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].
Palvanil is a capsaicin analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects[1][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].
Brevinin-1 is an antimicrobial peptide derived from the skin secretions of Rana esculenta[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].
D-(+)-Melezitose can be used to identify clinical isolates of indole-positive and indole-negative Klebsiella spp.
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].
H-Pro-Glu-OH is a protein secreted by pathogenic mycobacteria through the Type VII secretion system. H-Pro-Glu-OH targets LipY lipases to the cell Surface via the ESX-5 Pathway[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].
Bis-propargyl-PEG2 is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-propargyl-PEG2 is used for the synthesis of demethylvancomycin dimers[1][2].
Epimagnolin A, a furfuran lignan, shows mild antiplasmodial activities (IC50=5.7 μg/mL) without noticeable toxicity on mammalian normal cells[1].
Enduracidin is a polypeptide antibiotic produced by Streptomyces fungicides[1].
5,7-Dihydroxycoumarin is a coumarin isolated from the inflorescences of Macaranga triloba. 5,7-Dihydroxycoumarin has antibacterial activities[1][2].
Fumigaclavine A, a clavine alkaloid, is a Mycotoxin produced by Aspergillus fumigatus. A. fumigatus can be isolated from contaminating moldy silage[1].
NHC-triphosphate is an intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form. NHC-triphosphate is a weak alternative substrate for the viral polymerase and changes the mobility of the product in polyacrylamide electrophoresis gels[1].
Tropodithietic acid is a sulfur-containing antibiotic produced by the marine bacterium Phaeobacter inhibens. Tropodithietic acid exhibits a strong antibiotic activity against a broad spectrum of bacteria including alpha- and gammaproteobacteria, flavobacteria and actinobacteria[1].