Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
Kanzonol C, a flavonoid isolated from the twigs of Dorstenia barteri (Moraceae), has potential to treat bacterial and fungal infections[1].
Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties.Target: Glucocorticoid ReceptorMethylprednisolone is typically used for its anti-inflammatory effects. Common uses include arthritis therapy and short-term treatment of bronchial inflammation or acute bronchitis due to various respiratory diseases. Methylprednisolone is used both in the treatment of acute periods and long-term management of autoimmune diseases, most notably systemic lupus erythematosus. It is also used for vestibular neuritis [1].After six months the patients who were treated with methylprednisolone within eight hours of their injury had significant improvement as compared with those given placebo in motor function (neurologic change scores of 16.0 and 11.2, respectively; P = 0.03) and sensation to pinprick (change scores of 11.4 and 6.6; P = 0.02) and touch (change scores, 8.9 and 4.3; P = 0.03). Benefit from methylprednisolone was seen in patients whose injuries were initially evaluated as neurologically complete, as well as in those believed to have incomplete lesions [2].
Deapioplatycodin D is a triterpenoid saponin isolated from Platycodon grandiflorum, with anti-HCV activity[1].
Valganciclovir-d8 (hydrochloride) is the deuterium labeled Valganciclovir hydrochloride[1]. Valganciclovir hydrochloride, the L-valyl ester of ganciclovir, is actually a prodrug for ganciclovir[2][3][4].
Amphotericin X1 is an 13-O-methyl derivative of Amphotericin B with good antifungal activity. Amphotericin X1 inhibits Candida albicans 33/079, C.parapsilosis 937A, Cryptococcus neoformans 451, Aspergillus niger 57A and A.fumigatus with MIC values of 1 μg/mL, 8 μg/mL, 1 μg/mL, 2 μg/mL and 2 μg/mL, respectively[1].
Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.Target: beta-lactamaseImipenem with Relebactam is active against Escherichia coli, Klebsiella pneumoniae, and Enterobacter spp., including K. pneumoniae carbapenemase (KPC)-producing isolates. The combination of Imipenem with Relebactam demonstrated activity against KPC-producing Enterobacteriaceae and multidrug-resistant P. aeruginosa. The imipenem MIC50 and MIC90 values for the ESBL-producing isolates were 0.25 and 0.5 μg/ml, respectively; with the addition of Relebactam, the corresponding values were 0.25 and 0.25 μg/ml. Five isolates harbored blaKPC. For these 5 isolates, the imipenem MICs ranged from 0.5 to >32 μg/ml. With the addition of Relebactam, the MICs decreased to 0.12 to 0.5 μg/ml.[1] Relebactam inhibits most class A and class C β-lactamases, with selected inhibition of class D enzymes by avibactam. β-Lactamase inhibitors (BLIs) have played an important role in combatting β-lactam resistance in Gram-negative bacteria, but their effectiveness has diminished with the evolution of diverse and deleterious varieties of β-lactamases.[2]
4,5-O-Dicaffeoyl quinic acid methyl ester (compound 4), a dicaffeoylquinic acid, has potent antiviral activity against respiratory syncytial virus (RSV) with an IC50 of 0.63 μg/mL and a CC50 of 118.68 μg/mL.
rCRAMP (rat) is the rat cathelin-related antimicrobial peptide. rCRAMP (rat) contributes to the antibacterial activity in rat brain peptide/protein extracts. rCRAMP (rat) is a potential key player in the innate immune system of rat CNS[1][2].
Ophiobolin C inhibits CCR5 binding to the envelop protein gp120 and CD4, which is responsible for mediating the entry of HIV-1 into cells[1]. Ophiobolin C is also cytotoxic to chronic lymphocytic leukemia cells[2].
Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM.
5-[(2-Nitrophenyl)methylene]-2,4-thiazolidinedione (Compound 4) has antimicrobial, anti-diabetic and antioxidant activities. 5-[(2-Nitrophenyl)methylene]-2,4-thiazolidinedione inhibits B. subtilis, S. aureus, K. pneumonia, E. coli, and S. typhi with MICs of 4.5-9.9 μΜ/mL, and inhibits A. niger and C. albicans with MICs of 4.99 μΜ/mL[1].
Levofloxacin hydrate is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.Target: AntibacterialLevofloxacin reduced bacterial load compared with placebo by 4.9-fold (95% confidence interval, 1.4-25.7; P=0.02) at day 7 but had no effect at any point on any marker of neutrophilic airway inflammation. In patients with a baseline bacterial load of more than 10(6) cfu/mL, levofloxacin treatment was associated with a 26.5% (95% confidence interval, 1.8%-51.3%; P=0.04) greater reduction in the percentage neutrophil count compared with placebo at day 7 [1]. Levofloxacin was found to significantly improve the clinical and microbiological parameters in CP individuals [2]. A 30-day course of levofloxacin does not significantly improve BK viral load reduction or allograft function when used in addition to overall reduction of immunosuppression [3].
Lauric acid-13C-1 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively[1].
Lysostaphin is an antistaphylococcal agent. Lysostaphin has activities of three enzymes namely, glycylglycine endopeptidase, endo-β-N-acetyl glucosamidase and N-acteyl muramyl-L-alanine amidase[1].
Nerolidol is a natural membrane-active sesquiterpene, with antitumor, antibacterial, antifungal and antiparasitic activity[1].
Rolusafine is an antifungal agent[1].
LHVS is a potent, non-selective cysteine protease inhibitor[1]. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion[2].
Phaseollidin is an antifungal agent that can be isolated from Phaseolus vulgaris L.[1].
Clindamycin phosphate (Clindamycin 2-phosphate) hydrochloride is a broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin phosphate hydrochloride is the prodrug of Clindamycin (HY-B1455) with no antimicrobial activity in vitro but can be rapidly converted in vivo to the active parent drug, Clindamycin, by phosphatase ester hydrolysis. Clindamycin phosphate hydrochloride can be used for researching acne and bacterial vaginosis[1][2][3].
Helioxanthin (ACH126447) and its analogues exhibit significant in vitro antiviral activity against hepatitis B virus (HBV, EC50=1 uM) and flavivirus.IC50 value: 1/3/2 uM (EC50, HBV/HCV/HSV-1) [1]Target: Anti-HBV; Anti flavivirusin vitro: Helioxanthin and its analogues decreased cellular RNA levels of HBV and antigen expression as well as selective inhibition of HBV replication in a cell culture model [2]. Helioxanthin analogue 8-1 exhibited anti-DHBV activity as demonstrated by quantification of viral DNA, RNA, covalently closed circular DNA and protein synthesis. Analogue 8-1 did not affect the stability of cellular macromolecules and did not have a sustained antiviral effect after drug removal. When DHBV replication was induced, virus-harbouring cells were more susceptible to the cytotoxicity of 8-1 than non-induced cells [3].
Trimethoprim sulfate is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim sulfate is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim sulfate has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim sulfate can inhibit infection of Influenza A virus in chick embryo when combinated with zinc[1][2][3][4].
Maximin 2 is an antimicrobial peptide derived from skin secretions of Bombina maxima. Maximin 2 has cytotoxicity on tumor cells and spermicidal effect[1].
Benurestat is an orally active urease inhibitor. Benurestat can be used for infected ureolysis research[1].
Iedaborbactam, as a beta-lactamase inhibitor (WO2015191907, Example 62), can be used for the research of bacterial infections[1].
INSCoV-601I(1) is a potent inhibitor of Mpro (3CLpro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-601I(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1)[1].
Firzacorvir is a cyclic sulfamide compound and modulates HBV core protein. Firzacorvir has anti-HBV activity with EC50 < 1 μΜ[1].
ADG-2e is a potent antibacterial agent with MICs of 16, 4, 2, and 2 μg/mL for E. coli [KCTC 1682], P. aeruginosa [KCTC 1637], B.subtilis [KCTC 3068], and S. aureus [KCTC 1621], respectively. ADG-2e shows anti-metastatic activity against breast cancer cells[1].
SARS-CoV-IN-4 (compound 13) is a potent and specific inhibitor of SARS-CoV nsp14 N7-methyltransferase, with an IC50 of 0.6 μM (SARS-CoV nsp14)[1].