitumor antibiotic. Calphostin C has 1000 times more inhibitory to protein kinase C with an IC50 of 0.05 μM than other protein kinases. Calphostin C induces apoptosis in some tumor cell lines. Calphostin C has potent cytotoxic activity and antitumor activity[1].
FGI-106 tetrahydrochloride is a potent and broad-spectrum inhibitor with inhibitory activity against multiple viruses. FGI-106 tetrahydrochloride is active against Ebola, Rift Valley and Dengue Fever viruses with EC50s of 100 nM, 800 nM and 400-900 nM, respectively. FGI-106 tetrahydrochloride also inhibits non-hemorrhagic fever viruses HCV and HIV-1 with EC50s of 200 nM and 150 nM, respectively[1].
SEB Domain 144-153 is Staphylococcal Enterotoxin B domain amino acid residue 144-153. SEB Domain 144-153 inhibits transcytosis of multiple staphylococcal enterotoxins, SEA, SEE, and TSST-1. Staphylococcal enterotoxin B (SEB) is a toxin produced by Staphylococcus aureus[1].
WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. WX-081 exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for drug susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. WX-081 also inhibits hERG channel with the IC50 of 1.89 μM[1].
Mogroside III A2 is a cucurbitane glycoside. Mogroside III A2 can inhibit Epstein-Barr virus early antigen (EBV-EA) activation. Mogroside III A2 shows weak inhibitory effects on activation of NOR 1[1].
Quinfamide is an antiamebic agent. Quinfamide can be used to treat tropical parasitic infections such as Amoebiasis and Helminthiasis[1].