ML344 is a CqsS/LuxQ agonist probe that acts as an inducer of light production without autoinducers.
SARS-CoV-2-IN-68 (compound 6C) is a covalent SARS-CoV-2 PLpro/Mpro inhibitor with potent antiviral activities. SARS-CoV-2-IN-68 binds to Zn-finger domain of PLpro[1].
1-Monomyristin, extracted from Serenoa repens, inhibits the hydrolysis of 2-oleoylglycerol (IC50=32 μM) and fatty acid amide hydrolase (FAAH) activity (IC50=18 μM). 1-Monomyristin shows antibacterial activity against Staphylococcus aureus and Aggregatibacter actinomycetemcomitans and also antifungal activity against Candida albicans[1][2][3].
Senecivernine is a pyrrolizidine alkaloid isolated from Senecio species, exhibits a weakly mutagenic activity[1][2].
Micafungin sodium (FK 463) is an antifungal agent which inhibits 1, 3-beta-D-glucan synthesis.
Calcium mesoxalate blocks HIV-1 RT (IC50: 2.2 μM)[1][2].
Harzianum A is a trichothecene that isolated from the soil-borne fungus Trichoderma harzianum. Harzianum A shows no cytotoxicity against baby hamster kidney cells, no activity against Gram-negative and Gram-positive bacteria, but modest antifungal activity at 100 μg/mL[1].
Prostratin, a natural terpenoid compound, is a PKC activator, with a Ki of 12.5 nM and shows inhibitory effect on HIV-1.
HCV Core Protein (59-68) is a peptide containing residues 59-68 of the HCV core protein[1].
LED209 is a potent small molecule inhibitor of bacterial receptor QseC, is a potent prodrug that is highly selective for QseC. Target: AntibacterialLED209 has desirable pharmacokinetics and does not present toxicity in vitro and in rodents. This is a unique antivirulence approach, with a proven broad-spectrum activity against multiple Gram-negative pathogens that cause mammalian infections.The LED209 QseC inhibitor has a unique mode of action by acting as a prodrug scaffold to deliver a warhead that allosterically modifies QseC, impeding virulence in several Gram-negative pathogens.[1] LED209 is QseC sensor kinase inhibitor , as a potential lead compound to combat infections with Legionella or Mycobacterium spp. [2] LED209 inhibits the binding of signals to QseC, preventing its autophosphorylation and consequently inhibiting QseC-mediated activation of virulence gene expression. LED209 inhibits EHEC virulence traits in vitro. LED209 markedly inhibits the virulence of several pathogens in animals. Inhibition of signaling offers a strategy for the development of broad-spectrum antimicrobial drugs. [3]
Methicillin is a narrow-spectrum β-lactam antibiotic, acts by inhibiting penicillin-binding proteins (PBPs). Methicillin is active against Staphylococcus aureus and Staphylococcus epidermidis that are resistant to other penicillins.Methicillin can be used for the research of skin infections, osteomyelitis, and endocarditis[1].
HIV-1 inhibitor-27 (compound 5) is a potent HIV-1 inhibitor with IC50s of 16 μM, 0.5 μM and 0.39 μM for HIV-1 YU2, NL4-3 and 89.6 strain, respectively. HIV-1 inhibitor-27 has low cytotoxicity with a CC50 of 128 μM in TZM-bl cells. HIV-1 inhibitor-27 can be used for researching AIDS[1].
p-Anisic acid-d4 is the deuterium labeled p-Anisic acid[1]. p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties[2].
Sulfathiazole Sodium is an organosulfur compound that has been used as a short-acting sulfa drug.Target: AntibacterialSulfathiazole (20 μg/L) starts to be degraded between day 31 and day 38 in one of the two batch reactors containing different wastewater matrices. Sulfathiazole is degraded at a substantially faster rate than sulfamethoxazole or sulfamethazine in the nitrification process (S3) [1]. Recovery from spiked manure slurry samples is 64% for Sulfathiazole at pH 9. Sulfathiazole has acidity constant of pKa of 7.1and retention times (tR) of 7.8. S/N values for Sulfathiazole are above 100 at the 1 mg/kg level [2]. Sulfathiazole sorption to inorganic sorbents exhibits pronounced pH dependence consistent with sorbate speciation and sorbent charge properties. Sulfathiazole cations are most important for sorption to clay minerals, followed by neutral species [3].
Trilobatin, a natural sweetener derived from Lithocarpus polystachyus Rehd[1], Trilobatin is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope[2]. Neuroprotective effects[1]. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells[3].
Antibacterial agent 108 (Compound 1h) is a potent antibacterial agent with a MIC of both 3 μM against MRSA and antibiotic resistance strains[1].
Pyrantel pamoate is a deworming agent in the treatment of hookworms (all species) and roundworms in domesticated animal; acts as a depolarizing neuromuscular blocking agent.
Bacampicillin hydrochloride is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
Methyl 3-hydroxy-4,5-dimethoxybenzoate is a gallic acid derivant isolated from myricaria Laxiflora. Methyl 3-hydroxy-4,5-dimethoxybenzoate shows obvious antimicrobial activities. Methyl 3-hydroxy-4,5-dimethoxybenzoate shows fairly active for oxidation resistance in the presence of H2O2[1].
ME1111 is an antifungal agent that is active against dermatophytes. ME1111 is an inhibitor of the succinate dehydrogenase of Trichophyton species. ME1111 has an excellent ability to penetrate human nails and is used for onychomycosis research[1][2].
Chlorhexidine is an antibacterial used as an antiseptic and for other applications.Target: AntibacterialChlorhexidine belongs to a group of medicines called antiseptic antibacterial agents. It is used to clean the skin after an injury, before surgery, or before an injection. Chlorhexidine is also used to clean the hands before a procedure. It works by killing or preventing the growth of bacteria on the skin.
HHV-2 Envelope Glycoprotein G (552-574) is an immunodominant region of glycoprotein G (gG-2) reactive with all herpes simplex (HSV-2) sera[1].
Pafuramidine (DB289) is an orally bioavailable prodrug of furamidine, which has clinical activity against Pneumocystis pneumonia.IC50 Value: 4.5 nM (In vitro inhibitory activity against Trypanosoma brucei rhodesiense) [4]Target: AntiparasiticDB289 (pafuramidine maleate; 2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) is a prodrug of DB75 (furamidine dihydrochloride; 2,5-bis(4-guanylphenyl)furan dihydrochloride), an aromatic dication related to pentamidine that has demonstrated good efficacy against African trypanosomiasis, Pneumocystis carinii pneumonia, and malaria, but lacks adequate oral availability. in vitro: The results of this investigation suggest that DB75 inhibits mitochondrial function. Yeast cells relying upon mitochondrial metabolism for energy production are especially sensitive to DB75 [1].in vivo: Clearance of DB289 approximated the liver plasma flow and its large volume of distribution was consistent with extensive tissue binding. Plasma protein binding of DB289 was 97 to 99% in four animal species and humans, but that of DB75 was noticeably less and more species- and concentration-dependent [2]. Despite excellent oral activity against early-stage sleeping sickness, oral administration of DB289 exhibited limited efficacy in mouse models of late-stage disease [3].Clinical trial: DB289, a novel orally active prodrug of DB75, is undergoing phase IIb clinical trials for early-stage human African trypanosomiasis, Pneumocystis jiroveci carinii pneumonia, and malaria [1].
Irloxacin (Pirfloxacin) is a quinolone antibacterial agent. Irloxacin shows greater activity with an acid pH. Irloxacin has a good in vitro antimicrobial spectrum against both gram-positive and gram-negative bacteria. Orally active[1].
Sulbactam(Betamaze) is an irreversible β-lactamase inhibitor.Target: β-lactamase; AntibacterialSulbactam is a mechanism-based inhibitor of beta-lactamase enzymes used in clinical practice. sulbactam was the antimicrobial agent responsible for the killing of these organisms [1]. sulbactam may prove effective for non-life-threatening A. baumannii infections. Its role in the treatment of severe infections is unknown. However, the current formulation of sulbactam alone may allow its use at higher doses and provide new potential synergic combinations, particularly for those infections by A. baumannii resistant to imipenem [2].
2-Benzoxazolinone is an anti-leishmanial agent with an LC50 of 40 μg/mL against L. donovani[1]. A building block in chemical synthesis. 1,3-Benzoxazol-2(3H)-one derivatives have antimicrobial activity against a selection of Gram-positive, Gram-negative bacteria and yeasts[3]. Derivatives as anti-quorum sensing agent[4].
Cyclo(L-Trp-L-Trp) is an antibiotic, and shows antimicrobial activity. Cyclo(L-Trp-L-Trp) can inhibit A. baumannii, as well as Candida albicans, Bacillus subtilis, Micrococcus luteus, Saccharomyces cerevisiae, Aspergillus niger, Staphylococcus aureus. Cyclo(L-Trp-L-Trp) can be used in microbial infection research[1].
Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity[1][2][3][4].
HIV-1 inhibitor-57 (Compound 12g) is a HIV inhibitor. HIV-1 inhibitor-57 is active against wild-type and five prevalent NNRTI-resistant HIV-1 strains with EC50 values ranging from 0.024 to 0.0010 μM. HIV-1 inhibitor-57 forms additional interactions with residues around the binding site in HIV-1 RT[1].
Lindenenol is isolated from Radix linderae, with antioxidant and antibacterial activities[1].