Aureobasidin A (Basifungin), a cyclic depsipetide, is an antifungal antibiotic. Aureobasidin A (Basifungin) A is an inhibitor of the inositolphosphorylceramide synthase AUR1[1][2].
Aminoacyl tRNA synthetase-IN-1 is a bacterial aminoacyl tRNA synthetase (aaRS) inhibitor.
3-Fucosyllactose (3-Fucosyl-D-lactose) is one of the major fucosylated oligosaccharides found in human breast milk. 3-Fucosyllactose shows prebiotic, immunomodulator, neonatal brain development, and antimicrobial function[1].
Anti-MRSA agent 2 (compound 14) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and relatively low cytotoxicity in normal cells. Anti-MRSA agent 2 has strong ability to destroy bacterial membrane and bind to genomic DNA[1].
Clovamide (trans-Clovamide), a natural phenolic compound, is a potent antioxidant. Clovamide is an excellent ROS and oxygen radical scavenger. Clovamide also has anti-inflammatory and neuroprotective effects[1][2]. Clovamide is an anti-microbial with activity against the human pathogens influenza A subtype H5N1, Trypanosoma evansi, and Heliobacter pylori[3].
Walrycin B is a novel antibacterial compound specifically targeting the essential WalR response regulator.IC50 value: 0.39 ug/ml (MIC for B. subtilis 168); 3.13 ug/ml (MIC for S. aureus N315) [1]Target: bacterial WalR response regulator; AntibacterialWalrycin B is known as an analog of toxoflavin (a phytotoxin from Burkholderia glumae), which has been shown to have a strong MIC for B. subtilis and S. aureus but whose mode of action is not clear. The compound could also interact with WalR to cause bactericidal effects. Walrycins are a new class of potent small molecule compounds that kill bacterial cells by targeting the RR WalR and inhibiting this essential signal transduction pathway. They not only have therapeutic potential but will also prove to be useful reagents for the further study of the WalK/WalR TCS. Walrycin B target WalR andlead to cell death in both B. subtilis and S. aureus.
[1-13Cglc]Lactose monohydrate is an isotopic labeling drug[1].
Solanesol is an aliphatic terpene alcohol mainly found in Solanaceous plants, with anti-inflammatory, neuroprotective, and antimicrobial activities[1].
Ticarcillin disodium is an injectable antibiotic for the treatment of Gram-negative bacteria, particularly Pseudomonas aeruginosa. It is also one of the few antibiotics capable of treating Stenotrophomonas maltophilia infections.
Aviptadil acetate is an analog vasoactive intestinal polypeptide (VIP) with potent vasodilatory effects. Aviptadil acetate induces pulmonary vasodilation and inhibits vascular SMCs proliferation, platelet aggregation. Aviptadil acetate can be used for the research of pulmonary fibrosis, pulmonary arterial hypertension (PAH) and SARS-CoV-2 caused respiratory failure, et al[1].
Fusafungine (Bioparox; Fusaloyos; Locabiotal) is a potent and orally active antibiotic and anti-inflammatory agent. Fusafungine has the potential for the research of upper respiratory airways disease (URAD)[1][2].
β-Lactamase-IN-4 is a β-lactamase inhibitor extracted from patent WO2013149121A1, compound 708. β-Lactamase-IN-4 can be used for the research of bacterial infections[1].
3β-Acetoxyurs-12-en-11-one is a ursane triterpenoid with antimicrobial activity, can be isolated from the stem bark of Morus mesozygia and the leaves of Ficus hirta Vahl (Moraceae)[1][2].
Pleurocidin is an antibacterial peptide derived from skin secretions of Winter Flounder[1].
Antitubercular agent-21 (Compound 15) is an antitubercular agent with an MIC of o.4 µg/mL against M. tuberculosis H37Rv. Antitubercular agent-21 exhibits lower activity against other microorganism such as bacteria gram-positive, gram-negative or fungi. Antitubercular agent-21 shows low cytotoxicity[1].
Ditiocarb sodium (Sodium diethyldithiocarbamate) is an accelerator of the rate of copper cementation. Sodium diethyldithiocarbamate reduces the incidence of HIV infection.
Flurofamide is a potent bacterial urease inhibitor with potential clinical utility in the treatment of infection induced urinary stones[1].
Flucytosine (5-Fluorocytosine, 5-FC, Ancobon), a fluorinated pyrimidine analogue, is an antifungal drug.Target: antifungalFlucytosine, or 5-fluorocytosine, a fluorinated pyrimidine analogue, is a synthetic antimycotic drug. It is structurally related to the cytostatic fluorouracil and to floxuridine. It is available in oral and in some countries also in injectable form. A common brand name is Ancobon. Flucytosine was first synthesized in 1957 but its antifungal properties were discovered in 1964. The drug is dispensed in capsules of 250 mg and 500 mg strength. The injectable form is diluted in 250 mL saline solution to contain 2.5 g total (10 mg/mL). The solution is physically incompatible with other drugs including amphotericin B.Flucytosine is well absorbed (75 to 90%) from the gastrointestinal tract. Intake with meals slows the absorption, but does not decrease the amount absorbed. Following an oral dose of 2 grams peak serum levels are reached after approximately 6 hours. The time to peak level decreases with continued therapy. After 4 days peak levels are measured after 2 hours. The drug is eliminated renally. In normal patients flucytosine has reportedly a half-life of 2.5 to 6 hours. In patients with impaired renal function higher serum levels are seen and the drug tends to cumulate in these patients. The drug is mainly excreted unchanged in the urine (90% of an oral dose) and only traces are metabolized and excreted in the feces. Therapeutic serum levels range from 25 to 100 ?g/ml. Serum levels in excess of 100 ug are associated with a higher incidence of side effects. Periodic measurements of serum levels are recommended for all patients and are a must in patients with renal damage.
TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea[1][2].
Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity.
Antifungal agent 69 (compound 13) is a eugenol-imidazole against Candida albicans (MIC: 4.6 μM) with no relevant cytotoxicity. Antifungal agent 69 alters the fungal ergosterol biosynthesis and shows antifungal activity[1].
Broxaldine is an antiprotozoal drug.
L 696229 is a specific inhibitor ofhuman immunodeficiency virus type 1 (HIV-1)reverse transcriptase (RT) activity that possesses antiviral activity[1].
3β,7β,15β-Trihydroxy-11-oxo-lanosta-8-en-24→20 lactone is a natural compound that could be isolated from G. lucidum with antimycobacterial activity.
Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities[1]. Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE[2]. Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters[3].
FtsZ-IN-1 is a potent FtsZ inhibitor with quinolinium ring. FtsZ-IN-1 has stronger antibacterial activity against Gram-positive bacteria with MICs of 0.5-8 μg/mL. FtsZ-IN-1 significantly causes cell elongation of B. subtilis by enhancing FtsZ polymerization. FtsZ-IN-1 exhibits low hemolytic toxicity and low tendency to induce drug resistance. FtsZ-IN-1 has against drug-resistant bacteria activity[1].
Defensin HNP 4 (HNP 4) is a single 11 amino acid long fragment of HNP-41-11. Defensin HNP 4 has inhibitory effect against multidrug-resistant and non-resistant strains[1].
Phenothiazine is an antibiotic which has insecticidal, fungicidal, antibacterial and anthelmintic activities. Phenothiazine also can be used for the research of neurological diseases[1][2].
(-)-Ketoconazole-d3 is deuterium labeled (-)-Ketoconazole. (-)-Ketoconazole ((-)-R 41400) is one of the enantiomer of Ketoconazole. Ketoconazole is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole).
Pentamidine isethionate is an antimicrobial agent for prevention and treatment of Pneumocystis pneumonia (PCP) caused by Pneumocystis jirovecii.