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]
Pyromeconic acid is an antifungal substance[1].
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].
Monazomycin is a polyene-like antibiotic produced by Streptomyces. Monazomycin molecular weight is about 1200[1].
Mucrolidin is an eudesmane-type sesquiterpenoid isolated from aerial parts of homalomena occulta. Mucrolidin exhibits weak antibacterial activities when it compares to Rifampicin (HY-B0272)[1].
PI3Kδ-IN-13 (compound 89) is a PI3Kδ inhibitor (IC50=2.6 nM). PI3Kδ-IN-13 can be used in the research of cell proliferation diseases such as cancer, infection, inflammation and autoimmune diseases[1].
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].
Cheilanthifoline, an alkaloid, is isolated from Corydalis calliantha. Cheilanthifoline exhibits antiplasmodial activities against Plasmodium falciparum, with IC50s of 0.90 μg/mL and 1.22 μg/mL for wild type (TM4) and multidrug resistant (K1) strains, respectively[1].
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].
Panobinostat lactate is a potent and orally active non-selective HDAC inhibitor. Panobinostat lactate has antineoplastic activities. Panobinostat lactate effectively disrupts HIV latency. Panobinostat lactate induces cell apoptosis and autophagy. Panobinostat lactate can be used for the study of refractory or relapsed multiple myeloma[1][2][3][4][5].
LF11 is a peptide with antibacterial activity[1].
Dictamnine (Dictamine) has the ability to exert cytotoxicity in human cervix, colon, and oral carcinoma cells; A natural plant product has been reported to have antimicrobial activity against bacteria and fungi.IC50 value:Target: Dictamnine has antimicrobial activities against the model fungus Saccharomyces cerevisiae, with a minimum inhibitory concentration (MIC) value of 64 microg/ml [1]. Dic induced S phase cell cycle arrest at low concentration and cell apoptosis at high concentration in which loss of mitochondrial membrane potential (Δψmm) was not involved. In addition, inhibition of caspase-3 using the specific inhibitor, z-DQMD-fmk, did not attenuate Dic-induced apoptosis, implying that Dic-induced caspase-3-independent apoptosis [2].
Methyl indole-3-carboxylate is a natural product isolated from Sorangium cellulosum strain Soce895. Methyl indole-3-carboxylate shows a weak activity against the Gram-positive Nocardia sp with a MIC value of 33.33 μg/mL[1].
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].
Protocatechualdehyde (Catechaldehyde), a natural polyphenol compound isolated from the roots of radix Salviae Miltiorrhizae, is associated with a wide variety of biological activities and has been widely used in medicine as an antioxidant, anti-aging, an antibacterial and anti-inflammatory agent[1].
4-Methylcinnamic acid, a Cinnamic acid analog, can be used as a intervention catalyst for overcoming antifungal tolerance. 4-Methylcinnamic acid can improve the potency of cell wall-disrupting agents[1].
HBV-IN-16 is a potent inhibitor of covalently closed circular DNA (cccDNA). cccDNA serves as the template for viral RNA transcription and subsequent viral DNA generation. HBV-IN-16 is a quinoline derivative. HBV-IN-16 has the potential for the research of HBV infection (extracted from patent WO2019121357A1, compound 1)[1].
Catalpin is an iridoid that can be isoalted from Catalpae Fructus.Catalpin shows mutagenic activity towards Salmonella typhimurium strain TA100[1].
Tryptophanase, a bacterial enzyme, catalyzes degradation of tryptophan to indole, pyruvate and ammonia[1].
Chlorhexidine dihydrochloride is an antibacterial, used as an antiseptic and for other applications.
Interiotherin A is a lignan with a dibenzocyclooctadiene skeleton isolated from Kadsura interior. Interiotherin A inhibits HIV replication to exhibit anti-HIV activity, it has a role as a metabolite and an anti-HIV agent[1].
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].
HIV-1 inhibitor-20 is a potent HIV-1 inhibitor by non-classical isosteric replacement of amide to 1,2,4-oxadiazoles[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].
Fervenulin, isolated from a nematicidal actinomycete Streptomyces sp. CMU-MH021, has nematicidal activity and inhibits egg hatch and J2 mortality of M. incognita with MICs of 30 μg/mL and 120 μg/mL, respectively[1].
Mastoparan B is an antimicrobial peptide derived from hornet Vespa. Mastoparan B can cause the shape of red blood cells to change from normal disk-like to serrated[1].
Benzisothiazolone is an isothiazolone fungicide. Benzisothiazolone has growth inhibiting activity against E. coli ATCC 8739 and saccharornyces pombe NCYC 1354. Benzisothiazolone can be used in the study of growth inhibition model [1].
Fuberidazole (BAY 33172; Furidazole) is a fungicide. Fuberidazole shows a synergistic effect with cucurbituril (CB) macromolecules, such as CB7 and CB8. Studies have shown that, CB8 induces pKa shifts on Fuberidazole. Fuberidazole significantly inhibits the growth of B. cinerea[1].