Itraconazole-d5 (R51211-d5) is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects[1][2][3].
Mezlocillin (BAY-f 1353) is a β-lactam antibiotic, a semisynthetic and extended-spectrum antibiotic. Mezlocillin is active against both gram-negative and gram-positive bacteria. Mezlocillin can be used in bacterial infection research[1][2].
Isobonducellin is a flavonoid product and shows antimicrobial activity[1].
ML406 is a small molecule probe that shows anti-tubercular activity via MtbbioA (DAPA synthase) enzyme inhibition with an IC50 of 30 nM[1].
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection treatment[1][2][3][4].
Nifursemizone is an antiprotozoal drug.
SARS-CoV-2 3CLpro-IN-16 (Compound 3a) is a covalent SARS-CoV-2 3CLpro inhibitor (IC50s: 2.124 μM). SARS-CoV-2 3CLpro-IN-16 binds to the active site and forms a covalent bond with Cys145 of 3CLpro[1].
Saphenamycin is an antibiotic from a strain of Streptomyces.
Fosetyl-aluminum (Fosetyl-Al) is an active ingredient in many fungicides against downy mildew. Fosetyl-aluminum is used to control many diseases caused by Phytophthora spp. on agricultural and horticultural crops[1][2].
Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.Target: AntibacterialGatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Gatifloxacin had activity equal to that of tosufloxacin and activity more potent than those of norfloxacin, ofloxacin, ciprofloxacin, and sparfloxacin against the second-step mutants (grlA gyrA; gatifloxacin MIC range, 1.56 to 3.13 microg/ml) and had the most potent activity against the third-step mutants (grlA gyrA grlA; gatifloxacin MIC range, 1.56 to 6.25 microg/ml), suggesting that gatifloxacin possesses the most potent inhibitory activity against singly mutated topo IV and singly mutated DNA gyrase among the quinolones tested [1].Ophthalmic gatifloxacin 0.3% is at least as effective as ciprofloxacin at healing corneal ulcers infected with Pseudomonas aeruginosa when gatifloxacin is administered less frequently than ciprofloxacin. Trends favored gatifloxacin in fluorescein retention scores [2].Clinical indications: Bacterial infection FDA Approved Date: Toxicity: Hepatotoxicity; Acute pancreatitis [3]; Torsades de pointes [4]
Antibacterial agent 134 (compound 1) is an diketopiperazine alkaloid with antimicrobial activity. Antibacterial agent 134 is the major metabolite in the culture of Hymeniacidon perleve associated bioactive bacterium Pseudomonas sp. NJ6-3-1[1].
D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the KD values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively[1]. D13-9001 exhibits antibiotic activities[2].
Dolutegravir sodium is an inhibitor of HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM.
Sulfaclozine is an efficacious sulphonamide derivative with antibacterial and anticoccidial effects.Target: Antibacterial, AntiparasiticSulfaclozine is an antibiotic commonly used in poultry for the treatment of coccidiosis and various infectious diseases, in broiler chickens. Sulfaclozine is commonly used for the treatment of various poultry diseases (particularly, collibacteriosis, fowl cholera and coccidiosis).
Carindacillin (Carbenicillin indanyl) sodium is an orally active and broad-spectrum antimicrobial agent. Carindacillin sodium can be hydrolyzed to Carbenicillin in vivo. Carindacillin sodium can be used for the research of urinary-tract infection[1][2].
(+)-Epieudesmin is an antineoplastic agent. (+)-Epieudesmin has marginal cancer cell line inhibitory activities. (+)-Epieudesmin inhibits the growth of Gram-negative pathogen[1].
Tellimagrandin II (Eugeniin), the first intermediate in the 4C1-glucose derived series of ellagitannins, also inhibits antibiotic resistance of drug-resistant Staphylococcus aureus[1][2].
Verrucarin J (Muconomycin B) is a metabolite of the Myrothecium fungus family. Verrucarin J generates reactive oxygen species (ROS) and induces apoptosis of cancer cell lines, such as A549, HCT 116 and SW-620 cells. Verrucarin J shows activities against Candida albicans and Mucor miehei. Verrucarin J inhibits arenavirus Junin (JUNV) yield with an IC50 of 1.2 ng/mL[1][2][3][4][5].
Cys-TAT(47-57) (Cys-[HIV-Tat (47-57)]) is an arginine rich cell penetrating peptide derived from the HIV-1 transactivating protein.
Ferbam (Iron(III) dimethyldithiocarbamate) is a potent fungicide[1].
Erythromycin lactobionate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin lactobionate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin lactobionate also exhibits antitumor and neuroprotective effect in different fields of research[3][4].
Furaltadone-d8 (Altafur-d8) is the deuterium labeled Furaltadone. Furaltadone, a nitrofuran drug, has the potential for the study in infections of chickens with salmonella enteritidis. Furaltadone is inhibitory and bactericidal in vitro for staphylococci [1][2].
Arjunglucoside I, a natural compound, possesses antimicrobial activity with a MIC of 1.9 μg/mL[1].
Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.
Antibiotic tan-592B is an antibiotic agent.
Filipin, produced as a mixture of related compounds known as the filipin complex (filipins I-IV) in nature[1], is a 28-membered ring pentaene macrolide antifungal antibiotic produced by S. filipinensis, S. avermitilis and S. miharaensis. Filipin interacts with membrane sterols causing the alteration of membrane structure. Filipin III is the major component of Filipin[2].
Corianin is a sesquiterpene lactone that can be isolated from the fruits of Coriaria ruscifolia. Corianin shows antibacterial activity against S. aureus and S. epidermis[1].
Ga(III)protoporphyrin-IX is a model for the key interporphyrin interactions in malaria pigment. Ga(III)protoporphyrin-IX acts as a potent antibacterial against gram-negative, gram-positive, and acid-fast bacteria. Ga(III)protoporphyrin-IX is readily soluble in methanol (MeOH). Ga(III)protoporphyrin IX are as malarial pigment analogues for drug development and as potential antibacterial agents[1].
SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a potent inhibitor of SARS-CoV-2 3CLpro. 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. SARS-CoV-2 3CLpro-IN-1 has the potential for the research of infection diseases[1].
UCM53, a FtsZ inhibitor, is an antibacterial agent. UCM53 can inhibit the growth of clinical isolates of antibiotic-resistant Staphylococcus aureus and Enterococcus faecalis[1]