Lacto-N-fucopentaose I (LNFPI) is a human milk oligosaccharide (HMO), possessing antiviral and antibacterial activity. Lacto-N-fucopentaose I can reduce capsid protein VP1 to block virus adsorption, promote CDK2 and reduce cyclin E to recover cell cycle S phase block. Lacto-N-fucopentaose I inhibits ROS production and apoptosis in virus-infected cells. Lacto-N-fucopentaose I can also regulate intestinal microbiota to affect immune system development[1].
Inophyllum B ((+)-Inophyllum B) is a potent HIV Reverse Transcriptase inhibitor with an IC50 value of 38 nM. Inophyllum B inhibits HIV-1 (IC50=1.4 μM) in vitro cell culture. Inophyllum B can be isolated from the acetone extract of the giant African snail, Achatina fulica[1].
Pinokalant is a broad-spectrum and non-selectivecation channel inhibitor. Pinokalant significantly reduces cortical infarct volume. Pinokalant o improves the metabolic and electrophysiologic status of the ischemic penumbra. Pinokalant reduces lesion size on magnetic resonance images in the acute phase following middle cerebral artery occlusion in rats. Pinokalant has the potential for the research of stroke. Pinokalant also shows anti-SARS-CoV-2 activity[1].
AN0128 is a boron-containing antibacterial and anti-inflammatory agent. AN0128 against S. aureus, S. epidermidis, P. acnes, B. subtilis with minimum inhibitory concentration (MIC) values of 1, 0.5, 0.3, 1 μg/mL. AN0128 can be used for the research of periodontal disease and cutaneous diseases[1][2].
Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].
(±)-Hydnocarpin is a flavonolignan. (±)-Hydnocarpin can inhibit the growth of S. aureus with a MIC50 value of 3.1 μM[1].
Oosponol is a dopamine beta-hydroxylase inhibitor exhibiting hypotensive effects.Oospongol has strong antifungal activity against many antagonistic fungi[1][2].
Terminolic acid is a pentacyclic triterpenoid glucoside isolated from Combretum racemosum. Terminolic acid can inhibit the pro-inflammatory cytokines by binding to receptor active site of IL-1β and IL-6, and enhance anti-inflammatory cytokines by binding to IL-4 receptor binding sites. Terminolic acid also exhibits moderate antibacterial activity[1][1].
NSC5844 is a 4-aminoquinoline derivative, with antitumor and antimalarial activity.
Ceftazidime pentahydrate (GR20263 pentahydrate) is a third generation cephalosporin administered intravenously or intramuscularly. Ceftazidime pentahydrate has a broad spectrum of in vitro activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime pentahydrate is particularly active against Enterobacteriaceae (including beta-lactamase-positive strains) and is resistant to hydrolysis by most beta-lactamases[1].
Lycorenine is an alkaloid that has vasodepressor action. Lycorenine also exhibits anticancer and antibacterial activities[1][2][3].
Suptavumab (REGN2222) is a human monoclonal antibody. Suptavumab can bind and block a conserved epitope on RSV A and B subtypes. Suptavumab can be used for the research of RSV infection[1][2].
TP-6076 is a fully synthetic fluorocycline antibiotic, acts function via binding to the 30S ribosomal subunit and maintains its activity. TP-6076 displays potent mechanism-based antitranslational activity (Tet protein, IC50=0.18 μg/mL), shows a wide range of antimicrobial and antiparasitic activities[1][2].
Valopicitabine (NM283), an efficient prodrug of the potent anti-HCV agent 2'-C-methylcytidine, acts as a promising antiviral agent for reasearch of chronic HCV infection[1].
L-Norleucine-d9 ((S)-2-Aminohexanoic acid-d9) is the deuterium labeled L-Norleucine. L-Norleucine ((S)-2-Aminohexanoic acid) is an isomer of leucine, specifically affects protein synthesis in skeletal muscle, and has antivirus activity.
3-Oxobetulin, an antifungal agent, shows antifungal activities against white rot fungus L. betulina and the brown rot fungus L. sulphureus[1].
F8-S43-S3 is an inhibitor of SARS-CoV-2 main protease, with an IC50 of 9.69 μM[1].
Lanopepden (GSK 1322322) is a peptide deformylase inhibitor active against Staphylococcus aureus strains with MICs of 1 and 1 mg/L for ATCC 29213 and ATCC 25923 strain, respectively[1].
Albendazole D3 is the deuterium labeled Albendazole, which is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations[1].
Chitin synthase inhibitor 13 (compound 12g) is a non-competitive inhibitor of chitin synthase, with an IC50 of 106.7 μM. Chitin synthase inhibitor 13 exhibits a broad-spectrum of antifungal activity[1].
PC190723 (Compound 2) is an inhibitor of the bacterial cell division protein FtsZ with an IC50 of 55 ng/ml. FtsZ-IN-3 exhibits anti-staphylococcal activity with MIC values of 1 µg/ml for MSSA and MRSA[1].
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment[1][2][3][4].
Lascufloxacin (KRP-AM1977X) is a potent and orally active fluoroquinolone antibacterial agent. Lascufloxacin potently inhibits infections caused by various pathogens, including quinolone-resistant strains. Lascufloxacin has the potential for various infectious diseases treatment, including lower respiratory tract infections[1][2].
AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV)[1][2][3][4].
Ganoderone A is a triterpene compound that can be isolated from the fruiting body of Ganoderma pfeifferi and Ganoderma calidophilum. Ganoderone A has antiviral activity against HSV with IC50 value of 0.3 µg/mL. Ganoderone A has potential applications in viral infections and tumors[1][2][3].
Panobacumab (KBPA101) is a fully human IgM/κ monoclonal antibody generated by immortalizing human B lymphocytes against the LPS O polysaccharide of serotype O11 of P. aeruginosa[1].
Retapamulin(SB-275833) is a topical antibiotic, which binds to both E. coli and S. aureus ribosomes with similar potencies with Kd of 3 nM.IC50 Value: 3 nM(Kd, E.coli)Target: AntibacterialRetapamulin is a topical antibiotic developed by GlaxoSmithKline. Retapamulin(SB-275833) is the first drug in the new class of pleuromutilin antibiotics to be approved for human use.Retapamulin(SB-275833) is marketed as an ointment under the brand names Altabax and Altargo. Retapamulin(SB-275833) is useful for Antibiotics.
Sulfoxone (Aldesulfone) disodium is an orally active sulphonamide antibiotic that is used against leprosy. Sulfoxone disodium can also be used in study of dermatitis herpetiformis[1][2].
BAY 57-1293 represents a new class of potent inhibitors of herpes simplex virus (HSV) that target the virus helicase primase complex.IC50 Value: 20 nM (HSV-1) [1]Target: HSVin vitro: BAY 57-1293 is nearly two orders of magnitude more potent than acyclovirin vitro and the superiority was even more prominent when the viral load was increased (BAY 57-1293 IC50 = 12 nM, 20 nM and 50 nM; acyclovir IC50 = 1uM, 3M and 10 50 uM at a multiplicity of infection (m.o.i.) of 0.0025, 0.02 and 0.2, respectively). A minor increase in IC50 values at higher viral loads was observed for all thiazolyl compounds listed in Table 1. BAY 57-1293 was also active against porcine (IC50 = 5 uM) and bovine (IC50 = 0.12 uM) herpes strains [1].in vivo: Delayed treatment with BAY 57-1293 (20 mg/kg 2× daily per os, treatment day 4-14) abrogates progression of disease symptoms (mean of 10 animals per group) of HSV-2 infected guinea pigs within 1 d of treatment and healing is observed subsequently, whereas a 7.5 fold higher dose of valacyclovir (150 mg/kg 2× daily) shows marginal therapeutic efficacy compared with placebo [1]. The compound given orally, or intraperitoneally once per day at a dose of 15 mg/kg for 4 successive days was equally effective or superior to a much higher dose of famciclovir (1mg/ml, i.e. approximately 140-200mg/kg/day) given in the drinking water for 7 consecutive days, which, in our hands, is the most effective method for administering famciclovir to mice [2].Toxicity: Exploratory toxicology and safety pharmacology studies did not reveal any safety relevant findings at 30, 100 and 300 mg/kg BAY 57-1293 (once daily per os) in a 4-week chronic toxicity study in dogs. However, administration of the same dose to rats for 4 weeks resulted in a dose-dependent transitional hyperplasia of the urinary bladder epithelium [1].
AB131 is a MSMEG 6649 and Rv2172c inhibitor (Kd: 0.16 and 0.02 μM respectively). AB131 can sensitize the antimycobacterial activity of the antitubercular agent[1].