Fluazinam impurity 1 is an impurity of Fluazinam with antifungal activity. Fluazinam impurity 1 is active against Sphaerotheca fuliginea, Pyricularia oryzae and Rhizoctonia solani[1].
Tioxazafen is a disubstituted oxadiazole and a broad-spectrum seed treatment nematicide. Tioxazafen is designed to provide consistent broad-spectrum control of nematodes in corn, soy, and cotton[1].
Naringenin is the predominant flavanone in grapefruit; displays strong anti-inflammatory and antioxidant activities.
Viridicatol, a quinolinone alkaloid, is isolated from the fermentation of an endophytic fungus Penicillium sp. R22 in Nerium indicum. Viridicatol has strong antifungal activity against Staphylococcus aureus with MIC value of 15.6 μg/mL[1].
Butenafine hydrochloride is a synthetic benzylamine antifungal, works by inhibiting the synthesis of sterols by inhibiting squalene epoxidase.IC50 Value: Target: Antifungal; squalene epoxidaseButenafine Hydrochloride, a benzylamine derivative, is an antifungal which is used to control dermal fungal infections such as athletes foot and ring worm. Butenafine Hydrochloride is squalene epoxidase inhibitor, inhibits the synthesis of ergosterol needed in fungal cell membranes. The drug has excellent penetration into the epidermis and a prolonged retention time following topical application, conferring residual therapeutic activity after treatment cessation. Butenafine possess anti-inflammatory activity too. Butenafine hydrochloride 1% cream is safe and effective for tinea corporis cruris and tinea manuum pedis.
KIN101 is a potent RNA viral inhibitor with IC50s of 2 μM, >5 μM for influenza virus and Dengue virus (DNV), respectively. KIN101, an isoflavone agonist of IRF-3 dependent signaling, induces IRF-3 nuclear translocation. KIN101 has broad-spectrum activity against RNA viruses[1][2].
VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases[1][2][3][4].
Dehydroandrographolide is extracted from herbal medicine Andrographis paniculata (Burm f) Nees; alleviate oxidative stress in LPS-induced acute lung injury possibly by inactivating iNOS.
Clorsulon is used in the treatment of Fasciola hepatica infections in calves and sheep.Target: AntiparasiticClorsulon is a competitive inhibitor of both 3-phosphoglycorate and ATP and had a Ki of 0.29 mM, inhibits glucose utilization and acetate and propionate formation by mature Fasciola hepatica in vitro. [1] Clorsulon (a single dose of 15 mg/kg) is effective in removing over 90% of immature Fasciola hepatica from sheep (6 weeks after infection) and calves (8 weeks after infection). A 2.5 mg/kg dose removed over 90% of mature (16 weeks old) liver fluke from sheep [1]. Clorsulon causes severe disruption to the tegument and gut of Fasciola hepatica after in vivo incubation [2].
Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A is a promising photosensitizer for anticancer photodynamic therapy (PDT)[1][2][3][4].
Erysotrine, isolated from seed pods of Erythrina latissima, shows antibacterial activities[1].
MmpL3-IN-1 (compound 32) is a potent Mycobacterial membrane protein large 3 (MmpL3) inhibitor. MmpL3-IN-1 has anti-tuberculosis activity with the MIC<0.016 μg/mL in M. tuberculosis and can be used in studies of drug-resistant tuberculosis[1].
Dapivirine(TMC 120, TMC 120 R147681) is a NNRTI for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates.IC50 value: 24 nM [1]Target: HIV reverse transcriptase; NNRTIsin vitro: TMC120-R147681 is a diarylpyrimidine with high activity against wild-type and mutant HIV. A 24-h treatment with 1,000 nM UC-781 or 100 nM TMC120-R147681 prevented cell-free HIV infection, whereas 10-fold-higher concentrations blocked cell-associated HIV, TMC120-R147681 apparently blocked infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration [1]. Dapivirine is well tolerated by epithelial cells, T cells, macrophages, and cervical tissue explants with CC50 (50% cytotoxic concentration) of 10 μM to 20 μM. Dapivirine potently inhibits infection by both X4- and R5-utilizing HIV-1 strains with IC50 of 1.46 nM in cell-based assays. Dapivirine potently inhibits HIV-1BaL infection of human ectocervical explant tissue in a dose-dependent manner, as evaluated by the reduction in both p24 release and provirus content in cultured explants. Dapivirine inhibits the transmission of virus to permissive T cells in a dose-dependent manner, with an IC50 of 0.1 nM. Dapivirine results in significant inhibition of HIV infection when explants are challenged with virus immediately with IC90 of 100 nM. Dapivirine is also able to inhibit viral dissemination by migratory cells [2].in vivo: Dapivirine-containing gel at vaginal level inhibits cell-associated HIV infection in mice [3]. More placebo (7 of 12) than Dapivirine (3 of 24) gel users has positive vaginal swab results, with white blood cells being the most common finding. Dapivirine (0.05%) results in Cmax of 715 pg/mL, AUC of 15 ng×h/mL and T1/2 of 89.87 hours in plasma after 14 days post-dose. Mean Dapivirine (0.05%) concentrations in vaginal fluids collected at the introitus, mid vagina, and cervix are in the range of 62-265 μg/g on day 1 [4].
3-Deoxysappanchalcone is a naturally-occurring chalcone compound isolated from Caesalpinia sappan L. (Leguminosae), which possesses anti-allergic, antiviral, anti-inflammatory and antioxidant activities. 3-Deoxysappanchalcone exerts anti-inflammatory activity via induce heme oxygenase-1 (HO-1) expression by activating the AKT/mTOR pathway in murine macrophages. 3-Deoxysappanchalcone also exhibits anti-influenza virus activity (H3N2, IC50 = 1.06 μM)[1][2].
Neticonazole hydrochloride is an imidazole derivative and a potent and long-acting antifungal agent. Neticonazole hydrochloride is also an orally active exosome biogenesis and secretion inhibitor. Neticonazole hydrochloride has anti-infection and anti-cancer effects[1][2][3].
Voxilaprevir (GS-9857) is a fluorinated macrocyclic hepatitis C virus (HCV) nonstructural protein (NS) 3/4A protease inhibitor with potent in vitro antiviral activity against genotypes 1-6 HCV and broad coverage of NS3/4A protease polymorphisms. GS-9857 improves coverage against commonly encountered NS3 resistance-associated variants (RAVs)[1][2].
2'-OMe-G(ibu) Phosphoramidite is a modified phosphoramidite monomer, which can be used for the oligonucleotide synthesis.
Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC50 of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, cocaine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential treatment for multiple forms of drug abuse[1]. Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis[2].
1-Kestose, the smallest fructooligosaccharide component, which efficiently stimulates Faecalibacterium prausnitzii as well as Bifidobacteria.
RO8191 (RO4948191), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon[1].
Moracin D is a flavonoid that can be isolated from Morus alba. Moracin D induces cell apoptosis and shows hypoglycemic, antiadipogenic, antifungal and antitumor effects. Moracin D can be used for fungal infection and breast cancer research[1][2][3].
Coblopasvir (KW136, KW-136) is a novel HCV NS5A inhibitor under development for treatment of HCV infection. HCV Infection Phase 3 Clinical
Koaburaside is a cytoprotective and anti-inflammatory natural compound. Koaburaside shows antioxidant activity with an IC50 of 9.0 μM for DPPH-free radical scavenging assay. Koaburaside inhibits histamine release and expressions of IL-6 and TNF-α in human mast cells. Koaburaside also effectively inhibits influenza A neuraminidase[1].
CP19, a histamine receptor antagonist, is an entry inhibitor against both Ebolavirus (EBOV) and Marburgvirus (MARV) with IC50s of 3.4 μM and 29.5 μM, respectively. CP19 has SI values of 29.4 and 3.4 for EBOV and MARV, respectively. CP19 has antiviral activity[1].
Doxycycline (hyclate) is a tetracycline antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor.
2-Phenylacetophenone has broad-spectrum efflux pump inhibition activity. 2-Phenylacetophenone is a benzoin derivative used as a photoinitiator in vinyl polymerization[1].
HIV-1 inhibitor-45 (compound IA-6) is a potent HIV-1 RNase H inhibitor with an IC50 value of 0.067 μM. HIV-1 inhibitor-45 shows an antiviral activity[1].
cOB1 phermone, a bacterial sex pheromone, effectively inhibits multidrug-resistant Enterococcus faecalis V583[1].
Marbofloxacin hydrochloride is a potent antibiotic of which depends upon its inhibition of DNA-gyrase.Target: DNA-gyraseMarbofloxacin hydrochloride is a third-generation fluoroquinolone for veterinary use, the antimicrobial of which depends upon its inhibition of DNA-gyrase and topoisomerase IV. With a broad spectrum bactericidal activity and good efficacy, marbofloxacin hydrochloride is indicated for dermatological, respiratory and urinary tract infections due to both Gram-positive and Gram-negative bacteria and Mycoplasma [1].Administration of Marbofloxacin hydrochloride at 6 mg/kg once daily for 7 days in a Staphylococcus aureus infection in tissue cages in ponies is not effective for the elimination of S. aureus infections from secluded sites [2]. The pharmacokinetic properties of marbofloxacin hydrochloride were investigated in 6 horses after i.v., subcutaneous and oral administration of a single dose of 2 mg/kg bwt and the minimal inhibitory concentrations (MIC) assessed for bacteria isolated from equine infectious pathologies. The clearance of marbofloxacin hydrochloride was mean +/- s.d. 0.25 +/- 0.05 l/kg/h and the terminal half-life 756 +/- 1.99 h. The marbofloxacin hydrochloride absolute bioavailabilities after subcutaneous and oral administration were 98 +/- 11% and 62 +/- 8%, respectively. Considering the breakpoint values of efficacy indices for fluoroquinolones, a marbofloxacin hydrochloride dosage regimen of 2 mg/kg bwt/24 h by i.v., subcutaneous or oral routes was more appropriate for enterobacteriaceae than for S. aureus [3]. Toxicity: cramps; vomiting; anorexia; soft stools; diarrhoea
Ampicillin is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.