Glicophenone is an antibacterial agent with MICs of both 32 μg/mL against MRSA OM481, MRSA OM505, MRSA OM584, MRSA OM623 and MSSA 209P[1].
Ceftibuten dihydrate is a third-generation cephalosporin antibiotic.
Tosufloxacin (A-61827) is an orally active fluoroquinolone antibiotic. Tosufloxacin shows a broad spectrum of antibacterial activity against gram-positive and gram-negative bacteria[1][2].
Lactoferrin is a substance released by neutrophils. Lactoferrin is an orally active multifunctional iron binding glycoprotein. Lactoferrin prevents cell adhesion, growth and spreading of cell colonies. Lactoferrin also has antiviral activity and inhibits microbial and viral adhesion and entry into host cells. Besides, Lactoferrin has anti-inflammatory, immunomodulatory, and anti-cancer activities[1][2][3].
Urechistachykinin I (Uru-TK I), an invertebrate tachykinin-related peptides (TRPs) isolated from echiuroid worms, shows antimicrobial activities without a hemolytic effect[1][2].
Norfloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.Target: DNA gyrase; AntibacterialNorfloxacin is a synthetic chemotherapeutic antibacterial agent occasionally used to treat common as well as complicated urinary tract infections. Norfloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting DNA gyrase, a type II topoisomerase, and topoisomerase IV, enzymes necessary to separate bacterial DNA, thereby inhibiting cell division.There are currently three approved uses in the adult population (one of which is restricted) and the other ineffective due to bacterial resistance. Chibroxin (ophthalmic) is approved for use in children older than one year of age.Norfloxacin is associated with a number of rare serious adverse reactions as well as spontaneous tendon ruptures and irreversible peripheral neuropathy. Tendon problems may manifest long after therapy had been completed and in severe cases may result in lifelong disabilities. Hepatoxicity resulting in fatalities has also been reported with the use of norfloxacin.
Kadsuralignan A (compound 1) is a dibenzocyclooctadiene lignan isolated from the leaves and stems of Schisandra lancifolia. Kadsuralignan A has anti-HIV activity with EC50=2.23 μg/mL[1].
PXYC13 is a ribosomal protein S1 (RpsA) antagonist with Kds of 7.61 and 8.50 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb)[1].
Indolicidin is a potent antimicrobial peptide purified from the cytoplasmic granules of bovine neutrophils.
Cladosporin is a fungal metabolite produced in good yield in the mycelium of Cladosporium cladosporioid. Cladosporin completely inhibits growth of severa dermatophytes on agar medium at a concentration of 75 μg/mL[1].
Rilpivirine (R278474; TMC278) is a type of anti-HIV medicine called a non-nucleoside reverse transcriptase inhibitor (NNRTI).
Idoxuridine is an antiviral agent for feline herpesvirus type-1 with IC50 of 4.3 μM.Target: herpesvirus type-1Idoxuridine is mainly used topically to treat herpes simplex keratitis. Epithelial lesions, especially initial attacks presenting with a dendritic ulcer, are most responsive to therapy, while infection with stromal involvement are less responsive. Idoxuridine is ineffective against herpes simplex virus type 2 and varicella-zoster.
Dextrorotation nimorazole phosphate ester is an anti-anaerobic and anti-parasitic agent.Target: Antibacterial, AntiparasiticDextrorotary morpholine ornidazole organic phosphate is a newly developed, highly efficient, good tolerated, fourth-generation nitroimidazole derivative.
Nifuratel(NF 113, SAP 113) is a broad antibacterial spectrum agent, which is used as an antibacterial, antifungal, and antiprotozoal (Trichomonas).IC50 Value: 0.125-1 μg/mL(MIC, A. vaginae) [1]Target: Antibacterial; Antiprotozoal in vitro: In vitro, nifuratel is able to inhibit the growth of A. vaginae, with a MIC range of 0.125-1 μg/mL; it is active against G. vaginalis and does not affect lactobacilli [1].in vivo: Patients were randomized to receive a 2-week course of bismuth subcitrate (8 mg/kg/day, q.d.s.), amoxicillin (50 mg/kg/day, q.d.s.), with either nifuratel (15 mg/kg/day, q.d.s.) or furazolidone (10 mg/kg/day, q.d.s.), plus omeprazole (0.5 mg/kg, once daily) [2].Toxicity: There were no serious adverse reactions and were no withdrawals due to any side-effects. All of side-effects were self-limiting (dark stools, urine discoloration, blackening of the tongue, and others) [3].Clinical trial: N/A
Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor.Target: Antibacterial; CYP3A4Clarithromycin is a macrolide antibiotic used to treat pharyngitis, tonsillitis, acute maxillary sinusitis, acute bacterial exacerbation of chronic bronchitis, pneumonia (especially atypical pneumonias associated with Chlamydophila pneumoniae), skin and skin structure infections. Clarithromycin prevents bacteria from growing by interfering with their protein synthesis. It binds to the subunit 50S of the bacterial ribosome and thus inhibits the translation of peptides. Clarithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain Gram-negative bacteria, particularly Legionella pneumophila. Besides this bacteriostatic effect, clarithromycin also has bactericidal effect on certain strains, such as Haemophilus influenzae, Streptococcus pneumoniae and Neisseria gonorrhoeae. Clarithromycin is a CYP3A4 inhibitor. Even low doses of the cytochrome P4503A4 (CYP3A4) inhibitor clarithromycin increase the plasma concentrations and effects of repaglinide. Concomitant use of clarithromycin or other potent inhibitors of CYP3A4 with repaglinide may enhance its blood glucose-lowering effect and increase the risk of hypoglycemia [1, 2].
Propamocarb-d7 is the deuterium labeled Propamocarb[1]. Propamocarb is a systemic fungicide. Propamocarb is widely used to protect cucumbers, tomatoes and other plants from pathogens[2].
Amantadine (1-Adamantanamine) is an antiviral agent with activity against influenza A viruses. Amantadine blocks the proton flow through the M2 ion channel (M2 proton channel of influenza A) and thus prevents the release of viral RNA into the cytoplasm of the infected cells. Amantadine is an antiparkinsonian agent[1][2].
Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats[1][2].
(Rac)-Moxifloxacin ((Rac)-BAY 12-8039 free base) is the isoform of Moxifloxacin Hydrochloride (HY-66011), which is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia[1][2].
D1N8 is a potent SARS-CoV-2 3CLpro inhibitor with an IC50 and CC50 values of 0.44 μM and >20 μM, respectively. D1N8 has the potential for the research of anti-SARS-CoV-2 agents targeting 3CLpro[1].
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 Mpro inhibitor with an IC50 of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3[1].
Influenza virus-IN-5 (Compound 5f) is an inhibitor of influenza virus hemagglutinin (HA) with an EC50 of 1 nM against influenza A/H3N2 virus[1].
Flubendazole is a potent broad spectrum anthelmintic.Target: AntiparasiticFlubendazole is an anthelmintic. It is also available for human use to treat worm infections[1].
Nourseothricin sulfate (Streptothricin sulfate) is a broad-spectrum antibiotic that destroys the outer membrane of Gram-negative bacteria and is a dominant selective marker for Fonsecaea pedrosoi[1][2]. Nourseothricin sulfate inhibits protein biosynthesis in prokaryotic cells and strongly inhibits the growth of eukaryotes like fungi and can also be used as a elective marker for a wide range of organisms including bacteria, yeast, filamentous fungi, and plant cells[3].
Antibacterial agent 44 is an antibacterial agent extracted from patent WO2013030735A1, example 7. Antibacterial agent 44 can be used for the research of bacterial infections[1].
Delafloxacin (RX-3341, ABT-492) 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: N/A
As-358 has inhibitory effects against Ebola virus and Marburg virus, with IC50s of 47.5 μM and 3.7 μM[1].
Antiviral agent 19 (Compound 3) is a selective inhibitor against Zika virus infection with an EC50 of 1.3 µM. Antiviral agent 19 has low cytotoxicity[1].
Influenza virus-IN-1 (compound 14) is a potent influenza A virus inhibitor with an EC50 of 2.46 µM and CC50 of >200 µM. Influenza virus-IN-1 shows a concentration dependent inhibition activity for PAN endonuclease with EC50 of 312.36 nM. Influenza virus-IN-1 shows shows anti-influenza A virus activities[1].
SARS-CoV-2-IN-18 (Compound 26) is a potent SARS-CoV-2 3C-like protease inhibitor with an IC50 of 45 nM[1].