Antifungal agent 48 (Example 308) is an antifungal agent. Antifungal agent 48 is active against Cryptococcus neoformans with a MIC value of 11 μM[1].
Triclocarban is an antimicrobial agent used in personal cleaning products.
Haemanthamine is a crinine-type alkaloid isolated from the Amaryllidaceae plants with potent anticancer activity. Haemanthamine targets ribosomal that inhibits protein biosynthesis during the elongation stage of translation. Haemanthamine has pro-apoptotic, antioxidant, antiviral, antimalarial and anticonvulsant activities[1][2].
Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids, cruciala component of the cell wall of the Mycobacterium tuberculosis complex.In vitro: inhibits the synthesisi of mucolic acids, cruciala component of the cell wall of the Mycobacterium tuberculosis complex.[1]In in-vitro studies, delamanid shows more potent antibacterial activity against drug-susceptible and drug-resistant strains of M. tuberculosis.[2] Delamanid do not affect rifampin, pyrazinamide, and isoniazid exposure; the ethambutol AUCτ and Cmax values are about 25% higher with delamanid coadministration. [3] In vivo: Twice-daily oral dosing of delamanid at 30 mg kg-1 for 5 days resulted in sterile cures in a mouse model of VL. [4]
Astromicin (KW-1070) is a water-soluble aminoglycoside antibiotic that can be isolated from the genus Micromonospora. Astromicin exhibits broad spectrum antibacterial activity against gram positive and negative bacteria[1][2][3].
Gentamicin C1a is the precursor of the semi-synthetic antibiotic Etimicin, and has antibacterial activity. Gentamicin C1a is the major component of the Gentamicin complex[1][2].
Cefamandole Sodium Salt is a second-generation broad-spectrum cephalosporin antibiotic.
KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM[1].
LW3 is a potent antifungal agent. LW3 has antifungal activity with EC50 values of 0.54, 0.09, 1.52, and 2.65 mg/L against B. cinerea, R. solani, S. sclerotiorum, and F. graminearum, respectively[1].
NHC-diphosphate is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a diphosphate form[1]. NHC is a pyrimidine ribonucleoside and behaves as a potent anti-virus agent. NHC effectively inhibits the replication of venezuelan equine encephalitis virus (VEEV), Chikungunya virus (CHIKV) and hepatitis C virus (HCV)[1].
ABT-072 is a nonnucleoside NS5B polymerase inhibitor and a candidate drug evaluated for treatment of hepatitis C virus.
YH-53 is a potent 3CLpro inhibitor with Ki values of 6.3 nM, 34.7 nM for SARS-CoV-1 3CLpro and SARS-CoV-2 3CLpro, respectively. YH-53 strongly blocks the SARS-CoV-2 replication. YH-53 is a peptidomimetic compound with a unique benzothiazolyl ketone. YH-53 has the potential for COVID-19 research[1][2].
HBV Seq1 aa:63-71 is the fragment of hepatitis B virus (HBV)[1].
Tecovirimat(ST-246) is an orally bioavailable antipoxvirus compound; potent and selective active against multiple orthopoxviruses with EC50 about 10 nM.IC50 value: 10 nM [1]Target: antipoxvirusin vitro: ST-246 targets the cowpox virus V061 gene, which encodes a major envelope protein homologous to the vaccinia virus F13L gene product. The antiviral potency and selectivity of ST-246 was measured in CPE assays against a panel of DNA- and RNA-containing viruses. In these assays, the EC50 for inhibition of vaccinia virus was determined to be 0.01 μM, while the EC50 values for inhibition of unrelated viruses were >40 μM [1]. ST-246 was evaluated for activity against cowpox virus (CV), vaccinia virus (VV), and ectromelia virus (ECTV) and had an in vitro 50% effective concentration (EC50) of 0.48 microM against CV, 0.05 microM against VV, and 0.07 microM against ECTV. The selectivity indices were >208 and >2,000 for CV and VV, respectively. The in vitro antiviral activity of ST-246 was significantly greater than that of cidofovir, which had an EC50 of 41.1 microM against CV and 29.2 microM against VV, with selectivity indices of >7 and >10, respectively [2]. in vivo: Mice were treated with placebo (vehicle), ST-246 administered by oral gavage at 50 mg/kg twice a day (b.i.d.) for 14 days, or CDV administered as a single intraperitoneal (i.p.) injection at 100 mg/kg. ST-246-treated mice mounted a protective immune response to vaccinia virus infection [1]. ST-246 administered once daily by oral gavage to mice infected intranasally with CV beginning 4 h or delayed until 72 h postinoculation was highly effective when given for a 14-day duration using 100, 30, or 10 mg/kg of body weight. When 100 mg/kg of ST-246 was administered to VV-infected mice, a duration of 5 days was sufficient to significantly reduce mortality even when treatment was delayed 24 h postinoculation. Viral replication in liver, spleen, and kidney, but not lung, of CV- or VV-infected mice was reduced by ST-246 compared to levels for vehicle-treated mice [2].
Omadacycline-d9 is a deuterated aminomethylcycline omadacycline (HY-14865). Omadacycline is an orally active antibacterial agent and tetracycline antibiotic. Omadacycline binds to the 30S ribosomal subunit to inhibit bacterial protein synthesis. Omadacycline tosylate is indicated for the study of acute bacterial skin and skin structure infections, infectious pneumonia and urinary tract infections.
MAC13243, an antibacterial agent, is a likely inhibitor of the bacterial lipoprotein targeting chaperone, LolA.IC50 Value: Target: AntibacterialMAC13243, a molecule that belongs to a new chemical class and that has a unique mechanism and promising activity against multidrug-resistant Pseudomonas aeruginosa. MAC13243 inhibits the function of the LolA protein and represents a new chemical probe of lipoprotein targeting in bacteria with promise as an antibacterial lead with Gram-negative selectivity.
Resistomycin, a pentacyclic polyketide antibiotic, possesses anticancer activity and induces apoptosis[1][2][3][4].
Pyrindamycin B is an antibiotic, actives against gram-positive and gram-negative bacterias, and exhibits strong therapeutic effects against both drug-sensitive and resistant cells of P388 leukemia in mice[1].
Dermaseptin-S5 is an antimicrobial peptide derived from frog skin against filamentous fungi[1].
FG944 (FG-944) is a potent selective LpxC inhibitor with MIC50 of 0.5 ug/mL against K.pneumoniae, synergizes with rifampin in carbapenem resistant K. pneumoniae and E. coli.
Josamycin (EN-141) is a macrolide antibiotic exhibiting antimicrobial activity against a wide spectrum of pathogens, such as bacteria. The dissociation constant Kd from ribosome for Josamycin is 5.5 nM.
Diamthazole (Dimazole) is an antifungal agent. Diamthazole can be used for the research of infection[1].
Iodobananin is an effective inhibitor of the ATPase activity of the SARS Coronavirus helicase with an IC50 value of 0.54 μM.
Ofloxacin-d8 (Hoe-280-d8) is the deuterium labeled Ofloxacin. Ofloxacin (Hoe-280) is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase.
Sinapaldehyde, isolated from the stems of Rhodamnia dumetorum, exhibits moderate antibacterial against Methicillin resistant S. aureus (MRSA) and E. coli with MIC values of 128 and 128 μg/mL[1].
Marbofloxacin is a potent antibiotic of which depends upon its inhibition of DNA-gyrase. Marbofloxacin is a synthetic, broad spectrum bactericidal agent.Target: DNA-gyraseMarbofloxacin is a third-generation fluoroquinolone for veterinary use, the antimicrobial of which depends upon its inhibition of DNA-gyrase and topoisomerase IV. With a broad spectrum bactericidal activity and good efficacy, marbofloxacin is indicated for dermatological, respiratory and urinary tract infections due to both Gram-positive and Gram-negative bacteria and Mycoplasma [1].Administration of Marbofloxacin at 6 mg/kg once daily for 7 days in a Staphylococcus aureus infection in tissue cages in ponies is not effective for the elimination of S. aureus infections from secluded sites [2]. The pharmacokinetic properties of marbofloxacin were investigated in 6 horses after i.v., subcutaneous and oral administration of a single dose of 2 mg/kg bwt and the minimal inhibitory concentrations (MIC) assessed for bacteria isolated from equine infectious pathologies. The clearance of marbofloxacin was mean +/- s.d. 0.25 +/- 0.05 l/kg/h and the terminal half-life 756 +/- 1.99 h. The marbofloxacin absolute bioavailabilities after subcutaneous and oral administration were 98 +/- 11% and 62 +/- 8%, respectively. Considering the breakpoint values of efficacy indices for fluoroquinolones, a marbofloxacin dosage regimen of 2 mg/kg bwt/24 h by i.v., subcutaneous or oral routes was more appropriate for enterobacteriaceae than for S. aureus [3]. Toxicity: cramps; vomiting; anorexia; soft stools; diarrhoea
Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells.
KAMP-19, a keratin-derived antimicrobial peptide, is an antimicrobial peptide against P. aeruginosa. [1].
Taribavirin hydrochloride is an inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus[1]. Taribavirin hydrochloride is a Ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia[2].
7-Deaza-2',3'-dideoxyguanosine (7-Deaza-ddG) is a 2′,3′-dideoxynucleoside 5′-triphosphate, which can inhibit HIV-1 reverse transcriptase with a Ki of 25 nM[1].