Cadazolid (ACT-179811) is a new oxazolidinone antibiotic with potent activity against Clostridium difficile.
Tosufloxacin (tosylate hydrate) is a fluoroquinolone antibacterial agent. Tosufloxacin (tosylate hydrate) is effective against Gram-positive and Gram-negative aerobic bacteria, anaerobic bacteria and Chlamydia trachomatis. Tosufloxacin (tosylate hydrate) is also a bacterial Topo (DNA gyrase, topoisomerase)) inhibitor.
Ethylparaben is the ethyl ester of p-hydroxybenzoic acid, used as an antifungal preservative. and food additive
Sulbactam pivoxil is a prodrug of sulbactam. Sulbactam is a β-lactamase inhibitor which poorly adsorbed from gastrointestinal tract. Sulbactam pivoxil has a better absorption than the parent drug and provides high serum levels after oral administration[1].
Acetohydroxamic acid is a potent and irreversible inhibitor of bacterial and plant urease and also used as adjunctive therapy in chronic urinary infection.Target: UreaseAcetohydroxamic acid selectively inhibits arachidonate 5-lipoxygenase and thus has potential use in the treatment of asthma.
Octacosane-d58 is the deuterium labeled Octacosane[1]. Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l[2][3][4].
GSK3532795 (BMS-955176) is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively[1].
Sulfamonomethoxine D4 is a deuterium labeled Sulfamonomethoxine. Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate[1].
Lauric acid-d2 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
HIV-1 inhibitor-36 (Compound 2) is a potent HIV-1. HIV-1 inhibitor-36 has the potential for further development as novel latency reversing agents[1].
SARS-CoV-2 nsp13-IN-6 (compound C5) is a potent SARS-CoV-2 non-structural protein 13 (nsp13) inhibitor with IC50 values of 27 and 33 μM for ssDNA+ ATPase and ssDNA- ATPase. SARS-CoV-2 nsp13-IN-6 can be used for researching anti-COVID-19[1].
Artemisinin is an anti-malarial drug isolated from the aerial parts of Artemisia annua L. plants.
Cycloguanil, the active metabolite of Proguanil, acts on malaria schizonts in erythrocytes and hepatocytes[1].
Isopicropodophyllone, a natural compound that can be isolated from leaves of Podophyllum hexandrum, possesses antifungal activity[1].
LPRP-Et-97543 is a potent anti-HBV agent. LPRP-Et-97543 reduces Core, S, and preS but not X promoter activities. LPRP-Et-97543 can be used for acute and chronic HBV infections research[1].
Hetacillin is a beta-lactam antibiotic that is part of the aminopenicillin family. It is a prodrug and it has no antibacterial activity itself, but quickly splits of acetone in the human body to form ampicillin, which is active against a variety of bacteria.
Hypoglaunine D is an analogue of Triptonine B and acts as an anti-HIV compound. Hypoglaunine D inhibits HIV replication in H9 lymphocytes with an EC50 value of 22 μg/ml[1].
R803 is an effective HCV replication inhibitor. R803 is substantially more potent against genotype 1a and 1b replicons (EC50, ~30 nM) than against the genotype 2a replicon (EC50, ~1,000 nM).
CPFX2090 is a cephalosporin antibacterial compound extracted from patent WO2013052568A1, Compound Example 16g[1].
Tetracycline hydrochloride is a broad-spectrum antibiotic used to treat a wide range of infections.
Spiroxamine is a fungicide that can be used to kill grapes with less residue[1].
Dicloxacillin sodium is a narrow-spectrum β-lactam antibiotic of the penicillin family. Dicloxacillin sodium is active against β-lactamase-producing organisms such as Staphylococcus aureus[1].
MUT056399 is a highly potent inhibitor of the FabI enzyme of both S. aureus and E. coli with 50% inhibitory concentration IC50s of 12 nM and 58 nM, respectively. IC50 value: 12 nM (for S. aureus), 58 nM (for E. coli) [1]Target: FabI enzymein vitro: MUT056399 is a highly potent new inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli. MUT056399 is very active against S. aureus strains, including methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), linezolid-resistant, and multidrug-resistant strains, with MIC90s between 0.03 and 0.12 μg/ml. MUT056399 is also active against coagulase-negative staphylococci, with MIC90s between 0.12 and 4 μg/ml. MUT056399 is very active against the 118 S. aureus strains tested, including MSSA and MRSA isolates and linezolid-resistant and multidrug-resistant strains, with MIC90s between ≤0.03 and 0.12 μg/ml.In vivo: MUT056399, administered subcutaneously, protected mice from a lethal systemic infection induced by MSSA, MRSA, and vancomycin-intermediate S. aureus strains (50% effective doses ranging from 19.3 mg/kg/day to 49.6 mg/kg/day). In the nonneutropenic murine thigh infection model, the same treatment with MUT056399 reduced the bacterial multiplication of MSSA and MRSA in the thighs of immunocompetent mice.
Puromycin dihydrochloride is the dihydrochloride salt of puromycin. Puromycin is an aminoglycoside antibiotic that inhibits protein synthesis.
Indinavir(MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.Target: HIV ProteaseIndinavir(MK-639) is a protease inhibitor used as a component of highly active antiretroviral therapy (HAART) to treat HIV infection and AIDS.MK-639 appears to have significant dose-related antiviral activity and is well tolerated [1]. Inhibition constants (K(i)) of the antiviral drug indinavir for the reaction catalyzed by the mutant enzymes were about threefold and 50-fold higher for PR(L24I) and PR(I50V), respectively, relative to PR and PR(G73S). The dimer dissociation constant (K(d)) was estimated to be approximately 20 nM for both PR(L24I) and PR(I50V), and below 5 nM for PR(G73S) and PR. Crystal structures of the mutants PR(L24I), PR(I50V) and PR(G73S) were determined in complexes with indinavir, or the p2/NC substrate analog at resolutions of 1.10-1.50 Angstrom [2].
QStatin is a novel, potent, and selective Vibrio quorum sensing (QS) inhibitor, shows pan-QS inhibitor activity in diverse Vibrio species. QStatin attenuates representative QS-regulated phenotypes in various Vibrio speciesbinds tightly to a putative ligand-binding pocket in SmcR and changes the flexibility of the protein, thereby altering its transcription regulatory activity. QStatin may be a sustainable antivibriosis agent useful in aquacultures[1].
Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest[1][2][3].
Psoracorylifol C is a natural product. Psoracorylifol C has important activity against Helicobacter pylori. Psoracorylifol C can be isolated from the seeds of Psoralea corylifolia[1].