Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV[1][2][3].
Phenoxyethanol-d2 is the deuterium labeled Phenoxyethanol[1]. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[2].
PfGSK3/PfPK6-IN-2 is a potent dual PfGSK3/PfPK6 (Plasmodium falciparum GSK3/PK6) inhibitor (IC50: 172 nM and 11 nM respectively). PfGSK3/PfPK6-IN-2 can be used in the research of Malaria[1].
Erythromycin A enol ether is an acidic degradation product of Erythromycin A (macrolide antibiotic) and has no antibacterial effect[1][2].
Antibacterial agent 35, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Methyl anthranilate, a plant spice extract, is a quorum sensing inhibitor and anti-biofilm agent against Aeromonas sobria. Methyl anthranilate has been widely employed for the preparation of edible flavor and food additives in food processing industries[1].
Mafenide is a sulfonamide-type medication.Target: AntibacterialMafenide is a sulfonamide-type medication. Mafenide works by reducing the bacterial population present in the avascular tissues of burns and permits spontaneous healing of deep partial-thickness burns. It is used to treat severe burns. It is used topically as an adjunctive therapy for second- and third-degree burns. It is bacteriostatic against many gram-positive and gram-negative organisms, including Pseudomonas aeruginosa. Some sources state that mafenide is more appropriate for non-facial burns, while chloramphenicol/prednisolone or bacitracin are more appropriate for facial burns [1-3].
Ledipasvir acetone is the active pharmaceutical ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
(R)-Eucomol, a flavonoid derivative, displays marginal antibacterial activity. (R)-Eucomol shows cytotoxic activity against KB and P-388 cells[1].
Hardwickiic acid ((-)-Hardwikiic acid) is an antinociceptive compound that blocks Tetrodotoxin-sensitive voltage-dependent sodium channels. Hardwickiic acid shows insecticidal activity[1][2].
HIV-1 protease-IN-11 (compound 34a) is a HIV-1 protease inhibitor with an IC50 of 0.41 nM. HIV-1 protease-IN-11 also exhibits significant activity against drug-resistant variant[1].
Helvolic acid (Fumigacin) is an antibiotic isolated from Xylaria sp, active against the Gram-positive bacteria[1].
TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
Antimycobacterial agent-4 is a 2-amino-4-(2-pyridyl) thiazole derivative, with antimycobacterial activity, antiplasmodial activity, and cytotoxicity on a mammalian cell line[1][2].
3,5-Dicaffeoyl-epi-quinic acid can be extracted from Chrysanthemum morifolium. 3,5-Dicaffeoyl-epi-quinic acid has antioxidant activities. 3,5-Dicaffeoyl-epi-quinic acid can scavenge DPPH radical and superoxide anion radical, with IC50s of 5.6 and 2.9 μg/mL respectively[1].
Sulfanitran is a sulfonamide antiinfective drug.
p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties[1].
Voriconazole (UK-109496) camphorsulfonate is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole camphorsulfonate exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes[1][2].
Pirlindole is a novel potent inhibitor of Enteroviruse that targets Viral Protein 2C, inhibits EV-B and EV-D through the inhibition of genome replication (CV-B3 EC50=9.91 uM).
Cyclotriazadisulfonamide (CADA) is a specific CD4-targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibits the co-translational translocation of human CD4 (huCD4) into the ER lumen in a signal peptide (SP)-dependent way[1][2].
Delafloxacin meglumine is a fluoroquinolone antibiotic agent.IC50 Value: MICs ranging from 0.0078 to 0.125 micro g/ml for levofloxacin-resistant Streptococcus pneumoniae strains [1]Target: AntibacterialABT-492 was more potent against quinolone-susceptible and -resistant gram-positive organisms, had activity similar to that of ciprofloxacin against certain members of the family Enterobacteriaceae, and had comparable activity against quinolone-susceptible, nonfermentative, gram-negative organisms.in vitro: ABT-492 exhibited excellent in vitro activities against all 326 aerobic and anaerobic antral puncture sinus isolates tested with MICs (in micrograms per milliliter) at which 90% of the isolates tested were inhibited as follows: Haemophilus influenzae, 0.001; Moraxella catarrhalis, 0.008; and Streptococcus pneumoniae, 0.015 [2]. ABT-492 was as active as trovafloxacin against Chlamydia trachomatis, indicating good intracellular penetration and antibacterial activity [3].in vivo:Clinical trial:
AWZ1066S is a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis, with an EC50 of 2.5 nM in cell assay[1].
Penciclovir (VSA 671) sodium is a potent and selective anti-herpesvirus agent with EC50 values of 0.5, 0.8 µg/ml for HSV-1 (HFEM), HSV-2 (MS), respectively. Penciclovir sodium shows anti-herpesvirus activity with no-toxic. Penciclovir sodium preventes mortality in mouse[1][2].
Malonomicin (Antibiotic K16) is an antibiotic with anti-protozoa and anti-trypanosome activities. Malonomicin also shows anti-trypanosome activity in vivo[1][2].
Maximin 9 is an antimicrobial peptide derived from toad Bombina maxima[1].
Clorobiocin is a MlaC protein inhibitor that could bind to the MlaC protein. Clorobiocin has antibacterial effects[1].
Resveratrol (SRT 501), a natural polyphenol that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. It has a wide spectrum of targets including mTOR, JAK, β-amyloid.
Banksialactone A is the metabolite of an Australian fungus, Aspergillus banksianus[1].
β-Lactamase-IN-7 (compound 14) is a potent VIM-Type metallo-β-lactamase inhibitor, with Kis of 1.26 μM and 0.54 μM for VIM-1 and VIM-4, respectively. β-Lactamase-IN-7 can effectively inhibit Klebsiella pneumoniae[1].
Abietic acid, a diterpene isolated from Pimenta racemosa var. grissea, possesses antiproliferative, antibacterial, and anti-obesity properties. Abietic acid inhibits lipoxygenase activity for allergy treatment[1][2].