Glycolithocholic acid 3-sulfate (SLCG) is a cholic acid derivative and a metabolite of glycolithocholic acid. Glycolithocholic acid 3-sulfate inhibits replication of HIV-1 in vitro. Glycolithocholic acid 3-sulfate can be used for the research of HIV infection and gallbladder disease[1][2].
ABX464 is a potent anti-HIV agent. ABX464 inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) with an IC50 ranging between 0.1 μM and 0.5 μM.
Acriflavine hydrochloride (Acriflavinium chloride hydrochloride) is a fluorescent acridine dye that can be used to label nucleic acid[1][2]. Acriflavine hydrochloride is an antiseptic. Acriflavine hydrochloride is a potent HIF-1 inhibitor, with antitumor activity. Acriflavine hydrochloride has antimicrobial and antiviral activities[3][4][5]. Acriflavine hydrochloride is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2[6]
Decanoyl-RVKR-CMK (DecRVKRcmk) TFA inhibits over-expressed gp160 processing and HIV-1 replication[1].
Antiparasitic agent-18 (compound 3a) is active and selective against the T. brucei (EC50=0.4 μM), T. cruzi (EC50=0.21 μM), and L. donovani (EC50=0.26 μM). Antiparasitic agent-18 has potent antiprotozoal activity[1].
Histatin-8 is a part of the Histatin-3 central sequence and is known as hemagglutination-inhibiting peptide. Histatin-8 is a potent anti-fungal peptide. Histatin-8 shows antimicrobial activity against yeast strains. Histatin-8 can be used for oral thrush research[1][2].
Brevinin-1Ea is an antimicrobial peptide derived from the skin secretions of Rana esculenta[1].
Morusin is a prenylated flavonoid isolated from M. australis with various biological activities, such as antitumor, antioxidant, and anti-bacteria property. Morusin could inhibit NF-κB and STAT3 activity.
WU-04 is a non-covalent inhibitor of SARS-CoV-2, targeting the 3CLpro protein. WU-04 has high inhibitory effect on the 3CLpro protein of 6 SARS-CoV-2 variants (Alpha, Beta, Gamma, Delta, Lambda and Omicron) and 2 coronaviruses (SARS-CoV and MERS-CoV)[1].
Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ[1][2].
MptpB-IN-1 (Compound 13) is a potent and orally active inhibitor of MptpB. Mycobacterium tuberculosis protein-tyrosine-phosphatase B (MptpB) is a secreted virulence factor that subverts antimicrobial activity in the host. MptpB-IN-1 reduces multidrug-resistant mycobacterium tuberculosis survival and infection burden[1].
Cefepime hydrochloride is a cephalosporin antibiotic drug. Cefepime hydrochloride has inhibitory activity against human serum paraoxonase-1 (hPON1) with an IC50 value of 21.115 mM[1].
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].
(+)-Sorokinianin is a phytotoxin from an isolate of Bipolaris sorokiniana[1].
XZ426 is a potent integrase strand transfer inhibitor with anti- HIV activity[1].
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].
Undecane has anti-allergic and anti-inflammatory activities on sensitized rat basophilic leukemia (RBL-2H3) mast cells and HaCaT keratinocytes. In sensitized mast cells, Undecane inhibits degranulation and the secretion of histamine and TNF-α[
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]
LL-37, Human is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity[1]. LL-37, Human could help protect the cornea from infection and modulates wound healing[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.
Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin is an oral corticosteroid for asthma study[1][2][3].
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].