Triticonazole is a triazole pesticide. Triticonazole an azole fungicide, shows endocrine disrupting activities[1][2].
Benzothiazole is a natural occurring heterocyclic nuclei. Benzothiazole nucleus possesses a number of biological activities such as anticancer, antimicrobial, antidiabetic, anti-inflammatory, antiviral, antileishmanial, and antiviral[1].
Isorhamnetin-3-O-sophoroside-7-O-rhamnoside, the major flavonol glycoside, is isolated from sea buckthorn (Hippophaë rhamnoides). Isorhamnetin-3-O-sophoroside-7-O-rhamnoside has the algicidal activity against the growth of the harmful microalgae[1][2].
VNRX-5133 is a cyclic boronate β-lactamase inhibitor. VNRX-5133 has direct inhibitory activity against serine-active site β-lactamases (Ser-BL) and metallo-β-lactamases (MBL). VNRX-5133 is highly active against multidrug-resistant (MDR)-K. pneumonia and P. aeruginosa clinical isolates[1].
Danoprevir is a NS3/4A protease inhibitor for hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM. The inhibition effect on HCV genotypes 1A/1B/4/5/6 is approximately 10-fold higher than 2B/3A.
Antibacterial agent 38 is an antibacterial agent extracted from patent WO2015063714A1, compound C. Antibacterial agent 38 can be used for the research of bacterial infections[1].
PLpro/RBD-IN-1 (compound 5) is a dual SARS-CoV-2 PLpro and spike protein RBD inhibitor with IC50s of 7.197 μM and 8.673 μM, respectively[1].
Euparin, a monomeric compound of Benzofuran, is a reactive oxygen species (ROS) inhibitor. Euparin shows antiviral activity against poliovirus, and also has antidepressant effects[1][2].
Tirilazad is a nonglucocorticoid, 21-aminosteroid that inhibits lipid peroxidation. Tirilazad can attenuate brain or spinal cord injury caused by trauma, stroke, ischemia and reperfusion injury. Tirilazad has antiviral activities against nCoV. Tirilazad is neuroprotective for ischaemic stroke, can be used for subarachnoid hemorrhage research[1][2][3].
Antibacterial agent 105 (Compound 17) is a phenanthrolinic analog of quinolones show antibacterial activity against M. tuberculosis with antibacterial activity (MIC90=2.64 μM)。Antibacterial agent 105 exhibits antibacterial activities against different bacterial species with MIC90s of 11.18, 11.18，0.70，1.40，44.70, and 22.35 μM for M. smegmatis, M. aurum, M. marinum,BCG, E. aerogenes and S. aureus, respectively[1].
Kanamycin (Kanamycin A) is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin shows good inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia[1][2][3][4].
Borrelidin (Treponemycin) is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei, which acts as an inhibitor of bacterial and eukaryal threonyl-tRNA synthetase, can target ALL cell lines by inducing apoptosis and mediating G(1) arrest. Borrelidin (Treponemycin) is an inhibitor of a cyclin-dependent kinase (CDK) of the budding yeast, Cdc28/Cln2 with an IC50 of 24 μM. Borrelidin (Treponemycin) is a potent angiogenesis inhibitor with an IC50 of 0.8 nM for capillary tube formation, and induces apoptosis of the tube-forming cells. Borrelidin (Treponemycin) has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum[1][2][3].
ML336 is quinazolinone-based inhibitor against venezuelan equine encephalitis virus (VEEV), with IC50s of 32, 20, and 42 nM for VEEV TC-83 CPE , VEEV V3526 CPE, VEEV Wild Type CPE, respectively. ML336 potently inhibits a VEEV-induced cytopathic effect in three strains of the virus (TC-83, V3526, and wild type Trinidad donkey) in the low nanomolar range[1].
Garenoxacin mesylate hydrate is a novel oral des-fluoro(6) quinolone with potent antimicrobial activity, against common respiratory pathogens, including resistant strains.
HBV-IN-20 is a potent and oral active HBV inhibitor with an EC50 of 0.46 µM. HBV-IN-20 is a typical type II CpAM (core protein assembly modulators)[1].
GSK2838232 inhibit HIV reverse transcriptase activity across a broad panel of HIV-1 isolates, extracted from patent WO/2013090664A1, compound51.
PqsR/LasR-IN-3 (Compound 7a) is a potent inhibitor of PqsR and LasR systems in P. aeruginosa. PqsR/LasR-IN-3 also inhibits hERG with the IC50 of 109.01 µM[1].
CDK9-IN-30 is a CDK9 inhibitor that inhibits HIV-1 viral replication[1].
Filastatin is a long-lasting inhibitor of Candida albicans filamentation. Filastatin inhibits adhesion by multiple pathogenic Candida species with an IC50 of ~3 μM in the GFP-based adhesion assay. Filastatin inhibits fungal adhesion to polystyrene and human cells, the yeast-to-hyphal morphological transition, induction of the hyphal-specific HWP1 promoter. Filastatin has potent antifungal effect[1].
Amphotericin B is a polyene antifungal agent against a wide variety of fungal pathogens. It binds irreversibly to ergosterol, resulting in disruption of membrane integrity and ultimately cell death.
Torcitabine (2'-Deoxy-L-cytidine) is an antiviral agent. Torcitabine has the potential for chronic hepatitis B virus infection treatment[1][2].
Vitamin K5 (hydrochloride) is a naphthoquinones compound, shows trichomonacidal activity in vitro. Vitamin K5(hydrochloride) can be used for the research of anti-infection[1].
IQP-0528 is a highly potent nonnucleoside reverse transcriptase inhibitor (NNRTI). IQP-0528 shows nanomolar activity against both HIV-1 and HIV-2, with an HIV-1 EC50 of 0.2 nM and an HIV-2 EC50 of 100 nM[1].
Ebselen oxide, the selenone analogue of Ebselen, covalently modifies diguanylate cyclase (DGC) to inhibit c-di-GMP-receptor interactions and reduces DGC activity. Ebselen oxide also inhibits alginate production (IC50=14 μM) by Pseudomonas aeruginosa. Ebselen oxide inhibits HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9 (IC50 ranging from 0.2 to 4.7 μM)[1][2][3].
MCB-3681 is the antibacterial Oxaquin's active substance, active against gram-positive bacterium[1].
Stachartin B is a phenylspirodrimane-type analogue. Stachartin B can be isolated from the tin mine tailings-associated fungus Stachybotrys chartarum[1].
Methyl 2-amino-5-bromobenzoate (compound 8/12) can be used for synthesis of 2-benzamidobenzoic acids, which are known FabH inhibitors. The derivates also inhibit PqsD, the pqs quorum sensing (QS) system of Pseudomonas aeruginosa, involving the production of a number of virulence factors and biofilm formation[1].
Lefitolimod (MGN 1703) is a DNA-based TLR9 agonist and an immune surveillance reactivator. Lefitolimod induces HIV-specific immune responses and can be used for the research of cancer and HIV-1[1][4].
Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibits JNK and p38MAPK signals. Lucidone also has inhibitory activity against Dengue virus (DENV) (EC50=25 μM)[1][2].
Antitubercular agent-32 is a derivate of Benzothiazinone (HY-13579A), inhibits M. tuberculosis, and shows improved metabolic stability and enhanced water solubility. Antitubercular agent-32 exerts antitubercular effect by targeting decaprenylphosphoryl-β-D-ribose 2’-oxidase (DprE1, IC50=3.9 μM)[1].