L-739594 is a HIV-1 protease inhibitor, with an IC50 of 1.8 nM[1].
Ceftezole (CTZ) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole (CTZ) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity[1][2].
Octaethylene glycol monododecyl ether (C12E8) is an non-ionic detergent that can be used for membrane protein extraction. Octaethylene glycol monododecyl ether can solubilize the viral membrane of intact influenza virus[1][2].
Antiviral agent 25 (compound 6g) is a new non-peptide analog covalent inhibitor of SARS-CoV-2 3CLpro. Antiviral agent 25 has a strong inhibitory effect on SARS-CoV-2 3CLpro and SARS-CoV-2 PLpro with IC50 values of 0.118 µM, 0.448 µM, respectively. Antiviral agent 25 has antiviral effect on SARS-CoV-2 with an EC50 value of 7.249 µM[1].
1-Methyl-2-(8E)-8-tridecenyl-4(1H)-quinolinone is a potent antibacterial agent with an MIC50 value of 22 µM and an MIC90 value of 50 µM for Helicobacter pyloriStrain 51. 1-Methyl-2-(8E)-8-tridecenyl-4(1H)-quinolinone has the potential for the research of gastric and duodenal ulcers[1].
Polyphemusin I is a natural antimicrobial peptide with excellent antimicrobial activity against Gram-negative and Gram-positive bacteria. Polyphemusin I contains 18 amino acids and is stabilized into an amphiphilic, antiparallel β-hairpin by two disulfide bridges[1].
TH-Z145, a lipophilic bisphosphonate, is a FPPS inhibitor (IC50: 210 nM)[1].
Fluconazole (hydrate) is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections.Target: AntifungalFluconazole (hydrate) is the hydrate salt form of fluconazole, which is a triazole antifungal intended for oral treatment of superficial and systemic mycoses. In tests done in standard mycological media, the compound had minimal inhibitory concentrations against pathogenic Candida species that were usually in excess of 100 mg/l. Fluconazole inhibited branching and hyphal development in C. albicans at concentrations as low as 10(-6) M (0.3 mg/l), but miconazole and ketoconazole were still active in these tests at concentrations 100 times lower than this [1]. Oral fluconazole was not associated with a significantly increased risk of birth defects overall or of 14 of the 15 specific birth defects of previous concern. Fluconazole exposure may confer an increased risk of tetralogy of Fallot [2]. Fluconazole is predicted to be ineffective against Cryptococcus gattii in the koala as a sole therapeutic agent administered at 10 mg/kg p.o. every 12 h [3].Clinical indications: Balanitis; Candida infection; Cryptococcus infection; Cryptococcus neoformans meningitis; Dermatomycosis; Female genital tract infection; Fungal infection; Fungal respiratory tract infection; Fungal urinary tract infection; Prophylaxis; Tinea capitis; Tinea corporis; Tinea cruris; Tinea pedis .Toxicity: Symptoms of overdose include hallucinations and paranoid behavior.
Antitubercular agent-14 (Compound 1) is an antitubercular agent with an MIC of 0.3 µg/mL against M. tuberculosis[1].
Omodenbamab is an anti-SpA (Staphylococcal protein A) humanized monoclonal antibody with a KD value of 0.0467 nM. Omodenbamab circumvents a key S. aureus evasion mechanism by targeting the cell wall moiety Protein A (SpA). Omodenbamab can be used in research of S. aureus bloodstream infection[1].
BMS-707035 is an HIV-1 integrase (IN) inhibitor with an IC50 value of 15 nM. IC50 Value: 15 nMTarget: HIV IntegraseBMS-707035 was scheduled to be evaluated in a Phase II study to assess the antiretroviral activity, safety, pharmacodynamics, and pharmacokinetics in 50 HIV-infected subjects using a 10-day randomized, double-blind, placebo-controlled, ascending multiple-dose study design.
SARS-CoV-2-IN-17 (Compound 16) is a potent SARS-CoV-2 nucleocapsid protein (NPro) inhibitor. SARS-CoV-2-IN-17 exhibits potent anti-viral activity with the EC50 of 2.18 μM. SARS-CoV-2-IN-17 binds to NPro with the low KD value of 7.82 μM, suggesting that SARS-CoV-2-IN-17 is a potent NPro ligand[1].
Loracarbef-d5 is the deuterium labeled Loracarbef. Loracarbef, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class[1][2].
Hexahydrohippuric acid is a metabolite of Shikimate acid in both liver and kidney, under microbial metabolism effect. Hexahydrohippuric acid is made of cyclohexane carboxylic acid and glycinamide, and shows antibacterial activity[1][2].
Transtorine is a quinoline alkaloid, found from Ephedra transitoria, with antibacterial activity[1].
Allicin (diallyl thiosulfinate), a highly potent natural antimicrobial activity substance, inhibits growth of a variety of microorganisms, among them antibiotic-resistant strains[1].
D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).IC50 value: 23.8 μg/ml (EC50, in MT-4 cell ), 5.03 μg/ml (EC50, in C8166 cell)Target: HIV-1in vitro: D77 exhibits a highly specific binding affinity to HIV-1 integrase catalytic core domain.D77 induces a dramatic concentration-dependent decrease of α-galactosidase activity compared to the D77-untreated cells. D77 reveals a significant inhibition activity against the interaction of IN with IBD.
Diamthazole (Dimazole) hydrochloride is an antifungal agent. Diamthazole hydrochloride can be used for the research of infection[1].
Pikromycin is a macrolide antibiotic that has been found in S. venezuelae and active against E. coli, S. aureus and B. subtilis[1].
Macrocarpal D is a potent antibacterial agent. Macrocarpal D is a phloroglucinol dialdehyde diterpene derivatives that can be found in the leaves of Eucalyptus macrocarpa[1].
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive[1][2].
Sutezolid (PNU-100480) is an oxazolidinone antimicrobial being developed for the treatment of tuberculosis.Target: AntibacterialSutezolid is a much-awaited drug candidate for treatment of Mycobacterium tuberculosis. [1] Sutezolid is an oxazolidinone antibiotic currently in development as a treatment forextensively drug-resistant tuberculosis. Sutezolid is a linezolid analog with superior bactericidal activity against Mycobacterium tuberculosis in the hollow fiber, whole blood and mouse models. Like linezolid, it is unaffected by mutations conferring resistance to standard TB drugs. This study of sutezolid is its first in tuberculosis patients.[2]
STC314 is a small polyanion that interact electrostatically with histones. STC314 blocks disruption of lipid-bilayers by histones that inhibits the cytotoxic, platelet-activating and erythrocyte-damaging effects of histones. STC314 has anti-infective effects and can be uesd for sepsis research[1].
HCV-IN-41 (compound 4) is a highly potent hepatitis C virus (HCV) inhibitor with an EC50 value of 0.006762 nM, 5.183 nM, 1.365 nM and 142.2 nM for HCV genotype 1b, 2a, 3a and 4a, respectively. HCV-IN-41 reduces HCV RNA replication[1].
Gliovirin is an antibiotic active against Pythium ultimum. Gliovirin is isolated from Gliocla-dium virens. Gliovirin may be derived from L,L-phenylalanine anhydride, which is also isolated from G. virens[1].
Sertaconazole nitrate is a topical broad-spectrum antifungal that is developed to provide an additional agent for the treatment of superficial cutaneous and mucosal infections.Target: AntifungalSertaconazole nitrate reduces the release of cytokines from activated lymphocytes and mitigated inflammation in animal models of irritant contact dermatitis and neurogenic inflammation in a dose-dependent fashion. Sertaconazole nitrate is found to inhibit the proliferation of stimulated human lymphocytes with IC50 of 4 μg/mL [1]. Sertaconazole nitrate inhibits ergosterol synthesis by blockade of the P450-dependent enzyme pathway that catalyzes the methylation of lanosterol to ergosterol, thus inhibits fungal cell growth. Sertaconazole nitrate binds directly to nonsterol lipids in the membrane, which interferes with the regulation of the permeability of fungal cell membranes, thus induces fungal cell death [2].The mean ear weight of Tetradecanoyl phorbol acetate (TPA)-challenged murine treated with sertaconazole nitrate (1%) is 7.23 mg compared with 14.7 mg for controls, indicating a statistically significant reduction in irritant dermatitis. Sertaconazole nitrate 1% elicits a significant reduction in Resiniferatoxin-induced ear edema when compared with controls in CD-1 mice. Topical treatment with sertaconazole nitrate 1% significantly inhibits contact hypersensitivity and decreases the content of the pro-inflammatory cytokines TNFα, IL-2, and IFNγ in oxazolone exposed murine skin [1]. Clinical trials with sertaconazole nitrate cream 2% show efficacy in the treatment of superficial cutaneous fungal infections [2]. Sertaconazole reduces inflammation via inducing PGE2 production and the COX-2 inhibitor blocks sertaconazole from exerting its anti-inflammatory effects in a mouse model of TPA-induced ear edema [3].
BM635 is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 has an MIC50 of 0.12 μM against M. tuberculosis H37Rv.
Transketolase-IN-4 is a potent transketolase inhibitor (IC50=3.9 μM). Transketolase-IN-4 inhibits tumor cell proliferation of SW620, LS174T, and MIA PaCa-2. Transketolase-IN-4 is a possible Mycobacterium tuberculosis DXS inhibitor, with an IC50 value of 114.1 μM[1][2].
Beludavimab (BMS 4182137; VIR 7832) is a monoclonal antibody targeting the spike glycoprotein of SARS-CoV-2. Beludavimab binds to recombinant spike protein receptor-binding domain (S-RBD) with an EC50 value of 14.9 ng/mL and a Kd of 0.21 nM[1].
Pseudane IX, a compound isolated from the leaves of Ruta angustifolia, has strong anti-HCV activity with an IC50 value of 1.4 μg/mL. Pseudane IX reduces HCV RNA replication and viral protein synthesis levels[1].