Walrycin B is a novel antibacterial compound specifically targeting the essential WalR response regulator.IC50 value: 0.39 ug/ml (MIC for B. subtilis 168); 3.13 ug/ml (MIC for S. aureus N315) [1]Target: bacterial WalR response regulator; AntibacterialWalrycin B is known as an analog of toxoflavin (a phytotoxin from Burkholderia glumae), which has been shown to have a strong MIC for B. subtilis and S. aureus but whose mode of action is not clear. The compound could also interact with WalR to cause bactericidal effects. Walrycins are a new class of potent small molecule compounds that kill bacterial cells by targeting the RR WalR and inhibiting this essential signal transduction pathway. They not only have therapeutic potential but will also prove to be useful reagents for the further study of the WalK/WalR TCS. Walrycin B target WalR andlead to cell death in both B. subtilis and S. aureus.
Solanesol is an aliphatic terpene alcohol mainly found in Solanaceous plants, with anti-inflammatory, neuroprotective, and antimicrobial activities[1].
Pleurocidin is an antibacterial peptide derived from skin secretions of Winter Flounder[1].
Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity.
Broxaldine is an antiprotozoal drug.
L 696229 is a specific inhibitor ofhuman immunodeficiency virus type 1 (HIV-1)reverse transcriptase (RT) activity that possesses antiviral activity[1].
FtsZ-IN-1 is a potent FtsZ inhibitor with quinolinium ring. FtsZ-IN-1 has stronger antibacterial activity against Gram-positive bacteria with MICs of 0.5-8 μg/mL. FtsZ-IN-1 significantly causes cell elongation of B. subtilis by enhancing FtsZ polymerization. FtsZ-IN-1 exhibits low hemolytic toxicity and low tendency to induce drug resistance. FtsZ-IN-1 has against drug-resistant bacteria activity[1].
Defensin HNP 4 (HNP 4) is a single 11 amino acid long fragment of HNP-41-11. Defensin HNP 4 has inhibitory effect against multidrug-resistant and non-resistant strains[1].
Pentamidine isethionate is an antimicrobial agent for prevention and treatment of Pneumocystis pneumonia (PCP) caused by Pneumocystis jirovecii.
Icariside D2, isolated from Annona glabra fruit, inhibits angiotensin-converting enzyme. Icariside D2 shows significant cytotoxic activity on the HL-60 cell line with the IC50 value of 9.0 ± 1.0 μM. Icariside D2 induces apoptosis [1][2].
Tuberculosis inhibitor 12 (compound 12) is an oxadiazole derivative and an inhibitor of Mycobacterium tuberculosis. The inhibition rates of Tuberculosis inhibitor 12 (20 μM) on 7H9-Tw-OADC and 7H9-Tw-OADC reached 82% and 78% respectively[1].
5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells[1].
Methisazone (Marboran) is an antiviral agent that works by inhibiting mRNA and protein synthesis. Methisazone is also a SARS-CoV-2 (COVID-19) inhibitor. Methisazone is mainly used in pox viruses[1].
Nosiheptide (Multhiomycin), a thiopeptide antibiotic produced by Streptomyces actuosus, inhibits bacterial protein synthesis and bears a unique indole side ring system and regiospecific hydroxyl groups on the characteristic macrocyclic core. Nosiheptide has been widely used as a feed additive for animal growth[1][2].
MtTMPK-IN-4 (compound 2), a para-piperidine, is a potent mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 of 6.1 μM. MtTMPK-IN-4 is a potent tyrosinase inhibitor. MtTMPK-IN-4 is a potent antibacterial agent[1][2].
Triclosan-methyl is a transformation product of triclosan. Triclosan is a bactericide in personal care products such as toothpaste, shampoos, and soaps. Triclosan is also a stabilizing agent in a multitude of detergents and cosmetics[1].
Methasulfocarb is a fungicide compound.
Leachianone G is an antiviral flavonoid from the root bark of Morus alba L. Leachianone G shows potent antiviral activity against herpes simplex type 1 virus (HSV-1) with an IC50 value of 1.6 μg/mL[1].
Genkwanol C, a biflavonoid, has effective antiviral activity against respiratory syncytial virus (RSV) in vitro[1].
HIV-IN-4 (Compound 12) is a potent inhibitor of HIV. HIV-IN-4 shows promising anti-HIV activities[1].
HBV-IN-31 is a potent cccDNA (covalently closed circular DNA) inhibitor. HBV-IN-31 shows anti-HBV activity with an IC50 value of 0.13 µM for HBsAg. HBV-IN-31 inhibits cell growth[1].
Antibacterial agent 121 (Compound 10) is an antibacterial agent. Antibacterial agent 121 shows anti-mycobacterial and anti-inflammatory activities and can be used in Tuberculosis (TB) research[1].
Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria.
TXA6101 is a bacterial protein FtsZ (filamentous temperature-sensitive protein Z) inhibitor that inhibits bacterial division. TXA6101 has antimicrobial activity against MRSA isolates expressing either the G193D or G196S mutant FtsZ with the MIC value of 1 μg/mL, retains significant activity against the TXA707-resistant FtsZ mutant. TXA6101 can be used as a potential method against Gram-negative bacterial infections[1][2].
GSK3739936 (BMS-986180) is a potent, allosteric HIV-1 integrase (ALLINI), shows excellent potency in vitro against majority of the 124/125 variants (EC50=1.7 nM).
FLGFVGQALNALLGKL-NH2 is an antimicrobial peptide of frog origin. FLGFVGQALNALLGKL-NH2 has activity against Staphylococcus aureus ATCC 29213 (MIC=32 μM) [1].
Phosphatase-IN-1 (compound II-8), a propranolol (HY-B0573B) derivative, is a phosphatidate phosphatase (Pah) inhibitor. Phosphatase-IN-1 can binds to MoPah1, with an affinity constant of 19.8 μM. Phosphatase-IN-1 inhibits growth of plant pathogens and shows anti-fungal ability. Phosphatase-IN-1 is not toxic to rice seedlings and wheat heads[1].
Peritassine A, an alkaloid that could be isolated from Tripterygium wilfordii Hook. f., possesses anti-HIV activity[1][2].
CBS1117 is a virus entry inhibitor with an IC50 of 70 nM for influenza A viruses, A/Puerto Rico/8/34 (H1N1). CBS1117 interferes with the hemagglutinin (HA)-mediated fusion process[1].