Ajoene, a garlic-derived compound, is an antithrombotic and antifungal agent. Ajoene inhibits proliferation and induces apoptosis of human leukaemia CD34-negative cells including HL-60, U937, HEL and OCIM-I. Anticancer activities[1][2].
PNU-103017 is an HIV protease inhibitor.
CMX001 (Brincidofovir; HDP-CDV) was developed as an orally active, lipophilic form of cidofovir (CDV); has enhanced activity in vitro and in vivo compared to CDV against certain herpesviruses, adenoviruses and orthopoxviruses.IC50 Value: 5.5 nM (EC50, in PDA at 7 dpi) [3]Target: anti-CMVCMX001 is currently in Phase II clinical studies for development as a therapeutic agent for human CMV, adenovirus and BK virus infections, as well as, for adverse events following smallpox vaccinations.in vitro: In PDA at 7 dpi, the CMX001 50% effective concentration (EC50) was 5.55 nM, the 50% cytotoxic concentration (CC50) was 184.6 nM, and the 50% selectivity index (SI50) was 33.3. The EC90 was 19.7 nM, the CC90 was 5,054 nM, and the SI90 was 256.1. In COS-7 cells, JCV replication was faster and the EC50 and EC90 were 18- and 37-fold higher than those in PDA, i.e., 0.1 μM and 0.74 μM (CC50, 0.67 μM; SI50, 6.7; CC90, 12.2 μM; SI90, 16.5) at 5 dpi [3].in vivo: CMX001 and CDV are equally efficacious at protecting mice from mortality following high ectromelia virus doses (10,000 x LD(50)) introduced by the intra-nasal route or small particle aerosol. Using CMX001 at a 10mg/kg dose followed by 2.5mg/kg doses every other-day for 14 days provided solid protection against mortality and weight loss following an intra-nasal challenge of (100-200) x LD(50) of ectromelia virus [1]. When CMX001 was administered orally to mice infected with HSV-1, mortality was reduced significantly (p≤0.001) with all three dose levels when treatments were initiated 24 h post viral inoculation. When treatments were started 48 h post viral inoculation, 5 and 2.5 mg/kg significantly reduced mortality (p≤ 0.001). If treatments were delayed until 72 h post viral inoculation, CMX001 did not reduce mortality or increase the mean day to death. When mice were infected intranasally with HSV-1 and treatments initiated 24 h post viral inoculation using CMX001 at 5 mg/kg or ACV at 100 mg/kg, virus replication in target organs was reduced by both CMX001 and ACV when compared to vehicle treated mice [2]. Toxicity: Diarrhea was the most common adverse event in patients receiving CMX001 at doses of 200 mg weekly or higher and was dose-limiting at 200 mg twice weekly. Myelosuppression and nephrotoxicity were not observed [4].
Metconazole-d6 is the deuterium labeled Metconazole. Metconazole is a triazole fungicide agent.
AzddMeC (CS-92) is an antiviral nucleoside analogue and a potent potent, selective and orally active HIV-1 reverse transcriptase and HIV-1 replication inhibitor. In HIV-1-infected human PBM cells and HIV-1-infected human macrophages, the EC50 values of AzddMeC are 9 nM and 6 nM, respectively[1][2].
Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
α-Terpineol is isolated from Eucalyptus globulus Labill, exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria[1].α-Terpineol possesses antifungal activity against T. mentagrophytes, and the activity might lead to irreversible cellular disruption[2].
Ensitrelvir (S-217622) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM)[1][2].
Sanguisorbigenin is a natural antibacterial agent that inhibits methicillin-resistant S. aureus (MRSA)[1].
Debrisoquin (Isocaramidine) is a TMPRSS2 inhibitors that inhibits SARS-CoV-2 entry into human lung cell line by a TMPRSS2-depedent manner, with an IC50 of 22μM. Debrisoquin can be used for antiviral research[1].
Grepafloxacin (OPC-17116) is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile[1][2][3].
Antifungal agent 67 (compound 9) is an imidazole antifungal agent that is effective against Candida. Antifungal agent 67 has a CC50 value of 33.6 μM on healthy neonatal rat cardiomyoblasts[1].
Cefotetan is a semisynthetic cephamycin antibiotic that exerts its bactericidal effects by inhibition of cell-wall synthesis[1].
Juglone is a yellow pigment found in black walnut (Juglans regia). Juglone also shows antimicrobial activity[1].
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
Acetazolamide sodium is the sodium salt of Acetazolamide. Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX. Acetazolamide has diuretic, antihypertensive and anti-gonococcal activities[1][4][5][6].
Cefcapene pivoxil hydrochloride, an antibiotic, is an orally active and potent 3rd-generation cephalosporin with a wide spectrum of anti-bacterial activity[1].Cefcapene pivoxil hydrochloride has the potential for the palmoplantar pustulosis (PPP) treatment[2].
Pimeloyl-CoA is a biotin precursor of Escherichia coli. Pimeloyl-CoA can be used for the research of the pathway of de novo biotin biosynthesis in Escherichia coli[1].
1-O-Methylemodin is a nature product that could be isolated from Zopfiella longicaudata. 1-O-Methylemodin has antifungal activity[1].
Ecabet sodium (TA-2711) is currently applied to some clinical gastrointestinal disease by inhibiting the ROS production and improving Helicobacter pylori eradication[1]. Ecabet sodium reduces apoptosis[2].
Fenbendazole is a broad spectrum benzimidazole anthelmintic used against gastrointestinal parasites.Target: AntiparasiticFenbendazole is a broad spectrum benzimidazole anthelmintic used against gastrointestinal parasites including: giardia, roundworms, hookworms, whipworms, the taenia species of tapeworms(It is effective against the Taenia species of tapeworm but not against the common tapeworm, Dipylidium caninum.), pinworms, aelurostrongylus, paragonimiasis, strongyles and strongyloides and can be administered to sheep, cattle, horses, fish, dogs, cats, rabbits and seals. Drug interactions may occur if using bromsalan flukicides such as dibromsalan and tribromsalan. Abortions in cattle and death in sheep have been reported after using these medications together. Fenbendazole is poorly absorbed from the gastrointestinal tract in most species. The LD50 in laboratory animals exceeds 10 g/kg when administered orally. From Wikipedia.
Methacycline HCl is a tetracycline antibiotic.Target: Antibacterial Methacycline HCl is a broad-spectrum semisynthetic antibiotic related to tetracycline but excreted more slowly and maintaining effective blood levels for a more extended period.
RSV-IN-2 is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus fusion proteins (wild-type, EC50 = 0.27 nM; D486N-mutant, EC50 = 0.70 nM).
Sarafloxacin hydrochloride is a quinolone antibiotic drug.Target: Antibacterialsarafloxacin hydrochloride is a fluoroquinolone antibiotic registered for use against poultry diseases. Sarafloxacin treatment demonstrated mineralization to 14CO2 amounting to 0.58%, 0.49%, and 0.57% in loam, silt loam, and sandy loam soils, respectively, at the termination of the test [1]. The inhibitory level of sarafloxacin for the tested bacteria was strain dependent. It appeared that in broth culture Escherichia coli isolates were sensitive to sarafloxacin concentrations 5-fold lower than the concentrations present in the simulated gut model, suggesting that sarafloxacin may be partially unavailable due to absorption to organic matter in the model [2]. Administering Sarafloxacin hydrochloride in the feed for 5 d at a dose of 10 or 12.5 mg/kg of fish proved efficacious in treating channel catfish infected with E. ictaluri in all three field trials. Average survival of the nonmedicated group was 43% in trial 1, 11°% in trial 2, and 59% in trial 3. Survival of the corresponding Sarafloxacin hydrochloride-medicated groups averaged 68, 48, and 73%. Antibiotic therapy with Sarafloxacin hydrochloride significantly (P < 0.05) improved survival in all trials [3].
Ethionamide(2-ethylthioisonicotinamide) is an antibiotic used in the treatment of tuberculosis.Target: AntibacterialEthionamide is a second-line antitubercular agent that inhibits mycolic acid synthesis. It also may be used for treatment of leprosy. Ethionamide is a prodrug. It is activated by the enzyme EthA, a mono-oxygenase in Mycobacterium tuberculosis, and binds NAD+ to form an adduct which inhibits InhA in the same way as isoniazid. Expression of the ethA gene is controlled by EthR, a transcriptional repressor. It is understood that improving ethA expression will increase the efficacy of ethionamide and so EthR inhibitors are of great interest to co-drug developers. The action may be through disruption of mycolic acid [1, 2].
Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 and 1.5μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1[1][2][3][4].
Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase[1]. Rifalazil (KRM-1648; ABI-1648) is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis with MIC values from 0.00025 to 0.0025 μg/ml[3]. Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of Chlamydia infection, Clostridium difficile associated diarrhea (CDAD), and tuberculosis (TB)[2].
Papyracillic acid, a fungal metabolite, a Penicillic acid analog, is a nonselective herbicide. Papyracillic acid has anti-bacterial, anti-fungal, nematicidal, and phytotoxic effects[1].
Peptide 5g is an antimicrobial peptide. Peptide 5g inhibits E. coli, S. aureus, and C. albicans with MIC values of 30, 10, 12.5 μg/mL respectively[1].