Gomisin M2 ((+)-Gomisin M2) is a lignan isolated from the fruits of Schisandra rubriflora with anti-HIV activity (EC50 of 2.4 μM). Gomisin M2 exhibits anti-cancer and anti-allergic activities and has the potential for Alzheimer’s disease research[1][2].
5,7,2 ',6 '-Tetrahydroxyflavanone is an extract isolated from Scutellaria baicalensis. 5,7,2 ',6 '-Tetrahydroxyflavanone has significant antibacterial activity against gram-positive bacteria. 5,7,2 ',6 '-Tetrahydroxyflavanone can be used to study the treatment of inflammatory diseases [1].
Meropenem is a carbapenem antibiotic, which displaying a broad spectrum of antibacterial activity.Target: AntibacterialMeropenem, a new parenteral carbapenem demonstrated increased activity as compared to imipenem against 336 strains of Neisseria gonorrhoeae, 119 strains of Haemophilus influenzae, and 110 strains of H. Ceftriaxone and ciprofloxacin demonstrated activity superior to that of both carbapenems while the activity of ceftazidime was similar to that of meropenem [1]. Meropenem, like imipenem and various experimental penems, may overcome the resistance problems presented by Class I beta-lactamases [2]. MEROPENEM was rapidly penetrated to the pleural effusion and was retained for a more prolonged time in the pleural effusion than in the blood of patients with accumulated pleural effusion, and it suggested the usefulness of MEROPENEM in antibacterial therapy for patients with pleurisy causing accumulation of pleural effusion [3].Clinical indications: Appendicitis; Bacterial infection; Bacterial meningitis; Bacterial pneumonia; Bacterial respiratory tract infection; Bacterial skin infection; Bacterial urinary tract infection; Bacteroides fragilis infection; Bacteroides infection; Bacteroides thetaiotaomicron infection; Complicated skin and skin structure infectionFDA Approved Date: July 1996Toxicity: In mice and rats, large intravenous doses of meropenem (2200-4000 mg/kg) have been associated with ataxia, dyspnea, convulsions, and mortalities.
Thymol iodide is a compound of Iodide and Thymol. Thymol iodide acts as a substitute for iodoform[1]. Thymol iodide is an iodine derivative of Thymol (a phenol derived from thyme oil), which is mostly used as mild antiseptic and fungicide[2].
Variotin is an Anti-Fungal Agent. Variotin has a strong antibiotic activity on dermatophytes such as Trichophyton, Microsporum, and Epidermophyton, and also pathogenic fungi in internal mycosis such as Blastomyces and Cryptococcus[1].
Pseudoaspidin is isolated from the ferns of the class Pterophyta or Filicinae[1].
5-Nitrobarbituric acid is a herpes simplex virus type-1 (HSV-1) inhibitor (IC50=1.7 μM)[1].
Nanchangmycin, produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria. Nanchangmycin is a broad spectrum antiviral active against Zika virus.
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity[1][2].
Peptide 5g is an antimicrobial peptide. Peptide 5g inhibits E. coli, S. aureus, and C. albicans with MIC values of 30, 10, 12.5 μg/mL respectively[1].
Inz-1 is a potent and selective mitochondrial cytochrome bc1 inhibitor for yeast (IC50=8.092 μM) over humans (IC50=45.320 μM). Inz-1 reverses Fluconazole (HY-B0101) or other triazole antifungals’ resistance in the pathogenic fungus Candida albicans[1].
4 '-DTMP is a DHFR inhibitor with Ki of 5.1 nM (DHFRWT) and 34.3 nM (DHFRL28R), respectively. 4 '-DTMP carries a polar modification that induces additional local interactions with the enzyme. In particular, the hairpin structure on the M20 ring is related to the internal communication of the DHFR. 4 '-DTMP has potential inhibition of E.coli[1].
Tebuconazole is an agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively.
Pepstatin (Pepstatin A) acetate is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin acetate also inhibits HIV protease[1][2].
Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects[1][2][3].
Metallo-β-lactamase-IN-4 (compound 40) is a potent metallo-β-lactamases (MBL) inhibitor, with IC50 values of 0.1 μM (VIM-1), 1.3 μM (NDM-1), and 5.0 μM (IMP-7), respectively[1].
Polistes mastoparan is an antimicrobial peptide. Polistes mastoparan increases S. aureus cell K+ efflux and inhibits cell viability with EC50 of 5 μM[1].
Clindamycin is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla)[1].
Eritoran is a Toll-like receptor 4 (TLR4) antagonist. Eritoran protects mice against lethal influenza virus infection, such as Ebola virus (EBOV), Marburg virus (MARV). Eritoran decreases the level of granulocytosis, may alleviate the severity of the "cytokine storm". Eritoran inhibits pathogenesis of filovirus infection[1].
Esculentoside B (Phytolaccoside B) is a natural product from the roots of Phytolacca acinosa Roxb. Esculentoside B is neurotoxic to zebrafish larvae, and impairs their central nervous system development. Esculentoside B inhibits inflammatory response and has antifungal activity[1][2][3].
SARS-CoV-2 Mpro-IN-2 (compound GC-14) is a selective, low cytotoxic and non-covalent Mpro inhibitor (IC50=0.40 μM) with good anti-SARS-CoV-2 activity (EC50=1.1 μM). SARS-CoV-2 Mpro-IN-2 can be used in COVID-19 studies[1].
Isorhamnetin 7-O-α-L-rhamnoside shows binding affinity with COVID-19 virus main protease[1].
Sulfisoxazole (Sulfafurazole) diethanolamine is an endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A[1][2].
Niclosamide monohydrate is an inhibitor of STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
Antifungal agent 15 has the most potent activity with EC50 values of 0.52 and 0.50 μg/mL against S. sclerotiorum and B. cinerea, respectively.
Dehydrocavidine, a main active ingredient of Corydalis saxicola Bunting (Yanhuanglian), displays antinociceptive, hepatoprotective, and spasmolytic activities. Dehydrocavidine kills hepatitis viruses and promotes regeneration of hepatocytes[1].
SARS-CoV MPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 Mpro with an IC50 value of 72.07 nM. The main protease (Mpro) of the virus as the major enzyme processing viral polyproteins contributes to the replication and transcription of SARS-CoV-2 in host cells, and has been characterized as an attractive target in drug discovery. SARS-CoV MPro-IN-2 has the potential for the research of COVID-19[1].
Chloramphenicol is a broad-spectrum antibiotic.Target: AntibacterialChloramphenicol is a bacteriostatic drug that stops bacterial growth by inhibiting protein synthesis. Chloramphenicol prevents protein chain elongation by inhibiting the peptidyl transferase activity of the bacterial ribosome. It specifically binds to A2451 and A2452 residues in the 23S rRNA of the 50S ribosomal subunit, preventing peptide bond formation. While chloramphenicol and the macrolide class of antibiotics both interact with ribosomes, chloramphenicol is not a macrolide. It directly interferes with substrate binding, whereas macrolides sterically block the progression of the growing peptide [1, 2].
Cetalkonium chloride is an ammonium antiseptic agent used in many topical drugs for infections of mouth, throat and eye. Cetalkonium chloride acts as anti-inflammatory amphiphilic agent[1].
FNC-TP is the intracellular active form of FNC. FNC is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV[1].